Synthesis and Antitumor Activities of Novel 4-Morpholinothieno[3,2-d]pyrimidine Derivatives

doi:10.1007/s40242-013-3281-6

Chemical Research in Chinese Universities ›› 2014, Vol. 30 ›› Issue (1): 75-81.doi: 10.1007/s40242-013-3281-6

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Synthesis and Antitumor Activities of Novel 4-Morpholinothieno[3,2-d]pyrimidine Derivatives

SONG Kaizhen, MA Junjie, WANG Xiao, GONG Ping, ZHAO Yanfang

Key Laboratory of Structure-based Drug Design and Discovery, Ministry of Education, Shenyang Pharmaceutical University, Shenyang 110016, P. R. China

Received:2013-07-08 Revised:2013-10-09 Online:2014-02-01 Published:2013-10-23
Contact: ZHAO Yanfang,E-mail:yanfangzhao@126.com E-mail:yanfangzhao@126.com
Supported by:
Supported by the 2010 Program for Innovative Research Team of the Ministry of Education of China and the Program for Liaoning Innovative Research Team in University, China(No.IRT10732010)

Abstract

Abstract:

A series of novel 2-hydrazinyl-4-morpholinothieno[3,2-d]pyrimidine derivatives was designed and synthesized. All of them were screened for their cytotoxic activities against large cell lung cancer(H460), colon cancer (HT-29) and adenocarcinomic lung cancer(A549) cell lines in vitro. The pharmacological results indicate that most of the target compounds show moderate to significant activities. Especially compound 17 exhibits the most potent antitumor activities against H460, HT-29 and A549 cell lines with IC₅₀ values of 0.57, 0.45 and 1.45 μmol/L, respectively.

Key words: 2-Hydrazinyl-4-morpholinothieno[3,2-d]pyrimidine, Antitumor activity, Cytotoxic activity

SONG Kaizhen, MA Junjie, WANG Xiao, GONG Ping, ZHAO Yanfang. Synthesis and Antitumor Activities of Novel 4-Morpholinothieno[3,2-d]pyrimidine Derivatives[J]. Chemical Research in Chinese Universities, 2014, 30(1): 75-81.

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Synthesis and Antitumor Activities of Novel 4-Morpholinothieno[3,2-d]pyrimidine Derivatives

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