676629-67-7Relevant academic research and scientific papers
Compounds for treating tumors
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Page 39, (2008/06/13)
The invention provides compounds of formula (I): wherein E, A, B′, R6, R7, R8, and R9 are defined in the specification which compounds exhibit anticancer activity and are useful for treating cancer.
D-piece modifications of the hemiasterlin analog HTI-286 produce potent tubulin inhibitors
Zask, Arie,Birnberg, Gary,Cheung, Katherine,Kaplan, Joshua,Niu, Chuan,Norton, Emily,Yamashita, Ayako,Beyer, Carl,Krishnamurthy, Girija,Greenberger, Lee M.,Loganzo, Frank,Ayral-Kaloustian, Semiramis
, p. 4353 - 4358 (2007/10/03)
Modifications of the D-piece carboxylic acid group of the hemiasterlin analog HTI-286 gave tubulin inhibitors which were potent cytotoxic agents in taxol resistant cell lines expressing P-glycoprotein. Amides derived from proline had potency comparable to HTI-286. Reduction of the carboxylic acid to ketones and alcohols or its conversion to acidic heterocycles also gave potent analogs. Synthetic modifications of the carboxylic acid could be carried out selectively using a wide range of synthetic reagents. Proline analog 3 was found to be effective in a human xenograft model in athymic mice.
