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抗肿瘤剂。第204部分：取代的2-芳基喹唑啉酮的合成与生物学评价。

Antitumor agents. Part 204: synthesis and biological evaluation of substituted 2-aryl quinazolinones.

作者信息

Xia Y, Yang Z Y, Hour M J, Kuo S C, Xia P, Bastow K F, Nakanishi Y, Namrpoothiri P, Hackl T, Hamel E, Lee H K

机构信息

Natural Products Laboratory, School of Pharmacy, University of North Carolina, Chapel Hill 27599, USA.

出版信息

Bioorg Med Chem Lett. 2001 May 7;11(9):1193-6. doi: 10.1016/s0960-894x(01)00190-1.

DOI:10.1016/s0960-894x(01)00190-1
PMID:11354375
Abstract

A series of 2',3',4',6,7-substituted 2-aryl quinazolinones were synthesized and evaluated for biological activity. Among them, 17 displayed significant growth inhibitory action against a panel of tumor cell lines. Compound 17 was also a potent inhibitor of tubulin polymerization. Compounds 8-10 displayed selective activity against P-gp-expressing epidermoid carcinoma of the asopharynx.

摘要

合成了一系列2'，3'，4'，6，7-取代的2-芳基喹唑啉酮并对其生物活性进行了评估。其中，17种对一组肿瘤细胞系表现出显著的生长抑制作用。化合物17也是微管蛋白聚合的有效抑制剂。化合物8-10对表达P-糖蛋白的鼻咽表皮样癌表现出选择性活性。

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