Discovery and synthesis of novel 4-aminopyrrolopyrimidine Tie-2 kinase inhibitors for the treatment of solid tumors

…, MA Berliner, V Bernardo, M Boehm, GV Borzillo…

Index: Arcari, Joel T.; Beebe, Jean S.; Berliner, Martin A.; Bernardo, Vincent; Boehm, Merin; Borzillo, Gary V.; Clark, Tracey; Cohen, Bruce D.; Connell, Richard D.; Frost, Heather N.; Gordon, Deborah A.; Hungerford, William M.; Kakar, Shefali M.; Kanter, Aaron; Keene, Nandell F.; Knauth, Elizabeth A.; Lagreca, Susan D.; Lu, Yong; Martinez-Alsina, Louis; Marx, Matthew A.; Morris, Joel; Patel, Nandini C.; Savage, Doug; Soderstrom, Cathy I.; Thompson, Carl; Tkalcevic, George; Tom, Norma J.; Vajdos, Felix F.; Valentine, James J.; Vincent, Patrick W.; Wessel, Matthew D.; Chen, Jinshan M. Bioorganic and Medicinal Chemistry Letters, 2013 , vol. 23, # 10 p. 3059 - 3063

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Citation Number: 6

Abstract

The synthesis and biological evaluation of novel Tie-2 kinase inhibitors are presented. Based on the pyrrolopyrimidine chemotype, several new series are described, including the benzimidazole series by linking a benzimidazole to the C5-position of the 4-amino- pyrrolopyrimidine core and the ketophenyl series synthesized by incorporating a ketophenyl group to the C5-position. Medicinal chemistry efforts led to potent Tie-2 inhibitors. ...