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2-取代喹唑啉-4(3H)-酮的哌嗪-1-碳二硫代酸酯衍生物的合成及细胞毒性筛选

Synthesis and cytotoxicity screening of piperazine-1-carbodithioate derivatives of 2-substituted quinazolin-4(3H)-ones.

作者信息

Cao Sheng-Li, Guo Yan-Wen, Wang Xian-Bo, Zhang Mei, Feng Yu-Ping, Jiang Yu-Yang, Wang Yue, Gao Qian, Ren Jian

机构信息

Department of Chemistry, Capital Normal University, Beijing, China.

出版信息

Arch Pharm (Weinheim). 2009 Mar;342(3):182-9. doi: 10.1002/ardp.200800148.

DOI:10.1002/ardp.200800148
PMID:19212984
Abstract

A new series of piperazine-1-carbodithioate derivatives of 2-substituted quinazolin-4(3H)-ones were synthesized via a five-steps procedure starting from 2-amino-5-methylbenzoic acid. The cytotoxicity of the resulting compounds against A-549 (human lung cancer), HCT-8 (human colon cancer), HepG2 (human liver cancer), and K562 (human myelogenous leukaemia) cell lines was determined by the MTT assay. Preliminary screening results of these compounds are reported.

摘要

以2-氨基-5-甲基苯甲酸为起始原料，通过五步反应合成了一系列新的2-取代喹唑啉-4(3H)-酮的哌嗪-1-碳二硫代酸酯衍生物。采用MTT法测定了所得化合物对A-549（人肺癌）、HCT-8（人结肠癌）、HepG2（人肝癌）和K562（人髓性白血病）细胞系的细胞毒性。报道了这些化合物的初步筛选结果。

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