78860-77-2Relevant academic research and scientific papers
Pyridazinone substituted benzenesulfonamides as potent carbonic anhydrase inhibitors
Yaseen, Raed,Ekinci, Deniz,Senturk, Murat,Hameed, Alhamzah Dh.,Ovais, Syed,Rathore, Pooja,Samim, Mohammed,Javed, Kalim,Supuran, Claudiu T.
, p. 1337 - 1341 (2016)
A series of sulfonamide derivatives (2a-l) incorporating substituted pyridazinone moieties were investigated for the inhibition of two human cytosolic carbonic anhydrase isoforms, hCA I and hCA II. All these compounds, together with the clinically used su
Synthesis and biological evaluations of 1,2-diaryl pyrroles as analogues of combretastatin A-4
Sun, Jun,Chen, Lei,Liu, Chunjiang,Wang, Zhan,Zuo, Daiying,Pan, Jiatong,Qi, Huan,Bao, Kai,Wu, Yingliang,Zhang, Weige
, p. 1541 - 1547 (2016/02/05)
A series of novel 1,2-diaryl pyrroles as analogues of combretastatin A-4 (CA-4, 1a) were synthesized and evaluated for their antitumour potential against three cancer cell lines. Most compounds exhibited growth inhibition against all of the cancer cell lines. Compound 7q not only exhibited prominent antitumour efficacy with IC50 values of 0.390 μm in SGC-7901, 0.070 μm in HT-1080 and 0.045 μm in KB cell lines but also showed low activity with IC50 values of 30.08 μm in normal L929 cell line. Moreover, compound 7q inhibited tubulin polymerization into microtubules and caused microtubule destabilization. A molecular docking study of 7q was performed to determine its binding mode at the colchicine site in the tubulin dimer. 1,2-Diaryl pyrroles as combretastatin A-4 analogues were synthesized and evaluated for anti-proliferative activities. Compound 7q exhibited antitubulin activity.
