- Fluorogenic recognition of Zn2+, Cd2+ by a new Pyrazoline-based Multi-Analyte chemosensor and its application in live cell imaging
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A novel multi-response pyrazoline-based fluorescent probe 1 was designed and synthesized with a very simple molecular structure, which exhibited high sensitivity for detecting Zn2+ and Cd2+ in ethanol aqueous solution state based on
- Guo, Hui-Chen,Ma, Chun-Mei,Niu, Wei-Ya,Xue, Ji-Jun,Yang, Yun-Shang,Zhang, Ying-Peng
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Read Online
- An ESIPT coupled AIE fluorescent probe for biothiols detection and imaging based on a chalcone fluorophore
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Biothiols are closely related to numerous physiological and pathological processes in living organisms and cells. Fluorescent probes are powerful tools for sensitive detection and imaging of biothiols in biological samples. In this work, we developed a no
- Dai, Fangfang,Wang, Chao,Wang, Tingting,Yang, Fangzhou,Zhao, Min
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Read Online
- NIR luminescence for the detection of latent fingerprints based on ESIPT and AIE processes
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In this paper, a facile near infrared (NIR, 650-900 nm) probe 4-dimethylamino-2′-hydroxychalcone (NIR-LP) based on the excited state intramolecular proton transfer (ESIPT)-aggregation induced emission (AIE) processes for the detection of the latent finger
- Jin, Xiaodong,Dong, Libo,Di, Xiaoyu,Huang, Hai,Liu, Jingning,Sun, Xiaoli,Zhang, Xueqiong,Zhu, Hongjun
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Read Online
- An ultrasensitive rapid-response fluorescent probe for highly selective detection of HSA
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A fluorescent probe HCAB based on twisted intramolecular charge transfer (TICT) mechanism has been designed and synthesized by introducing benzoyl moiety to 4-dimethylamino-2′-hydroxychalcone. HCAB showed excellent selectivity towards human serum albumin
- Li, Pengbo,Wang, Yiru,Zhang, Shufang,Xu, Liang,Wang, Gongchen,Cui, Jingnan
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Read Online
- Flavone-based hydrazones as new tyrosinase inhibitors: Synthetic imines with emerging biological potential, SAR, molecular docking and drug-likeness studies
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Targeting tyrosinase (TYR), a key enzyme responsible for melanogenesis disorders, is a well-known approach utilized for the development of melanogenesis inhibitor. A variety of dermatological disorders and microbial skin infections can cause hyperpigmentation. Hence, exploring new scaffolds for the treatment of melanogenesis disease is an inspiring goal. In this context, a series of varyingly substituted flavone-based hydrazones have been designed, synthesized and characterized successfully. The present study describes the discovery of novel mushroom tyrosinase inhibitors (TIs) for treating hyperpigmentation. In due course, flavone scaffold has been incorporated into the novel chemotypes that exhibit in vitro inhibitory effects against mushroom tyrosinase for the purpose of discovering anti‐melanogenic agents. Biological investigations of prepared analogs herein demonstrated moderate to excellent activity against most of the fungal-bacterial strains and their activity is comparable to those of commercially available antibiotics i.e., Ciprofloxacin and Ketoconazole. Based on in vitro tyrosinase inhibitory assay, some compounds exhibited potent inhibition particularly, 3g (IC50 = 1.40 ± 0.16 μM), 3j (IC50 = 0.95 ± 0.07 μM), 3o (IC50 = 1.13 ± 0.11 μM), and 3q (IC50 = 1.01 ± 0.1 μM) showed best inhibition i.e., 0.7, 0.5, 0.6 and 0.5 folds, respectively, than kojic acid (IC50 = 1.79 ± 0.6 μM). Lineweaver-Burk plots demonstrated that the most potential derivative 3j tyrosinase inhibition proceeds via non-competitive pathway and the Michaelis-Menton constant (Km) value is 0.0265. Molecular modeling was performed for all tested analogs (3a–3q) using a model of mushroom tyrosinase to find crucial binding modes liable for inhibitory activity. The SARs were preliminarily examined, and the docking study revealed that analogs 3j, 3o and 3p had a strong binding association to tyrosinase (2Y9X). Furthermore, a drug-likeness study was employed and confirmed the favorable activity of the new analogs as a new anti-tyrosinase agent.
- Alsantali, Reem?I.,Mughal, Ehsan?Ullah,Naeem, Nafeesa,Alsharif, Meshari?A.,Sadiq, Amina,Ali, Anser,Jassas, Rabab.?S.,Javed, Qamar,Javid, Asif,Sumrra, Sajjad Hussain,Alsimaree, Abdulrahman?A.,Zafar, Muhammad?Naveed,Asghar, Basim?H.,Altass, Hatem?M.,Moussa, Ziad,Ahmed, Saleh?A.
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- A fluorescence turn-on probe for hydrogen sulfide and biothiols based on PET & TICT and its imaging in HeLa cells
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In this paper, a photoinduced electron transfer (PET)& twisted intramolecular charge transfer (TICT)-based fluorescent probe (1) for detecting biothiols (GSH/Cys/Hcy) and hydrogen sulfide with fluorescence turn on was developed. The probe could recognize
- Jin, Xiaodong,Zhang, Caiting,Zhang, Xueqiong,Zhong, Hui,Zhu, Hongjun
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- A simple chalcone molecular rotor for specific fluorescence imaging of mitochondrial viscosity changes in living cells
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Mitochondrial viscosity is related to numerous physiological processes such as solute diffusion, enzyme catalysis, protein folding, translocation, and conformation change. It is significant to evaluate and monitor the mitochondrial viscosity changes in li
- Dai, Fangfang,Ma, Yangmin,Niu, Zhuolan,Wang, Chao,Wang, Tingting,Zhang, Wenqing,Zhao, Min
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- Experimental and theoretical insights into the photophysical and electrochemical properties of flavone-based hydrazones
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A small library of flavone-based hydrazones has been designed, synthesized and characterized. In this context, thirteen flavone hydrazones (3a-3 m) were synthesized by the acid-catalyzed condensation of flavone with 2,4-dinitrophenylhydrazine (2,4-DNPH) and characterized by different spectral techniques (IR, UV–Vis, NMR and mass spectrometry). The electrochemical, photophysical and theoretical investigations of such type of compounds are hitherto unknown. The electrochemical behavior of these hydrazones at a platinum electrode has been analyzed by cyclic voltammetry (CV) and was investigated at 200, 100 and 40 mVs?1 in acetonitrile (CH3CN). These hydrazones showed a quasi-reversible redox reaction. The oxidation–reduction reactive sites of these derivatives were located via geometry optimization using density functional theory (DFT) at the B3LYP/3–21 g in the Guassian-09 level of theory. Moreover, the target compounds exhibited interesting fluorescent properties. Owing to their excellent photophysical and redox results, a detailed structure-property relationship was established to assess the substituents impact and their position on the physicochemical and electronic properties. All the experimental results were in accordance with the computational studies.
- Ahmed, Ishtiaq,Ahmed, Safeer,Ahmed, Saleh A.,Alsantali, Reem I.,Alsharif, Meshari A.,Altaf, Ataf Ali,Altass, Hatem M.,Jassas, Rabab. S.,Kausar, Samia,Mughal, Ehsan Ullah,Mumtaz, Amara,Naeem, Nafeesa,Obaid, Rami J.,Sadiq, Amina,Zafar, Muhammad Naveed
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- Glycolytic inhibition and antidiabetic activity on synthesized flavanone scaffolds with computer aided drug designing tools
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Background: Diabetes mellitus is a challengeable metabolic disorder that leads to a group of complications when the HbA1c level is not maintained. Most of the existing drugs avail-able in the market in long-term use may lead to serious adverse effects. He
- Kiruthiga, Natarajan,Saravanan, Govindaraj,Selvinthanuja, Chellappa,Sivakumar, Thangavel,Srinivasan, Kulandaivel
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p. 574 - 592
(2021/09/30)
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- Synthesis and kinetic study for the interconversion process of some 2'-hydroxychalcones to their corresponding flavanones
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In this work, five substituted2'-Hydroxychalconeswere prepared using Claisen - Schmidt condensation and used as a synthone for substituted flavanones via base catalyzed isomerization process. The latter process has been studied kinetically using HPLC technique in (8:2) (CH3CN:CH3OH) medium at different temperatures (298 K - 318 K). The obtained results were inconsonance with a four-step mechanism which considered the existence of phenoxide ion as the key intermediate. The reaction was achieved as a pseudo first order reaction in which the rate of the studied compounds followed the sequence 1>2>3>4>5, and the activation energy had the same sequence for these compounds. The reaction rate was affected by the electronic behavior of the different substituents at ring B since they played an important role in the stability of the intermediate that led to the final product.
- Majed, Zainab Waleed,Said, Said Abdelqader,Shareef, Omar Adil
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p. 4379 - 4386
(2020/12/09)
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- Chloro and bromo-pyrazole curcumin Knoevenagel condensates augmented anticancer activity against human cervical cancer cells: design, synthesis, in silico docking and in vitro cytotoxicity analysis
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With an endeavor to develop novel curcumin analogs as potential anti-cancer agents, we designed and synthesized a series of Knoevenagel condensates by clubbing pyrazole carbaldehydes at the active methylene carbon atom of the curcumin backbone. Molecular docking studies were carried out to target the proposed derivatives on human kinase β (IKKβ), a potential anti-cancer target. The chloro derivative displayed five hydrogen bond interactions with a docking score of ?11.874 kcal/mol higher than curcumin (docking score = ?7.434 kcal/mol). This was supported by the fact that the propellant shaped derivatives fitted aptly into the binding pocket. Molecular simulations studies were also conducted on the lead molecule and the results figured out that the stable complexes were developed as the minimal deviations per residue of protein within the range of 0.11–0.92 ?. The screened compounds were synthesized, characterized and evaluated in vitro for cytotoxicity against cervical cancer cell line, HeLa using standard cell proliferation assay. Chloro derivative and bromo analog demonstrated IC50 (half maximal inhibitory concentration) value of 14.2 and 18.6 μg/ml, respectively, significantly lower than 42.4 μg/ml of curcumin and higher than 0.008 μg/ml of paclitaxel. Induction of apoptosis was evaluated in the terms of cleavage of caspase-3 enzyme and they also exhibited 69.6 and 65.4% of apoptosis significantly higher than 19.9% induced by curcumin. In conclusion, chloro and bromo derivatives must be evaluated under a set of stringent in vitro and in vivo parameters for translating in to a clinically viable product. Communicated by Ramaswamy H. Sarma.
- Chaudhary, Monika,Kumar, Neeraj,Baldi, Ashish,Chandra, Ramesh,Arockia Babu,Madan, Jitender
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p. 200 - 218
(2019/03/08)
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- Bismuth(III) Flavonolates: The Impact of Structural Diversity on Antibacterial Activity, Mammalian Cell Viability and Cellular Uptake
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A series of homoleptic and heteroleptic bismuth(III) flavonolate complexes derived from six flavonols of varying substitution have been synthesised and structurally characterised. The complexes were evaluated for antibacterial activity towards several problematic Gram-positive (Staphylococcus aureus, methicillin-resistant Staphylococcus aureus (MRSA), and vancomycin-resistant Enterococcus (VRE)) and Gram-negative (Escherichia coli, Pseudomonas aeruginosa) bacteria. The cell viability of COS-7 (monkey kidney) cells treated with the bismuth flavonolates was also studied to determine the effect of the complexes on mammalian cells. The heteroleptic complexes [BiPh(L)2] (in which L=flavonolate) showed good antibacterial activity towards all of the bacteria but reduced COS-7 cell viability in a concentration-dependent manner. The homoleptic complexes [Bi(L)3] exhibited activity towards the Gram-positive bacteria and showed low toxicity towards the mammalian cell line. Bismuth uptake studies in VRE and COS-7 cells treated with the bismuth flavonolate complexes indicated that Bi accumulation is influenced by both the substitution of the flavonolate ligands and the degree of substitution at the bismuth centre.
- Burke, Kirralee J.,Stephens, Liam J.,Werrett, Melissa V.,Andrews, Philip C.
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supporting information
p. 7657 - 7671
(2020/06/02)
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- A Selective, Dual Emission β-Alanine Aminopeptidase Activated Fluorescent Probe for the Detection of Pseudomonas aeruginosa, Burkholderia cepacia, and Serratia marcescens
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Selective detection of β-alanyl aminopeptidase (BAP)-producing Pseudomonas aeruginosa, Serratia marcescens, and Burkholderia cepacia was achieved by employing the blue-to-yellow fluorescent transition of a BAP-specific enzyme substrate, 3-hydroxy-2-(p-dim
- Váradi, Linda,Najib, Elias Y.,Hibbs, David E.,Perry, John D.,Groundwater, Paul W.
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- Synthesis, characterization and antimicrobial evaluation of cobalt(III) complexes of 4-(2-substituted phenylimino)-2-(4-substituted phenyl)-4H-chromen-3-ol
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A series of eight Co(III) complexes [CoL1-8(H2O)2Cl] (I-1 to I-8) incorporating 4-(2-substituted phenylimino)-2-(4-substituted phenyl)-4H-chromen-3-ol, as a tridentate imino flavone ligands (L1 to L8, 2-sub. = NH2, SH, 4-sub. = OMe, OH, Cl, NMe2) have been synthesized, characterized and the geometry of the complexes were optimized by DFT. The chemical structure of synthesized imino flavone ligands and their complexes were characterized by elemental analysis, 1H NMR, 13C NMR, UV-visible, IR, ESI-mass spectral data, conductometric and magnetic measurements. The synthesized compounds have been screened for their in vitro antibacterial activities against bacteria Vibrio cholerae, Salmonella typhi, Staphylococcus aureus, Escherichia coli and antifungal activities against fungi Candida albicans and Aspergillus flavus by paper disc diffusion method. The complexes I-3, I-4, I-7 and I-8 showed good antimicrobial activities against pathogens.
- Singh, Ashok K.,Patel, Suresh K.,Jafri, Asif
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p. 2015 - 2021
(2019/08/08)
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- Synthesis of 3-HCF2S-Chromones through Tandem Oxa-Michael Addition and Oxidative Difluoromethylthiolation
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A simple protocol for the synthesis of difluoromethylthiolated chromen-4-ones using elemental sulfur and ClCF2CO2Na as the difluoromethylthiolating agent is described. Three-component reactions of 2′-hydroxychalcones, ClCF2CO2Na, and sulfur under basic conditions using TEMPO as the oxidant afforded HCF2S-containing 4H-chromen-4-one and 9H-thieno[3,2-b]chromen-9-one derivatives in good yield. The protocol is practical and efficient, and the starting materials are cheap and readily available.
- Zhang, Pingshun,Chen, Wanzhi,Liu, Miaochang,Wu, Huayue
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supporting information
p. 9326 - 9329
(2019/12/24)
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- Design, synthesis and biological evaluation of novel dihydropyrimidine-2-thione derivatives as potent antimicrobial agents: Experimental and molecular docking approach
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Introduction: Dihydropyrimidine scaffold represent an important class of pharmacologically active nitrogen containing heterocyclic compounds. A wide range of molecules with dihydropyrimidine moieties have important role in medicinal chemistry on account of their potential biological activities. Methodology: A series of 3,4-dihydropyrimidine-2(1H)-thione derivatives have been designed and synthesized in a concise way through condensation of variously substituted chalcones with thiourea in alkaline alcoholic solutions. In order to investigate their biological significance, these compounds were tested for their in vitro antimicrobial potential against various bacterial and fungal strains. Moreover, the experimental results were supported by molecular docking studies. Results and Discussion: The newly synthesized compounds were characterized by the usual spectroscopic techniques In case of antibacterial activity, the compounds 5 (40.3±0.44 mm), 12 and 13 (almost 35 mm) exhibited highest zone of inhibitions against Methicillin-resistant Staphylococcus auerus (MRSA) bacterial strain as compared to the standard drug Cefixime. These compounds displayed moderate to good activities against all attempted fungal strains. In docking analysis, it has been observed that compounds 8 (-6.4017 Kcal/mol) and 10 (-6.1319 Kcal/mol) revealed significant binding affinity against penicillin binding protein (PDB ID: 1VQQ), while compounds 1 (-143.23 Kcal/mol) and 2 (-146.99 Kcal/mol) showed best activity for shikimate dehydrogenase (PDB ID: 3DON). Conclusion: In conclusion, we have designed, synthesized and characterized an interesting series of biologically active dihydropyrimidine derivatives. Remarkably, most of the synthesized compounds were found more active against all tested bacterial strains in comparison to the standard drug Cefixime as manifested by experimental as well as theoretical results.
- Mughal, Ehsan Ullah,Sadiq, Amina,Hamayun, Muhammad,Zafar, Muhammad Naveed,Fatima, Nighat,Yameen, Muhammad Arfat,Muhammad, Syed Aun,Mumtaz, Amara,Ahmed, Ishtiaq,Fatima, Tehseen
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p. 1189 - 1201
(2018/11/01)
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- In vitro and in vivo anticancer studies of 2′-hydroxy chalcone derivatives exhibit apoptosis in colon cancer cells by hdac inhibition and cell cycle arrest
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Considering the therapeutic values of bioflavonoids in colon cancer treatment, six 2′-hydroxy chalcones (C1-C6) were synthesized, characterized and screened for in vitro cytotoxicity on human colon carcinoma (HCT116) and African green monkey kidney epithe
- Pande, Aditya Narayan,Biswas, Subhankar,Reddy, Neetinkumar D.,Jayashree,Kumar, Nitesh,Rao, C. Mallikarjuna
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p. 448 - 463
(2017/05/29)
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- Synthesis, characterization and biological evaluation of ruthenium flavanol complexes against breast cancer
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Four Ru(II) DMSO complexes (M1R-M4R) having substituted flavones viz. 3-Hydroxy-2-(4-methoxyphenyl)-4H-chromen-4-one (HL1), 3-Hydroxy-2-(4-nitrophenyl)-4H-chromen-4-one (HL2), 3-Hydroxy-2-(4-dimethylaminophenyl)-4H–chromen-4-one (HL3) and 3-Hydroxy-2-(4-chlorophenyl)-4H-chromen-4-one (HL4) were synthesized and characterized by elemental analysis, IR, UV–Vis, 1H NMR spectroscopies and ESI-MS. The molecular structures of the complexes were investigated by integrated spectroscopic and computational techniques (DFT). Both ligands as well as their complexes were screened for anticancer activities against breast cancer cell lines MCF-7. Cytotoxicity was assayed by MTT [3-(4, 5-dimethyl thiazol-2-yl)-2, 5-diphenyl tetrazolium bromide] assay. All ligands and their complexes exhibited significant cytotoxic potential of 5–40?μM concentration at incubation period of 24?h. The cell cytotoxicity increased significantly in a concentration-dependent manner. In this series of compounds, HL2 (IC50 17.2?μM) and its complex M2R (IC50 16?μM) induced the highest cytotoxicity.
- Singh, Ashok Kumar,Saxena, Gunjan,Sahabjada,Arshad
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- Characterization of the Fluorescence Properties of 4-Dialkylaminochalcones and Investigation of the Cytotoxic Mechanism of Chalcones
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Understanding the mechanisms responsible for the various biological activities of chalcones, particularly the direct cellular targets, presents an unmet challenge. Here, we prepared a series of fluorescent chalcone derivatives as chemical probes for their
- Zhou, Bo,Jiang, Peixin,Lu, Junxuan,Xing, Chengguo
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p. 539 - 552
(2016/08/26)
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- Synthesis, biological evaluation and molecular modelling of 2′-hydroxychalcones as acetylcholinesterase inhibitors
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A series of 2′-hydroxy- and 2′-hydroxy-4′,6′-dimethoxychalcones was synthesised and evaluated as inhibitors of human acetylcholinesterase (AChE). The majority of the compounds were found to show some activity, with the most active compounds having IC
- Sukumaran, Sri Devi,Chee, Chin Fei,Viswanathan, Geetha,Buckle, Michael J. C.,Othman, Rozana,Rahman, Noorsaadah Abd.,Chung, Lip Yong
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- In vitro enzyme inhibition potentials and antioxidant activity of synthetic flavone derivatives
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Free radicals are produced by an important chemical process known as oxidation that in turn initiates chain reactions to damage the cells and originate oxidative stress. Flavones have got special position in research field of natural and synthetic organic chemistry due to their biological capabilities as antioxidant. The antioxidants are known to possess extensive biological effects that include antiviral, antibacterial, anti-inflammatory, antithrombotic, and vasodilatory activities. The simple flavone (F1) and substituted flavone derivatives (F2-F5) have been synthesized from o-hydroxyacetophenone and benzaldehyde derivatives in good yield. The structures have been established by different spectroscopic techniques like 1H NMR, 13C NMR, IR, and elemental analysis. Antioxidant profile of these compounds was established using DPPH and H2O2 free radical scavenging assay. The findings showed that halogenated flavones showed more enzyme inhibitions and antioxidant activities than simple flavones and are potential candidates for the treatment of wide range of diseases.
- Shoaib, Mohammad,Shah, Syed Wadood Ali,Ali, Niaz,Shah, Ismail,Naveed Umar, Muhammad,Shafiullah,Ayaz, Muhammad,Tahir, Muhammad Nawaz,Akhtar, Sohail
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- Organic Crystals with Near-Infrared Amplified Spontaneous Emissions Based on 2′-Hydroxychalcone Derivatives: Subtle Structure Modification but Great Property Change
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A series of highly efficient deep red to near-infrared (NIR) emissive organic crystals 1-3 based on the structurally simple 2′-hydroxychalcone derivatives were synthesized through a simple one-step condensation reaction. Crystal 1 displays the highest qua
- Zhang, Hongyu,Cheng, Xiao,Wang, Kai,Huang, Shuo,Zhang, Houyu,Wang, Yue
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p. 8369 - 8373
(2015/11/27)
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- Quantum-chemical analysis of the Algar-Flynn-Oyamada reaction mechanism
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This work is devoted to improving the understanding of Algar-Flynn-Oyamada reaction mechanism and the analysis of factors that affect the formation of flavonols. The calculation of thermodynamic parameters for the key reaction steps pointed to a mechanism involving chalcone epoxides as intermediates. A correlation was identified between the nucleophilicity of oxygen atom at position 2' of epoxide anions and the yields of flavonols. An increased charge at the nucleophilic center was shown to reduce the effectiveness of β-cyclization of epoxide anions.
- Serdiuk,Roshal,B?a?ejowski
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p. 396 - 403
(2014/08/05)
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- Cyclization of 2'-hydroxychalcones to flavones using ammonium iodide as an iodine source - An eco-friendly approach
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Ammonium iodide on exposure to air decomposes to ammonia and iodine. The in situ generated iodine was used for the cyclization of 2'-hydroxychalcones to the corresponding flavones under solvent-free conditions in good to excellent yields. This method could serve as an attractive alternative to the existing methods for synthesis of flavones and the use of toxic molecular iodine is avoided. Copyright
- Kulkarni, Pramod S.,Kondhare, Dasharath D.,Varala, Ravi,Zubaidha, Pudukulathan K.
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p. 909 - 916
(2013/08/23)
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- Microwave assisted synthesis of some substituted 1,3-diaryl propenones and 3,5-diaryl-6-carbethoxy cyclohexenones and their antibacterial activity
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Microwave induced solvent free solid phase syntheses of substituted 1,3-diaryl propenones 1a-f using basic alumina and their subsequent rapid transformation to 3,5-diaryl-6-Carbethoxy cyclohexenones 2a-i with ethyl acetoacetate in the presence of basic al
- Baboo, Harish,Sahdev
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p. 501 - 505
(2013/11/06)
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- Synthesis of flavanones by use of anhydrous potassium carbonate as an inexpensive, safe, and efficient basic catalyst
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Anhydrous potassium carbonate has been utilized as an inexpensive, safe, and efficient basic catalyst for the synthesis of flavanones starting either from 2′-hydroxychalcones or from 2′-hydroxyacetophenones. In both the cases the favored reaction condition was either refluxing in a solvent with added catalyst or microwave irradiation on the catalyst.
- Mondal, Rina,Gupta, Arpita Das,Mallik, Asok K.
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experimental part
p. 5020 - 5024
(2011/10/19)
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- Synthesis and pharmacological screening of some novel chalconyl derivatives of substituted phenyl semicarbazide
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In the present study, we have synthesized chalcone and semicarbazide-linked chalonyl derivatives and the titled compounds confirmed by MS, IR, and 1H NMR techniques. The anticonvulsant activity was determined by maximal electroshock (MES) induced seizure method. A majority of the compounds exhibited significant anticonvulsant activity after intraperitoneal administration. The results show the importance of hydrogen bonding for activity. In the present study 5e, 5h, 5i, 6e, 6h, and 6i emerged as the most active molecules, showed significant anticonvulsant of activity. Springer Science+Business Media, LLC 2010.
- Singh, Hemendra Pratap,Pandeya,Chauhan,Sharma, Chandra Shekhar
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experimental part
p. 74 - 80
(2012/02/04)
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- Polymorphism of 4′-dimethylamino-3-hydroxyflavone
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Structures of two polymorphic crystals 1a and 1b of 4′ -dimethylamino-3-hydroxyflavone (1) have been determined. Each crystal has intermolecular hydrogen-bonded dimers with the adjacent molecule. The dimeric structure in crystal 1a is nearly planar, where
- Hino, Kazuyuki,Nakajima, Kiyohiko,Kawahara, Miyoko,Kiyota, Issui,Sekiya, Hiroshi
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body text
p. 1234 - 1236
(2012/01/31)
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- Chalconsemicarbazone: A new scaffold for antiepileptic drug discovery
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During our investigation in the area of epileptic drug discovery, we have identified that the available conventional antiepileptic drugs are effective in 60-80% patients and in specific type of seizures and having various undesirable side effects. But in present time a new class aryl semicarbazone is emerged as new pharmacophore in epileptic drug discovery having broad spectrum activity. On the bases of work done in this area we have applied hybridization of pharmacophore strategy of drug design and developed a new pharmacophore. We have also designed a scheme for synthesizing such pharmacophore and performed their pharmacological screening for the protection of seizures, behavioral study and CNS activity. The compound 1-[1-(2,4-dihydroxyphenyl)-3-(2-hydroxyphenyl) allylidene]-4-(2-fluorophenyl) semicarbazide (8) emerged as the most active prototype molecule in all the models.
- Singh, Hemendra Pratap,Chauhan,Pandeya,Sharma, Chandra Shekhar
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experimental part
p. 103 - 106
(2010/08/06)
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- Highly activated Michael acceptor by an intramolecular hydrogen bond as a fluorescence turn-on probe for cyanide
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An activated Michael acceptor type of probe by an intramolecular hydrogen bond has shown a selective fluorescence turn-on response to cyanide through a conjugated addition of the nucleophilic anion to the enone probe with a 1300-fold increase in its fluor
- Park, Seokan,Kim, Hae-Jo
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supporting information; experimental part
p. 9197 - 9199
(2011/02/22)
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- Synthesis and biological activity of some novel pyrazolines
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Chalcones were prepared from substituted acetophenones and substituted benzaldehydes and condensed with hydrazine hydrate in ethanol to get the corresponding pyrazolines (Pdc1 to Pdc 14). The compounds were synthesized and characterizes by TLC, melting po
- Venkataraman, Setaraman,Jain, Saras,Shah, Kamal,Upmanyu, Neeraj
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experimental part
p. 361 - 366
(2011/09/13)
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- Solvent-free improved syntheses of some substituted 1,3-diaryl-propenones and 3,5-diaryl-6-carbethoxycyclohexenones under microwave irradiation and their antibacterial activity
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Microwave induced solvent-free solid phase syntheses of substituted 1,3-diarylpropenones (chalcones) 3a-f using basic alumina and their subsequent rapid transformation to 3,5-diaryl-6-carbethoxycyclohexenones 4a-f with ethyl acetoacetate in the presence o
- Jhala, Yajuvendra S.,Dulawat, Shiv S.,Verma
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p. 466 - 469
(2007/10/03)
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- Synthesis and antidepressant activity of some 1,3,5-triphenyl-2-pyrazolines and 3-(2″-hydroxy naphthalen-1″-yl)-1,5-diphenyl-2-pyrazolines
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Five new 1,3,5-triphenyl-2-pyrazolines were synthesised by reacting 1,3-diphenyl-2-propene-1-one with phenyl hydrazine hydrochloride and another five new 3-(2″-hydroxy naphthalen-1″-yl)-1,5-diphenyl-2-pyrazolines were synthesised by reacting 1-(2′-hydroxy
- Rajendra Prasad,Lakshmana Rao,Prasoona,Murali,Ravi Kumar
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p. 5030 - 5034
(2007/10/03)
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