Design, Synthesis and Antitumor Activity of a Novel Series of PAC-1 Analogues  

作　　者：LUO Hao-ming YANG Chun-ling ZHANG Xiao-ying ZHAO Ming-ming JIANG Dan XIAO Jun-hai YANG Xiao-hong LI Song 

机构地区：[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, Beo'ing 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

出　　处：《Chemical Research in Chinese Universities》2013年第5期906-910,共5页高等学校化学研究（英文版）

基　　金：Supported by the National Natural Science Foundation of China（Nos.20771030, 20671025）.

摘　　要：A novel series of first procaspase activating compound（PAC-1） analogues was designed, synthesized and evaluated for antitumor activity towards two cell lines[human promyelocytic leukemia cell line（HL60） and human embryonic lung fibroblast cell line（HLF）] by the MTT[3-（4,5）-dimethylthiahiazo（-z-yl）-3,5-di-phenytetrazo- liumromide] method in vitro. The structures of all the compounds were confirmed by IH NMR, MS and elemental analysis. Among the compounds synthesized^（E）-2-[（3-{[4-（tert-buty~）benzy~]（methy~）amin~}pr^py~）（methy~）amin~]- 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.A novel series of first procaspase activating compound（PAC-1） analogues was designed, synthesized and evaluated for antitumor activity towards two cell lines[human promyelocytic leukemia cell line（HL60） and human embryonic lung fibroblast cell line（HLF）] by the MTT[3-（4,5）-dimethylthiahiazo（-z-yl）-3,5-di-phenytetrazo- liumromide] method in vitro. The structures of all the compounds were confirmed by IH NMR, MS and elemental analysis. Among the compounds synthesized^（E）-2-[（3-{[4-（tert-buty~）benzy~]（methy~）amin~}pr^py~）（methy~）amin~]- 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.

关 键 词：PAC-1 analogue Anticancer activity MTT assay HL60 

分 类 号：TQ463.5[化学工程—制药化工] TQ457.29