作者
Andre Stander, Fourie Joubert, Annie Joubert
发表日期
2011/3
期刊
Chemical biology & drug design
卷号
77
期号
3
页码范围
173-181
出版商
Blackwell Publishing Ltd
简介
In the present study, Autodock 4.0 was employed to discover potential carbonic anhydrase IX inhibitors that are able to interfere with microtubule dynamics by binding to the Colchicine binding site of tubulin. Modifications at position 2′ of estrone were made to include moieties that are known to improve the antimitotic activity of estradiol analogs. 2‐ethyl‐3‐O‐sulphamoyl‐estra‐1,3,5(10),15‐tetraen‐3‐ol‐17‐one estronem (C9) and 2‐ethyl‐3‐O‐sulphamoyl‐estra‐1,3,5(10)16‐tetraene (C12) were synthesized and tested in vitro. Growth studies were conducted utilizing spectrophotometrical analysis with crystal violet as DNA stain. Compounds C9 and C12 were cytotoxic in MCF‐7 and MDA‐MB‐231 tumorigenic and metastatic breast cancer cells, SNO non‐keratinizing squamous epithelium cancer cells and HeLa cells after 48 h exposure. Compounds C9 inhibited cell proliferation to 50% of the vehicle‐treated …
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