Selective cytotoxicity of azatyrosinamides against ras-transformed NIH 3T3 cells |
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| Authors: | Wang H P Hwang T L Lee On Tseng Y J Shu C Y Lee S J |
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| Affiliation: | Graduate Institute of Natural Products, Chang Gung University College of Medicine, 259 Wen-Hwa 1st Road, Kwei-Shan, Tao-Yuan 333, Taiwan. hpw@mail.cgu.edu.tw |
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| Abstract: | This study aims to develop novel azatyrosinamide compounds structurally modified from ras-specific antioncogenic azatyrosine. Analogues 4-15 were prepared and their inhibition on the growth of wild-type and ras-transformed NIH 3T3 cell lines was compared. Compound 12 was found to be the most active with IC50 16.5+/-2.2 microM which is 458-fold more potent than that of azatyrosine. The selective toxicity, defined as IC(50 wild-type)/IC(50 ras-transformed) for this compound was 138.5. |
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