MedChemComm p. 1257 - 1266 (2013)
Update date:2022-08-05
Topics:
Singh, Satyajit
Baviskar, Ashish Triambak
Jain, Vaibhav
Mishra, Nidhi
Chand Banerjee, Uttam
Bharatam, Prasad V.
Tikoo, Kulbhushan
Singh Ishar, Mohan Paul
Substituted 3-formylchromones were synthesized and evaluated as inhibitors of the human DNA topoisomerase IIα (hTopo-IIα) enzyme. The results of the decatenation, relaxation and DNA intercalation assays revealed that the compounds (11b, 12a, 12b, 12d, 12e, 13a and 13b) exhibited potent inhibitory activity against the hTopo-IIα enzyme, and are nonintercalating agents. These compounds also possess significant in vitro cytotoxicity (LC50 ranges from 0.5-8.6 μM) against prostate (PC-3) cancerous cell line as seen in comparison to the standard drug etoposide. To further probe the plausible mode of action of 3-formylchromone derivatives, molecular docking studies have also been carried out, which showed that the compounds under investigation fitted well in the ATP binding pocket of hTopo-IIα enzyme with good docking scores and form nonbonding interactions with the crucial residues of the catalytic site. The Royal Society of Chemistry.
View MoreKAIYUAN CHEMICAL COMPANY LIMITED.
website:http://www.kaiyuanchem.com
Contact:+86-22-59891255/66/77
Address:B-2205, Kuangshi International Building, Yingbin Road, XiangLuo Bay Business District, Binhai New area, Tianjin, China.
Reliable Pharma Technology (Shanghai) Co., Ltd.
Contact:0086-21-67676847-8008
Address:Lane 1500, No.68, Xinfei Road, Songjiang District, Shanghai, 201611, P.R.China.
Nantong Auxin Electronic Technology Co., LTD
Contact:86-513-88760026
Address:NO.5-1, Aoxin Road, Haian Hi-tech Development Zone, Jiangsu Province, China
Beijing Zhongshuo Pharmaceutical T & D Co.,Ltd
Contact:0086-10-64430626
Address:ea No 16, HEPINGLI,DONGCHENG DISTRICT,BEIJING,P.R.CHINA.
Shanghai Hohance Chemical Co., ltd
Contact:13914753421
Address:Fl.5;Bld. 70, Lane 1500; Xinfei Road
Doi:10.1021/ja903175g
(2009)Doi:10.1021/jo00259a014
(1988)Doi:10.1016/j.tetlet.2009.01.016
(2009)Doi:10.1021/ja01545a050
(1958)Doi:10.1021/om801199q
(2009)Doi:10.1007/s10600-006-0210-7
(2006)