✦ LIBER ✦
Synthesis and biological activity of 5-[(2,5-dihydroxybenzyl)amino]salicylic acid analogs as inhibitors of EGF receptor-associated protein tyrosine kinase
✍ Scribed by Tianming Liu; Ryuichi Shirai; Takashi Matsui; Kazuo Umezawa; Shigeo Iwasaki
- Publisher
- Elsevier Science
- Year
- 1997
- Tongue
- English
- Weight
- 181 KB
- Volume
- 7
- Category
- Article
- ISSN
- 0960-894X
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✦ Synopsis
The synthesis and biological activity of a series of 5-[(2,5dihydroxybenzyl)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 IaM) was about four times more potent than 2.