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新型2-(3-取代-6-氯-1,1-二氧代-1,4,2-苯并二硫嗪-7-基)-3-苯基-4(3H)-喹唑啉酮的合成及细胞毒性测试

Synthesis and cytotoxicity testing of novel 2-(3-substituted-6-chloro-1,1-dioxo-1,4,2-benzodithiazin-7-yl)-3-phenyl-4(3H)-quinazolinones.

作者信息

Pomarnacka Elzbieta, Maruszak Magdalena, Langowska Karolina, Reszka Przemyslaw, Bednarski Patrick J

机构信息

Department of Chemical Technology of Drugs, Medical University of Gdansk, Al. Gen. J. Hallera 107, Gdansk, Poland.

出版信息

Arch Pharm (Weinheim). 2008 Aug;341(8):485-90. doi: 10.1002/ardp.200700258.

DOI:10.1002/ardp.200700258
PMID:18618486
Abstract

A new series of thirteen 2-[3-(substituted amino)-6-chloro-1,1-dioxo-1,4,2-benzodithiazin-7-yl]-3-phenyl-4(3H)-quinazolinones 4-16 were prepared in order to evaluate their cytotoxic activity against 12 human cancer cell lines. The bioassay indicated that the quinazolinone derivatives 5, 8-12, 15, and 16 possess cancer-cell growth-inhibitory properties. Compounds 5 and 12 showed a high level of selectivity for certain cell lines. The most active compounds 9, 10, 15, and 16 showed moderate antiproliferative activity and were approximately 4-fold less potent than cisplatin.

摘要

为了评估一系列13种新型的2-[3-(取代氨基)-6-氯-1,1-二氧代-1,4,2-苯并二硫氮杂卓-7-基]-3-苯基-4(3H)-喹唑啉酮（4-16）对12种人类癌细胞系的细胞毒性活性。生物测定表明喹唑啉酮衍生物5、8-12、15和16具有癌细胞生长抑制特性。化合物5和12对某些细胞系表现出高度选择性。活性最高的化合物9、10、15和16表现出中等的抗增殖活性，其效力比顺铂低约4倍。

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引用本文的文献

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