New antimitotic agents with activity in multi-drug-resistant cell lines and in vivo efficacy in murine tumor models

…, SL Gwaltney, JR Wu-Wong, L Gehrke…

Index: Szczepankiewicz; Chiou; Credo; Alder; Nukkala; Zielinski; Jarvis; Mollison; Frost; Bauch; Hui; Liu; Claiborne; Li; Rosenberg; Jae; Tasker; Gunawardana; Von Geldern; Gwaltney II; Wu-Wong; Gehrke Journal of Medicinal Chemistry, 2001 , vol. 44, # 25 p. 4416 - 4430

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Citation Number: 69

Abstract

During a screen for compounds that could inhibit cell proliferation, a series of new tubulin- binding compounds was identified with the discovery of oxadiazoline 1 (A-105972). This compound showed good cytotoxic activity against non-multi-drug-resistant and multi-drug- resistant cancer cell lines, but its utility in vivo was limited by a short half-life. Medicinal chemistry efforts led to the discovery of indolyloxazoline 22g (A-259745), which ...