Design, Synthesis and In Vitro Biological Activity of Novel C-7 Methylene Congeners of Furanoallocolchicinoids

Autor:	Iuliia A. Gracheva, Elena V. Svirshchevskaya, Ekaterina S. Shchegravina, Yulia B. Malysheva, Alsu R. Sitdikova, Alexey Yu. Fedorov
Jazyk:	angličtina
Rok vydání:	2023
Předmět:	colchicine antiproliferative activity tubulin activated C=C bond Pharmacy and materia medica RS1-441
Zdroj:	Pharmaceutics, Vol 15, Iss 4, p 1034 (2023)
Druh dokumentu:	article
ISSN:	15041034 1999-4923
DOI:	10.3390/pharmaceutics15041034
Popis:	A series of novel heterocyclic colchicine derivatives bearing a C-7 methylene fragment were synthesized via Wittig, Horner–Wadsworth–Emmons and Nenajdenko–Shastin olefination approaches. The in vitro biological activities of the most promising compounds were investigated using MTT assays and cell cycle analyses. Compounds with an electron withdrawing group on the methylene fragment exhibited substantial antiproliferative activity towards COLO-357, BxPC-3, HaCaT, PANC-1 and A549 cell lines. The spatial orientation of the substituent at the double bond significantly influenced its biological activity.
Databáze:	Directory of Open Access Journals
Externí odkaz:	https://doaj.org/article/b4340d9791064e65afca17c8a9af43a3 Zobrazit plný text záznamu View record in DOAJ Plný text ve formátu PDF Plný text ve formátu HTML
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