Discovery of 5-[5-fluoro-2-oxo-1, 2-dihydroindol-(3 Z)-ylidenemethyl]-2, 4-dimethyl-1 H-pyrrole-3-carboxylic acid (2-diethylaminoethyl) amide, a novel tyrosine kinase …

…, C Liang, S Shirazian, Y Zhou, T Miller…

Index: Sun, Li; Liang, Chris; Shirazian, Sheri; Zhou, Yong; Miller, Todd; Cui, Jean; Fukuda, Juri Y.; Chu, Ji-Yu; Nematalla, Asaad; Wang, Xueyan; Chen, Hui; Sistla, Anand; Luu, Tony C.; Tang, Flora; Wei, James; Tang, Cho Journal of Medicinal Chemistry, 2003 , vol. 46, # 7 p. 1116 - 1119

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Citation Number: 435

Abstract

To improve the antitumor properties and optimize the pharmaceutical properties including solubility and protein binding of indolin-2-ones, a number of different basic and weakly basic analogues were designed and synthesized. 5-[5-Fluoro-2-oxo-1, 2-dihydroindol-(3 Z)- ylidenemethyl]-2, 4-dimethyl-1 H-pyrrole-3-carboxylic acid (2-diethylaminoethyl) amide (12b or SU11248) has been found to show the best overall profile in terms of potency for the ...