Synthesis and in vitro Antitumor Activity of 6-Chloro-4-piperazinquinazolinethiosemicarbazone Derivatives

doi:10.3724/SP.J.1095.2012.00481

Chinese Journal of Applied Chemistry

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Synthesis and in vitro Antitumor Activity of 6-Chloro-4-piperazinquinazolinethiosemicarbazone Derivatives

LIU Haibin^*, LV Ping, PAN Ningning, WANG Wenzhong, WANG Qiang

(School of Biomedicine & Chemical Engineering,Liaoning Institute of Science and Technology,Benxi 117004,China)

Received:2011-11-01 Revised:2012-03-09 Published:2012-09-10 Online:2012-09-10

Abstract

Abstract: Three new quinazoline derivatives 5a~5c bearing piperazine have been designed and synthesized by four-step reactions of cyclization, chlorination, substitution and condensation using 2-amino-5-chlorobenzoic acid and formamide as starting materials. Their structures were confirmed by 1H NMR, 13C NMR, ESI-MS and IR. The in vitro cytotoxicities against SGC-7901(human gastric cancer), KB(human oral epidermoid cancer) and HT-1080(human fibrosarcoma) cell lines of compounds 5a~5c were tested with colorimetric MTT assay. The results indicated that compounds 5a~5c had poor anticancer activities against SGC-7901 and HT-1080 cell lines, while had no notable inhibitory activity against KB cell lines.

Key words: chloropiperazinquinazoline N-thiosemicarbazone substituted derivatives, antitumor activity, MTT assay,synthesis

CLC Number:

O621.3

LIU Haibin*, LV Ping, PAN Ningning, WANG Wenzhong, WANG Qiang. Synthesis and in vitro Antitumor Activity of 6-Chloro-4-piperazinquinazolinethiosemicarbazone Derivatives[J]. Chinese Journal of Applied Chemistry, DOI: 10.3724/SP.J.1095.2012.00481.

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Synthesis and in vitro Antitumor Activity of 6-Chloro-4-piperazinquinazolinethiosemicarbazone Derivatives

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