Design,synthesis and biological evaluation of new rhodacyanine analogues as potential antitumor agents

Li Yang Xiong Zhai Xin Liao Wei Ke Zhu Wu Fu He Ying Gong Ping ^*

文摘	In an attempt to develop potent antitumor agents,new rhodacyanine analogues containing the pyridinium ring（5a-5h）,the isoquinolinium ring（6a-6c） and the quinolinium ring（7a-7e） linked to the rhodanine ring via N-N covalent bond were designed, synthesized and evaluated for antitumor activity against human lung cancer cell line（H460） by MTT assay in vitro.Most of the tested compounds showed enhanced antitumor activity with IC_(50) values ranging from 0.006 to 9.2 u,mol/L as compared to the lead compound MKT-077.Among them,the most promising compound 7d(IC_(50) = 0.006μmol/L) was 216.7 times more active than MKT-077(IC_(50) = 1.3μmol/L).The preliminary structure-activity relationship of the target compounds was discussed.
来源	Chinese Chemical Letters ,2012,23(4):415-418 【核心库】
DOI	10.1016/j.cclet.2012.01.015
关键词	Rhodacyanine analogues ; Antitumor ; Synthesis
地址	School of Pharmaceutical Engineering, Shenyang Pharmaceutical University, Key Laboratory of Structure-based Drug Design and Discovery of Ministry of Education, Shenyang, 110016
语种	英文
文献类型	研究性论文
ISSN	1001-8417
学科	化学工业
文献收藏号	CSCD:4513738