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
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container_end_page 3158
container_issue 22
container_start_page 3153
container_title Bioorganic & medicinal chemistry letters
container_volume 8
creator Ohsumi, Koji
Hatanaka, Toshihiro
Fujita, Koichi
Nakagawa, Ryusuke
Fukuda, Yumiko
Nihei, Yukio
Suga, Yasuyo
Morinaga, Yoshihiro
Akiyama, Yukio
Tsuji, Takashi
description 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.
doi_str_mv 10.1016/S0960-894X(98)00579-4
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source MEDLINE; Access via ScienceDirect (Elsevier)
subjects 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
title Syntheses and antitumor activity of cis-restricted combretastatins: 5-Membered heterocyclic analogues
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