Synthesis and Biological Evaluation of Furanoallocolchicinoids; Journal of Medicinal Chemistry; Vol. 58, iss. 2

Synthesis and Biological Evaluation of Furanoallocolchicinoids; Journal of Medicinal Chemistry; Vol. 58, iss. 2

Bibliographic Details
Parent link:Journal of Medicinal Chemistry: Scientific Journal
Vol. 58, iss. 2.— 2015.— [P. 692–704]
Corporate Author: Национальный исследовательский Томский политехнический университет Управление проректора по научной работе и инновациям Центр RASA в Томске Лаборатория изучения механизмов сигнальной трансдукции
Other Authors: Voitovich Y. V. Yuliya, Shegravina E. S. Ekaterina, Sitnikov N. S. Nikolay, Faerman V. I. Vladimir, Fokin V. V. Valery Valerjevich, Schmalz H.-G. Hans-Gunther, Combes S. Sebastien, Allegro D. Diane, Barbier P. Pascal, Beletskaya I. P. Irina, Svirshchevskaya E. V. Elena, Fedorov A. Yu. Alexey
Summary:Title screen
A series of conformationally flexible furan-derived allocolchicinoids was prepared from commercially available colchicine in good to excellent yields using a three-step reaction sequence. Cytotoxicity studies indicated the potent activity of two compounds against human epithelial and lymphoid cell lines (AsPC-1, HEK293, and Jurkat) as well as against Wnt-1 related murine epithelial cell line W1308. The results of in vitro experiments demonstrated that the major effect of these compounds was the induction of cell cycle arrest in the G2/M phase as a direct consequence of effective tubulin binding. In vivo testing of the most potent furanoallocolchicinoid 10c using C57BL/6 mice inoculated with Wnt-1 tumor cells indicated significant inhibition of the tumor growth.
Режим доступа: по договору с организацией-держателем ресурса
Language:English
Published: 2015
Subjects:
электронный ресурс
труды учёных ТПУ
Online Access:http://dx.doi.org/10.1021/jm501678w
Format: Electronic Book Chapter
KOHA link:https://koha.lib.tpu.ru/cgi-bin/koha/opac-detail.pl?biblionumber=650316

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