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Synthesis and antitumor activities of novel 4-morpholinothieno[3,2-d]pyrimidine derivatives

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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.

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Authors and Affiliations

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

    Kaizhen Song, Junjie Ma, Xiao Wang, Ping Gong & Yanfang Zhao

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  1. Kaizhen Song
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  2. Junjie Ma
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  3. Xiao Wang
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  4. Ping Gong
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  5. Yanfang Zhao
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Correspondence to Yanfang Zhao.

Additional information

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)

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Song, K., Ma, J., Wang, X. et al. Synthesis and antitumor activities of novel 4-morpholinothieno[3,2-d]pyrimidine derivatives. Chem. Res. Chin. Univ. 30, 75–81 (2014). https://doi.org/10.1007/s40242-013-3281-6

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  • DOI: https://doi.org/10.1007/s40242-013-3281-6

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