Author/Authors :
H.P. Wang، نويسنده , , T.L. Hwang، نويسنده , , On Lee، نويسنده , , Y.J. Tseng، نويسنده , , C.Y. Shu، نويسنده , , S.J. Lee، نويسنده ,
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 μM which is 458-fold more potent than that of azatyrosine. The selective toxicity, defined as IC50 wild-type/IC50 ras-transformed for this compound was 138.5.
