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Design, synthesis and anticancer activity of novel 6-(aminophenyl)-2,4-bismorpholino-1,3,5-triazine derivatives bearing arylmethylene hydrazine moiety

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Chemical Research in Chinese Universities Aims and scope

Abstract

In an attempt to develop potent and selective anticancer agents, we designed and synthesized a series of novel bis(morpholino-1,3,5-triazine) derivatives bearing aylmethylene hydrazine moiety and evaluated their cytotoxicity, in vitro, against H460(non-small-cell lung cancer), HT-29(human colorectal cancer) and MDA-MB-231(human breast cancer) cell lines. The pharmacological results indicate that all the compounds exhibit enhanced cytotoxicity than BMCL-200908069-1, and six target compounds(7e, 7h, 7j, 9a, 9b, 9c) were superior to PAC-1 against all the tested cancer cell lines. The most active compound 7j, with IC50^(inhibitory concentration 50%) values of 0.75, 0.34 and 0.60 μmol/L against HT-29, H460 and MDA-MB-231 cancer cell lines, was 39-, 28-, and 60-fold more potent than BMCL-200908069-1(29.24, 9.52 and 36.21 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

    Qiang Huang, Qiangqiang Fu, Yajing Liu, Jinying Bai, Qianying Wang, Huimin Liao & Ping Gong

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  1. Qiang Huang
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  2. Qiangqiang Fu
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  3. Yajing Liu
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  4. Jinying Bai
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  5. Qianying Wang
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  6. Huimin Liao
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  7. Ping Gong
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Corresponding author

Correspondence to Ping Gong.

Additional information

Supported by the Program for Innovative Research Team of the Ministry of Education and Program for Liaoning Innovative Research Team in University, China(No.IRT1073).

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Huang, Q., Fu, Q., Liu, Y. et al. Design, synthesis and anticancer activity of novel 6-(aminophenyl)-2,4-bismorpholino-1,3,5-triazine derivatives bearing arylmethylene hydrazine moiety. Chem. Res. Chin. Univ. 30, 257–265 (2014). https://doi.org/10.1007/s40242-014-3253-5

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  • DOI: https://doi.org/10.1007/s40242-014-3253-5

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