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Design, synthesis and biological evaluation of new rhodacyanine analogues as potential antitumor agents
Alternative TitleDesign, 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
2012
Source PublicationCHINESE CHEMICAL LETTERS
ISSN1001-8417
Volume23Issue:4Pages:415-418
AbstractIn 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 IC50 values ranging from 0.006 to 9.2 mu mol/L as compared to the lead compound MKT-077. Among them, the most promising compound 7d (IC50 = 0.006 p.,mol/L) was 216.7 times more active than MKT-077 (IC50 = 1.3 mu mol/L). The preliminary structure activity relationship of the target compounds was discussed. (C) 2012 Ping Gong. Published by Elsevier B.V. on behalf of Chinese Chemical Society. All rights reserved.
Other AbstractIn 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.
KeywordTOXICITY MKT-077 Rhodacyanine analogues Antitumor Synthesis
Indexed ByCSCD
Language英语
CSCD IDCSCD:4513738
Citation statistics
Document Type期刊论文
Identifierhttp://ir.imr.ac.cn/handle/321006/147585
Collection中国科学院金属研究所
Affiliation中国科学院金属研究所
Recommended Citation
GB/T 7714
Li Yang Xiong,Zhai Xin,Liao Wei Ke,et al. Design, synthesis and biological evaluation of new rhodacyanine analogues as potential antitumor agents[J]. CHINESE CHEMICAL LETTERS,2012,23(4):415-418.
APA Li Yang Xiong,Zhai Xin,Liao Wei Ke,Zhu Wu Fu,He Ying,&Gong Ping.(2012).Design, synthesis and biological evaluation of new rhodacyanine analogues as potential antitumor agents.CHINESE CHEMICAL LETTERS,23(4),415-418.
MLA Li Yang Xiong,et al."Design, synthesis and biological evaluation of new rhodacyanine analogues as potential antitumor agents".CHINESE CHEMICAL LETTERS 23.4(2012):415-418.
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