6552-64-3Relevant academic research and scientific papers
Synthesis of new schiff base of 1,3-oxazine and 1,3-thiazine derivatives derived from 4-phenyl substituted chalcones and evaluation of their antibacterial activity
Sharma, Anupama,Khaturia, Sarita,Singh, Har Lal
, p. 531 - 536 (2021/02/27)
Oxazine and thiazine heterocycles have distinctive interests due to their important class of natural and non-natural products and exhibit high biological activities in the pharmaceutical and biological fields. This work was planned to synthesize Schiff ba
Synthesis and biological evaluation of 3,5-substituted pyrazoles as possible antibacterial agents
Asmara, Anjar P.,Bottomley, Amy L.,Harry, Elizabeth J.,Och, Anthony,Payne, Matthew,Ung, Alison T.
, (2021/09/24)
The emergence of multi-drug resistant bacteria has increased the need for novel antibiotics to help overcome what may be considered the greatest threat to modern medicine. Here we report the synthesis of fifteen novel 3,5-diaryl-1H- pyrazoles obtained via
Synthesis and characterization of 2-phenylpyrazoline derivatives and evaluation of their activities against antimicrobial and breast cancer cell line in vitro and in silico studies
Chinnamanayakar, Raja,Ezhilarasi
, p. 1311 - 1320 (2019/06/10)
The new series of 2-phenylpyrazoline derivatives (2a-j) were synthesized and evaluated for their antimicrobial, in silico and in vitro anticancer activity was performed by MTT assay using MDA-MB-231 (human breast adenocarcinoma) cell line. The 2-phenylpyr
Design, synthesis, and biological evaluation of polyphenols with 4,6-diphenylpyrimidin-2-amine derivatives for inhibition of Aurora kinase A
Lee, Young Han,Park, Jihyun,Ahn, Seunghyun,Lee, Youngshim,Lee, Junho,Shin, Soon Young,Koh, Dongsoo,Lim, Yoongho
, p. 265 - 281 (2019/07/03)
Background: Several 4,6-diarylpyrimidin-2-amine derivatives show anticancer properties. However, their mode of action is not fully characterized. To develop potent anticancer chemotherapeutic agents, we designed and synthesized 25 4,6-diphenylpyrimidin-2-amine derivatives containing a guanidine moiety. Methods: Clonogenic long-term survival assays were performed to screen anticancer compounds. To derive the structural conditions showing good cytotoxicities against cancer cells, quantitative structure-activity relationships (QSAR) were calculated. Biological activities were determined by flow cytometry for cell cycle analysis and by immunoblot analysis for the detection of Aurora kinase A (AURKA) activity. Because 2-(2-Amino-6-(2,4-dimethoxyphenyl)pyrimidin-4-yl) phenol (derivative 12) selectively inhibited AURKA activity from the kinome assay, in silico docking experiments were performed to elucidate the molecular binding mode between derivative 12 and AURKA. Results: The pharmacophores were derived based on the QSAR calculations. Derivative 12 inhibited AURKA activity and reduced phosphorylation of AURKA at Thr283 in HCT116 human colon cancer cells. Derivative 12 caused the accumulation of the G2/M phase of the cell cycle and triggered the cleavages of caspase-3, caspase ?7, and poly(ADP-ribose) polymerase. The binding energies of 30 apo-AURKA – derivative 12 complexes obtained from in silico docking ranged from ?16.72 to ?11.63 kcal/mol. Conclusions: Derivative 12 is an AURKA inhibitor, which reduces clonogenicity, arrests the cell cycle at the G2/M phase, and induces caspase-mediated apoptotic cell death in HCT116 human colon cancer cells. In silico docking demonstrated that derivative 12 binds to AURKA well. The structure-activity relationship calculations showed hydrophobic substituents and 1-naphthalenyl group at the R2 position increased the activity. The existence of an H-bond acceptor at C-2 of the R1 position increased the activity, too.
Synthesis and characterization of 2-pyrazoline derivatives and their in silico and in vitro studies on antimicrobial and anticancer activities
Rathinamanivannan,Megha,Chinnamanayakar, Raja,Kumar, Ashok,Ezhilarasi
, p. 2191 - 2196 (2019/09/03)
The new series of 1-(4,5-dihydro-5-phenyl-3-diphenylpyrazol-1-yl)butan-1-one derivatives were synthesized by cyclization method using biphenyl chalcone with n-butyric acid and hydrazine hydrate. The synthesized 1-(4,5-dihydro-5-phenyl-3-diphenylpyrazol-1-
An efficient synthesis and in vitro antimicrobial screening of 2-cyanoimino-4-aryl-6-(1,1′-biphenyl-4-yl)-3, 4-dihydro-1H-pyrimidines
Swaminathan, Sivagami,Ingarsal, Namasivayam
, p. 777 - 782 (2018/05/28)
An efficient synthesis of 2-Cyanoimino-4-aryl-6-(1,1′-biphenyl-4-yl)-3,4-dihydro-1H-pyrimidines from stryl-4-biphenylketones and cyanoguanidine in presence of sodium hydroxide has been described. Cyanoguanidine serves as N-C=N source for the construction of desired cyanoiminopyrimidines. The structural assignments of the titled products were done accordingly to their spectra like Mass, FT-IR, Proton and Carbon-13NMR spectroscopy. The more stable tautomeric form was ascertained using computational frequency analysis. The tested microorganism profile of compounds exhibits significant antimicrobial activity.
Synthesis and cytotoxicity evaluation of new 3-substituted 4-(4-methyloxy phenyl)-1H-pyrrole derivatives
Zhan, Xiaoping,Lan, Lan,Zhang, Yuankui,Chen, Jian,Zhao, Kai,Wang, Shuai,Xin, Yuxuan,Mao, Zhenmin
, p. 200 - 206 (2016/02/26)
A new series of 3-substituted 4-(4-methyloxy phenyl)-1H-pyrrole derivatives were synthesized and biologically evaluated for potential anticancer activity. Fifteen targeted compounds showed high selectivity toward normal cells and cancer cells: that is, al
Synthesis and antifungal activity of chalcone derivatives
Zheng, Yuanyuan,Wang, Xuesong,Gao, Sumei,Ma, Min,Ren, Guiming,Liu, Huabing,Chen, Xiaohong
, p. 1804 - 1810 (2015/03/04)
In the present study, using chalcone as a lead compound, a series of its derivatives (compounds 1-30) were designed and synthesised. Their activity of anti-pathogenic fungi of plants has been evaluated. It is found that these compounds have good antifunga
SAR studies of differently functionalized 4′-phenylchalcone based compounds as inhibitors of cathepsins B, H and L
Ravish, Indu,Raghav, Neera
, p. 50440 - 50453 (2015/06/25)
Conditions related to the elevated levels of cathepsin B [3.4.22.1], cathepsin H [3.4.22.16] and cathepsin L [3.4.22.15] in various cancerous, rheumatoid arthritis and tissue degenerative disorders motivate the design, synthesis and evaluation of compound
Solvent free synthesis of different substituted pyrazoles under microwave irradiation via one pot synthesis and their biological evaluation
Shorey, Shweta,Choudhary, Prakash,Intodia, Kumud
, p. 5930 - 5932,3 (2020/09/15)
Pyrazoles and their derivative are widely used as pharmaceutical and agrochemical agents and consequently a large number of synthetic routes to pyrazole have been reported. Due to the property of reducing blood sugar by pyrazole, it has resulted in the sy
