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Synthesis and biological evaluation of novel AM80 derivatives as antileukemic agents

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Abstract

A series of novel AM80 derivatives as antileukemic agents were synthesized and their structures were confirmed by IR, 1H-NMR, and HR-MS spectra. All the target compounds were evaluated for in vitro antiproliferative activities against human leukemic HL-60, NB4, and K562 cell lines. Among these derivatives, compound 4g showed much stronger antiproliferative activities against all the three human leukemic cell lines than the positive control AM80, and compound 4b exhibited more active antiproliferative effects against HL-60 and K562 cells than AM80. Furthermore, the preliminary SAR analysis suggested that AM80 conjugating with HDAC inhibitors with small steric hindrance could give more effective antileukemic agents. These results would be helpful to design more potent antileukemic drugs for the treatment of human leukemia.

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Acknowledgments

The authors are grateful to the National Nature Science Foundation of China (Grant No.90713041) and National Science and Technology Major Project of the Ministry of Science and Technology of China (Grant No.2009ZX09103-118) for financial support for this research.

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  1. Institute of Medicinal Chemistry, School of Pharmaceutical Sciences, Shandong University, Jinan, Shandong, 250012, China

    Haiyong Bian, Jinhong Feng & Wenfang Xu

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  1. Haiyong Bian
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  2. Jinhong Feng
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  3. Wenfang Xu
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Correspondence to Wenfang Xu.

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Bian, H., Feng, J. & Xu, W. Synthesis and biological evaluation of novel AM80 derivatives as antileukemic agents. Med Chem Res 22, 175–185 (2013). https://doi.org/10.1007/s00044-012-0019-9

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  • DOI: https://doi.org/10.1007/s00044-012-0019-9

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