Synthesis and Biological Evaluation of Furanoallocolchicinoids; Journal of Medicinal Chemistry; Vol. 58, iss. 2
| Parent link: | Journal of Medicinal Chemistry: Scientific Journal Vol. 58, iss. 2.— 2015.— [P. 692–704] |
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| Autor Corporativo: | |
| Outros autores: | , , , , , , , , , , , |
| 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 |
| Idioma: | inglés |
| Publicado: |
2015
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| Subjects: | |
| Acceso en liña: | http://dx.doi.org/10.1021/jm501678w |
| Formato: | Electrónico Capítulo de libro |
| KOHA link: | https://koha.lib.tpu.ru/cgi-bin/koha/opac-detail.pl?biblionumber=650316 |
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| 200 | 1 | |a Synthesis and Biological Evaluation of Furanoallocolchicinoids |f Y. V. Voitovich [et al.] | |
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| 300 | |a Title screen | ||
| 320 | |a [References: p. 702-704 (47 tit.)] | ||
| 330 | |a 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. | ||
| 333 | |a Режим доступа: по договору с организацией-держателем ресурса | ||
| 461 | |t Journal of Medicinal Chemistry |o Scientific Journal | ||
| 463 | |t Vol. 58, iss. 2 |v [P. 692–704] |d 2015 | ||
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