Tyrosine Kinase Inhibitors. 4. Structure-Activity Relationships among N-and 3-Substituted 2, 2'-Dithiobis (1H-indoles) for in vitro Inhibition of Receptor and Nonreceptor …

BD Palmer, GW Rewcastle, AM Thompson…

Index: Palmer; Rewcastle; Thompson; Boyd; Showalter; Sercel; Fry; Kraker; Denny Journal of Medicinal Chemistry, 1995 , vol. 38, # 1 p. 58 - 67

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Citation Number: 66

Abstract

A series of 3-substituted 2, 2'-dithiobis (lH-indoles) were synthesized and evaluated for their ability to inhibit the tyrosine kinase activity of both the epidermal growth factor receptor (EGFR) and the nonreceptor pp60v-src tyrosine kinase, to extend the available structure- activity relationships for this series. The majority of the compounds were prepared either by reaction of 2-chloro-1-methylindole-3-carbonyl chloride with amines, followed by ...