4′-Alkoxyl substitution enhancing the anti-mitotic effect of 5-(3′,4′,5′-substituted)anilino-4-hydroxy-8-nitroquinazolines as a novel class of anti-microtubule agents

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• 作者：Yi Jin ; Zu-Yu Zhou ; Wei Tian ; Qiang Yu and Ya-Qiu Long
• 关键词：Quinazoline ; Mitosis inhibitor ; Tubulin polymerization ; Anti-microtubule agent ; Alkoxyl substitution ; Aniline ; Antiproliferative effect ; Cell cycle ; Tumor cells
• 刊名：Bioorganic and Medicinal Chemistry Letters
• 出版年：2006
• 出版时间：15 November 2006
• 年：2006
• 卷：16
• 期：22
• 页码：5864-5869
• 全文大小：456 K

文摘

Mitosis inhibitors are powerful anticancer drugs. Based on a novel anti-microtubule agent of 5-(4′-methoxy)anilino-4-hydroxy-8-nitroquinazoline, a series of 5-(3′,4′,5′-substituted)anilino-4-hydroxy-8- nitroquinazolines were designed and synthesized to investigate the effect of the substitution on the inhibitory activity against mitotic progression of tumor cells. The large alkoxyl substitution on the 4′-position of 5-anilino ring is beneficial for the potency. The 5-(3′,4′,5′-trimethoxy)anilino-8-nitroquinazoline (rong>1hrong>) displays an overwhelming activity in arresting the cells at the G2/M phase, providing a promising new template for further development of potent microtubule-targeted anti-mitotic drugs.