Design and Synthesis of 1??(6??(2??(2??Arylethynyl) Phenyl) Hexyn??5??yl) Piperidin??2??Ones as Antitumor Agents that Induce Apoptotic Progress

I Lin, I Chen, CF Lin, YH Lo, SH Yang…

Index: Lin, I.-Ling; Chen, I.-Hsiang; Lin, Chi-Fong; Lo, Yu-Hsiang; Yang, Sheng-Huei; Lin, Shinne-Ren; Wu, Ming-Jung Journal of the Chinese Chemical Society, 2008 , vol. 55, # 3 p. 668 - 674

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Citation Number: 2

Abstract

Abstract A series of 1-(6-(2-(2-arylethynyl) phenyl) hexyn-5-yl) piperidin-2-ones 2a-j were synthesized and their antitumor activities were evaluated. Of these compounds, 1-(6-(2-(2-(4- nitrophenyl) ethynyl) phenyl) hexyn-5-yl) piperidin-2-one (2j) showed the highest potency of growth inhibition activity, especially against the RPMI-8226 (0.4 μM) and SR (0.02 μM) cell lines of human leukemia. Compound 2j also induced significant apoptotic progress in the ...