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( Hue Thi My Van ),( Hyun Jung Woo ),( Hyung Min Jeong ),( Daulat Bikram Khadka ),( Su Hui Yang ),( Caho Zhao ),( Yi Feng Jin ),( Eung Seok Lee ),( Kwang Youl Lee ),( Young Joo Kwon ),( Won Jea Cho ) 전남대학교 약품개발연구소 2014 약품개발연구지 Vol.23 No.-
A series of 3-heteroarylisoquinolinamines were designed. synthesized and evaluated for cytotoxicity, topoisomerases (topos) inhibitory activities and cell cycle inhibition, Several of the 3heteroarylisoquinolines exhibited selective cytotoxicity against human ductal breast epithelial tumor (T47D) cells over non-cancerous human breast epithelial (MCF-10A) and human prostate cancer (DU14S) cells. Most of the derivatives showed greater cytotoxicity in human colorectal adenocarcinoma (HCT-1S) cells than camptothecin (CPT), etoposide and doxorubicin (DOX). Generally, 3-heteroarylisoquinolinamines displayed greater affinity for topo I than topo n. 3-Heteroarylisoquinolinamines with greater topo 1 inhibitory effect exhibited potent cytotoxicity. Piperazine-substituted derivative. Sb, with potent topo 1 and moderate topo n activities intercalated between DNA bases and interacted with topos through H-bonds at the DNA cleavage site of a docking model. Moreover. flowcytometry indicated that cytotoxic 3heteroarylisoquinolinamines led to accumulation of human cervical (HeLa) cancer cells in the different phases of the cell cycle before apoptosis. Taken together. 3-heteroarylisoquinolinamines possessed potent cytotoxicity with topos and cell cycle inhibitory activities. ⓒ 2014 Elsevier Masson SAS. All rights reserved.