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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.
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 NN covalent bond were designed , synthesized and evaluated for antitumor activity against human lung cancer cell line (H460) by MTT assay in vitro. Host 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 = 0.006 μmol / L) was 216.7 times more active than MKT-077 (IC 50 = 1.3 μmol / L) -activity relationship of the target compounds was discussed.