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 ...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.展开更多
基金Supported by the National Natural Science Foundation of China（Nos.20771030, 20671025）.
文摘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.
