Tyrosine kinase inhibitors. 1. Structure-activity relationships for inhibition of epidermal growth factor receptor tyrosine kinase activity by 2, 3-dihydro-2-thioxo-1H-indole …

AM Thompson, GW Rewcastle, M Tercel…

Index: Thompson; Rewcastle; Tercel; Dobrusin; Fry; Kraker; Denny Journal of Medicinal Chemistry, 1993 , vol. 36, # 17 p. 2459 - 2469

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Citation Number: 30

Abstract

Corresponding 2, 3-dihydro-2-oxo-lH-indole-3-alkanoic acid esters. The monomeric thiones undergo facile and reversible oxidation to the corresponding 2, 2'-dithiobis (1H-indole-3- alkanoic acids). The compounds were evaluated for their abilities to inhibit the tyrosine kinase activity of the epidermal growth factor receptor using a native complex contained in plasma membrane vesicles shed from cultured A431 cells, and to inhibit the growth of ...

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