The synthesis and biological activity of C2-fluorinated pyrrolo [2, 1-c][1, 4] benzodiazepines

IA O'Neil, S Thompson, SB Kalindjian, TC Jenkins

Index: O'Neil, Ian A.; Thompson, Stephen; Kalindjian, S. Barret; Jenkins, Terence C. Tetrahedron Letters, 2003 , vol. 44, # 42 p. 7809 - 7812

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Citation Number: 29

Abstract

The novel C2-fluorinated pyrrolobenzodiazepines (1, 2 and 3) have been prepared from commercially available trans-hydroxyproline in good overall yield and were screened for in vitro cytotoxicity against a number of cancer cell lines. The 2R-fluoro isomer 2 exhibits an activity of 76 nM against the CH1 cell line.