Syntheses and antitumor activity of cis-restricted combretastatins: 5-Membered heterocyclic analogues

A series of cis-restricted combretastatin analogues with 5-membered heterocycles were synthesized and their inhibitory activity against microtubule assembly and cytotoxic activity against the colon 26 adenocarcinoma cancer cell line were evaluated. Some of the heterocyclic analogues showed potent an...

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Veröffentlicht in:	Bioorganic & medicinal chemistry letters 1998-11, Vol.8 (22), p.3153-3158
Hauptverfasser:	Ohsumi, Koji, Hatanaka, Toshihiro, Fujita, Koichi, Nakagawa, Ryusuke, Fukuda, Yumiko, Nihei, Yukio, Suga, Yasuyo, Morinaga, Yoshihiro, Akiyama, Yukio, Tsuji, Takashi
Format:	Artikel
Sprache:	eng
Schlagworte:	Animals Antineoplastic agents Antineoplastic Agents, Phytogenic - chemical synthesis Biological and medical sciences Cattle General aspects Humans Medical sciences Pharmacology. Drug treatments Stilbenes - chemical synthesis Stilbenes - pharmacology Structure-Activity Relationship
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Zusammenfassung:	A series of cis-restricted combretastatin analogues with 5-membered heterocycles were synthesized and their inhibitory activity against microtubule assembly and cytotoxic activity against the colon 26 adenocarcinoma cancer cell line were evaluated. Some of the heterocyclic analogues showed potent antitubulin activity and cytotoxicity. Compounds 16 and 35 showed marked tumor growth suppression in the colon 26 murine tumor model. The syntheses and antitumor activity of cis-restricted AC-7739 analogues are discussed.
ISSN:	0960-894X 1464-3405
DOI:	10.1016/S0960-894X(98)00579-4