Design,Synthesis and Antitumor Activity of a Novel Series of PAC-1 Analogues |
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Authors: | LUO Hao-ming YANG Chun-ling ZHANG Xiao-ying ZHAO Ming-ming JIANG Dan XIAO Jun-hai YANG Xiao-hong LI Song |
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Institution: | 1. School of Pharmaceutical Sciences, Jilin University, Changchun 130021, P. R. China;
2. National Engineering Research Center for the Strategic Drugs, Beijing Institute of Pharmacology and Toxicology, Beijing 100850, P. R. China;
3. The First Hospital of Jilin University, Changchun 130021, P. R. China;
4. School of Pharmaceutical Engineering, Shenyang Pharmaceutical University, Shenyang 110016, P. R. China |
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Abstract: | A novel series of first procaspase activating compound(PAC-1) analogues was designed, synthesized and evaluated for antitumor activity towards two cell lineshuman promyelocytic leukemia cell line(HL60) and human embryonic lung fibroblast cell line(HLF)] by the MTT3-(4,5)-dimethylthiahiazo(-z-y1)-3,5-di-phenytetrazo-liumromide] method in vitro. The structures of all the compounds were confirmed by 1H NMR, MS and elemental analysis. Among the compounds synthesized,(E)-2-(3-{4-(tert-butyl)benzyl](methyl)amino}propyl)(methyl)amino]-N'-4-(diethylamino)-2-hydroxybenzylidene]acetohydrazide(compound 6n) exhibits a good anti-proliferative activity to the majority of tumor cells tested, and selectively cleaves cancer cells. Thus, compound 6n was identified as promising lead compound for further structural modification. |
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Keywords: | PAC-1 analogue Anticancer activity MTT assay HL60 |
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