2,4-Diamino-9H-pyrimido[4,5-b]indol-5-ols: Synthesis, in vitro cytotoxic activity, and QSAR investigations

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• 作者：Bernd Dotzauer ; Renate Grü ; nert ; Patrick J. Bednarski ; Harald Lanig ; Jens Landwehr and Reinhard Troschü ; tz
• 关键词：Ellipticine analogues ; Nenitzescu reaction ; Cytotoxicity ; QSAR
• 刊名：Bioorganic and Medicinal Chemistry
• 出版年：2006
• 出版时间：1 November 2006
• 年：2006
• 卷：14
• 期：21
• 页码：7282-7292
• 全文大小：224 K

文摘

A series of novel 2,4-diaminopyrimido[4,5-b]indol-6-ols has been synthesized and the in vitro cytotoxic activities were evaluated against four human cancer cell lines originating from solid tumors. An increase in activity was observed when a heteroaromatic ring was annulated on side g of the pyrimido[4,5-b]indole system to give compounds with activities comparable to ellipticine and cisplatin. To understand the experimental cytotoxic activities, QSAR investigations were performed, which showed a very good linearity between the experimental and predicted IC₅₀.