13129-68-5Relevant articles and documents
Synthesis, neuro-protection and anti-cancer activities of simple isatin mannich and schiff bases
Chen, Gang,Ning, Yang,Zhao, Wei,Zhang, Yanqiu,Zhang, Yu,Hao, Xiaojiang,Wang, Ye,Mu, Shuzhen
, p. 395 - 400 (2016/05/24)
The study of isatin, as well as its kind of derivatives, has become a hot topic for a long time. To explore the new compounds and bioactivities, in this work, a series of simple isatin Mannich and Schiff bases was synthesized through the condensation reac
Hybrid pharmacophore design and synthesis of isatin-benzothiazole analogs for their anti-breast cancer activity
Solomon, V. Raja,Hu, Changkun,Lee, Hoyun
experimental part, p. 7585 - 7592 (2011/02/23)
A hybrid pharmacophore approach was used to design and synthesize isatin-benzothiazole analogs to examine their anti-breast cancer activity. The cytotoxicity of these compounds were determined using three different human breast tumor cell lines, MDA-MB231, MDA-MB468, MCF7, and two non-cancer breast epithelial cell lines, 184B5 and MCF10A. Although all compounds examined were quite effective on all the cancer cell lines examined, the compounds 4-bromo-1-diethylaminomethyl-1H-indole-2,3-dione (21) and 4-chloro-1- dimethylaminomethyl-3-(6-methyl-benzothiazol-2-ylimino)-1,3-dihydroindol-2-one (5e) emerged as the most active compounds of this series. Importantly, the cytotoxic effect of 21 was 10-15-fold higher on cancer than non-cancer cells, suggesting that this compound can be very effective for the control of breast cancer with low side effects. Since 21 showed effective cytotoxicity on MCF7 cells and arrested the cells at G2/M at a similar concentration, these two phenomena may be closely correlated. We conclude that the isatin-linked benzothiazole analog can serve as a prototype molecule for further development of a new class of anti-breast cancer agents.
