| Design, synthesis and biological evaluation of new rhodacyanine analogues as potential antitumor agents | |
| Alternative Title | 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 | |
| 2012 | |
| Source Publication | CHINESE CHEMICAL LETTERS
 |
| ISSN | 1001-8417 |
| Volume | 23Issue:4Pages:415-418 |
| Abstract | 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 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 Abstract | 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. |
| Keyword | TOXICITY MKT-077 Rhodacyanine analogues Antitumor Synthesis |
| Indexed By | CSCD |
| Language | 英语 |
| CSCD ID | CSCD:4513738 |
| Citation statistics | |
| Document Type | 期刊论文 |
| Identifier | http://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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