57077-27-7Relevant academic research and scientific papers
Synthesis and biological evaluation of pyrimidine bridged combretastatin derivatives as potential anticancer agents and mechanistic studies
Kumar, Bhupinder,Sharma, Praveen,Gupta, Vivek Prakash,Khullar, Madhu,Singh, Sandeep,Dogra, Nilambra,Kumar, Vinod
, p. 130 - 140 (2018/03/23)
A number of pyrimidine bridged combretastatin derivatives were designed, synthesized and evaluated for anticancer activities against breast cancer (MCF-7) and lung cancer (A549) cell lines using MTT assays. Most of the synthesized compounds displayed good
Synthesis and Anticancer Activity of 3-(Substituted Aroyl)-4-(3,4,5-trimethoxyphenyl)-1H-pyrrole Derivatives
Zhan, Xiao-Ping,Lan, Lan,Wang, Shuai,Zhao, Kai,Xin, Yu-Xuan,Qi, Qi,Wang, Yao-Lin,Mao, Zhen-Min
, (2017/02/23)
A series of 3-(substituted aroyl)-4-(3,4,5-trimethoxyphenyl)-1H-pyrrole derivatives were synthesized and determined for their anticancer activity against eleven cancer cell lines and two normal tissue cell lines using MTT assay. Among the synthesized comp
Novel polyfunctional pyridines as anticancer and antioxidant agents. Synthesis, biological evaluation and in silico ADME-T Study
Badr, Mona Hany,Rostom, Sherif Ahmed Fawzi,Radwan, Mohammed Fouad
, p. 442 - 454 (2017/05/17)
Two series of novel alkoxylated 2-oxo(imino)-3-pyridinecarbonitriles (structurally-relevant to some reported anticancer pyridines with phosphodiesterase 3A (PDE3A) inhibitory activity) were synthesized and evaluated for their in vitro differential tumor c
A new series of cytotoxic pyrazoline derivatives as potential anticancer agents that induce cell cycle arrest and apoptosis
Wang, Hong,Zheng, Jinhong,Xu, Weijie,Chen, Cheng,Wei, Duncan,Ni, Wenxiu,Pan, Ying
, (2017/10/13)
A new series of pyrazoline derivatives 1b–12b was designed, synthesized and evaluated for antiproliferative activity against three cancer cell lines (HepG-2, Hela and A549). Additionally, NIH/3T3 cell cytotoxicity were tested and the structure activity re
Synthesis and cytotoxic activities of some pyrazoline derivatives bearing phenyl pyridazine core as new apoptosis inducers
George, Riham F.,Fouad, Marwa A.,Gomaa, Iman E.O.
, p. 48 - 59 (2016/08/08)
The cyclization of chalcones 3a-3u with 3-hydrazinyl-6-phenylpyridazine 7 under basic condition led to the formation of new pyrazoline derivatives 8a-8u. All final compounds were characterized by spectral and elemental analyses. They were screened for their antiproliferative activities against A549 (lung), HepG-2 (liver), CaCo-2 (intestinal) and MCF-7 (breast) cancer cell lines. Some of the synthesized compounds exhibited promising antiproliferative activities especially compound 8k with IC50values of 8.33, 1.67 and 10?μM against HepG-2, MCF-7 and CaCo-2 cancer cell lines, respectively. Moreover, their antiproliferative activity was due to apoptosis rather than necrosis induction except compound 8h which exhibited equal apoptotic and necrotic properties. Compound 8k showed 5 fold increase in caspase-3 activity indicating that the apoptosis proceeds via caspase-3 activation.
Synthesis and biological evaluation of substituted 4,6-diarylpyrimidines and 3,5-diphenyl-4,5-dihydro-1H-pyrazoles as anti-tubercular agents
Pathak, Vinay,Maurya, Hardesh K.,Sharma, Sandeep,Srivastava, Kishore K.,Gupta, Atul
supporting information, p. 2892 - 2896 (2014/06/10)
Various substituted 4,6-diarylpyrimidin-2-amine (4), 4,6-diaryl-2- (heteroaryl)pyrimidine (6) and 1-(3,5-diaryl-4,5-dihydro-1H-pyrazol-1-yl) ethanone (7) derivatives were synthesized in good yields using simple methodology. The synthesized compounds (4-7)
Design, synthesis and molecular docking study of some substituted 4,5-dihydro-2H-indazole derivatives as potential anti-inflammatory agents
Badr, Mona H.,Elbayaa, Rasha Y.,El-Ashmawy, Ibrahim M.
, p. 718 - 730 (2013/09/23)
A new series of 4,5-dihydro-2H-indazoles was synthesized and evaluated for anti-inflammatory activity using formalin-induced paw edema and turpentine oil-induced granuloma pouch bioassays. In addition, the inhibitory activity of cyclooxygenase, ulcerogenic effect, and acute toxicity (ALD50) values were also determined. Compounds 10, 13, 15, 16, 18 and 22 were proved to display distinctive anti-inflammatory profiles with a fast onset of action. They revealed super GI safety profile and are well tolerated by the experimental animals with high safety margin (ALD50 > 300 mg/Kg). The same active compounds exhibited moderate to powerful selectivity profile towards the inhibition of COX-2 enzyme. Docking poses for the most active compounds separately in the active site of human COX-2 enzyme were also obtained.
Synthesis and biological evaluation of simple methoxylated chalcones as anticancer, anti-inflammatory and antioxidant agents
Bandgar, Babasaheb P.,Gawande, Shrikant S.,Bodade, Ragini G.,Totre, Jalinder V.,Khobragade, Chandrahas N.
experimental part, p. 1364 - 1370 (2010/04/26)
Chalcones have been identified as interesting compounds with cytotoxicity, anti-inflammatory and antioxidant properties. In the present study, simple methoxychalcones were synthesized by Claisen-Schmidt condensation reaction and evaluated for above biological activities. The structures of the compounds were established by IR, 1H NMR and mass spectral analysis. The data revealed that compound 3s (99-100% at 10 μM concentration) completely inhibit the selected five human cancer cell lines as compared to standard flavopiridol and gemcitabine (70-90% at 700 nM and 500 nM concentrations, respectively), followed by 3a, 3n, 3o, 3p, 3q, 3r. Among the tested compounds 3l, 3m, 3r, and 3s exhibited promising anti-inflammatory activity against TNF-α and IL-6 with 90-100% inhibition at 10 μM concentration. DPPH free radical scavenging activity was given by the compounds 3o, 3n, 3l, 3r, 3m, 3a, 3p, 3c and 3s at 1 mM concentration. Overall, 3s was obtained as lead compound with promising anticancer, anti-inflammatory and antioxidant activities. Bioavailability of compounds were checked by in vitro cytotoxicity study and confirmed to be nontoxic. The structure activity relationship (SAR) and in silico drug relevant properties (HBDs, HBAs, PSA, c Log P, ionization potential, molecular weight, EHOMO and ELUMO) further confirmed that the compounds were potential candidates for future drug discovery study.
Reinvestigation of structure-activity relationship of methoxylated chalcones as antimalarials: Synthesis and evaluation of 2,4,5-trimethoxy substituted patterns as lead candidates derived from abundantly available natural β-asarone
Kumar, Rakesh,Mohanakrishnan, Dinesh,Sharma, Abhishek,Kaushik, Naveen Kumar,Kalia, Kalpana,Sinha, Arun Kumar,Sahal, Dinkar
experimental part, p. 5292 - 5301 (2011/02/23)
We have examined the antimalarial structure-activity relationship of a series of methoxylated chalcones (A-CHCH-CO-B) against Plasmodium falciparum (3D7 strain) using fluorescence-based SYBR Green assay. Our study has revealed that electron releasing methoxy groups on ring A and electron withdrawing groups on ring B increases antimalarial potency while the positional interchange of these groups causes a decrease. In particular, 2,4,5-trimethoxy substitution pattern at ring A provided potent analogues which were easily derived from abundantly available natural β-asarone rich Acorus calamus oil. Cytotoxic evaluation indicated that the most active compounds 27 (IC50: 1.8 μM) and 26 (IC50: 2 μM) were also relatively non-toxic. Furthermore, compound 12 showed excellent resistance index of 1.1 against chloroquine resistant Dd2 strain of P. falciparum.
Studies on Cycloimmonium Ylids: Synthesis of Some New 2,4,6-Triarylsubstituted Pyridines via Pyridinium Ylids
Singhal, R. K.,Mishra, Naresh K.
, p. 1079 - 1080 (2007/10/02)
2,4,6-Triarylsubstituted pyridines (4a-r) have been synthesised by the reaction of pyridinium ylids (1a-c) with α,β-unsaturated ketones (2a-f) in the presence of ammonium acetate and acetic acid.These compounds (4a-r) have been characterised on the basis
