Novel Malonamide Derivatives as. ALPHA. v. BETA. 3 Antagonists. Syntheses and Evaluation of 3-(3-Indolin-1-yl-3-Oxopropanoyl) aminopropanoic Acids on …

S Nagashima, S Akamatsu, E Kawaminami…

Index: Nagashima; Akamatsu; Kawaminami; Kawazoe; Ogami; Matsumoto; Okada; Suzuki; Tsukamoto Chemical and Pharmaceutical Bulletin, 2001 , vol. 49, # 11 p. 1420 - 1432

Full Text: HTML

Citation Number: 10

Abstract

In attempt to find novel integrin α v β 3 antagonists, we selected SC65811 and its guanidine analogue (1) as lead compounds. Modification of the glycine part of SC65811 led to a new series of malonamide derivatives that exhibited α v β 3 inhibitory activity. Among them,(R, S)- 3-{3-[6-(3-benzylureido) indolin-1-yl]-3-oxopropanoyl-amino}-3-(pyridin-3-yl) propanoic acid (43a) showed not only potent activity with an IC 50 value of 3.0 nM but also good ...