Design,synthesis and biological evaluation of new rhodacyanine analogues as potential antitumor agents |
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Authors: | Yang Xiong Li Xin Zhai Wei Ke Liao Wu Fu Zhu Ying He Ping Gong |
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Affiliation: | Key Laboratory of Structure-based Drug Design and Discovery of Ministry of Education, School of Pharmaceutical Engineering, Shenyang Pharmaceutical University, Shenyang 110016, China |
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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 u,mol/L as compared to the lead compound MKT-077.Among them,the most promising compound 7d(IC50 = 0.006μmol/L) was 216.7 times more active than MKT-077(IC50 = 1.3μmol/L).The preliminary structure-activity relationship of the target compounds was discussed. |
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Keywords: | Rhodacyanine analogues Antitumor Synthesis |
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