Bioorganic and Medicinal Chemistry Letters p. 365 - 368 (1997)
Update date:2022-07-29
Topics:
Liu, Tianming
Shirai, Ryuichi
Matsui, Takashi
Umezawa, Kazuo
Iwasaki, Shigeo
The synthesis and biological activity of a series of 5-[(2,5-dihydroxybenzyl)amino]salicylic acid derivatives (3-6) as analogs of the active partial structure (2) of the potent EGF-R tyrosine kinase inhibitor lavendustin A (1) are described. Analogs with an electron-withdrawing group in place of the carboxyl group of 2 showed activity. The N-hexylsalicylamide analog 6b (IC50 = 0.9 μM) was about four times more potent than 2.
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(1997)
