SYNTHESIS AND BIOLOGICAL-ACTIVITY OF 5-[(2,5-DIHYDROXYBENZYL)AMINO]SALICYLIC ACID ANALOGS AS INHIBITORS OF EGF RECEPTOR-ASSOCIATED PROTEIN-TYROSINE KINASE

The synthesis and biological activity of a series of 5-[(2,5-dihydroxy benzyl)amino]salicylic acid derivatives (3-6) as analogs of the active partial structure (2) of the potent EGF-R tyrosine kinase inhibitor l avendustin A (1) are described. Analogs with an electron-withdrawing g roup in place of the carboxyl group of 2 showed activity. The N-hexyls alicylamide analog 6b (IC50 = 0.9 mu M) was about four times more pote nt than 2. (C) 1997, Published by Elsevier Science Ltd.