Anilinoquinazoline inhibitors of fructose 1, 6-bisphosphatase bind at a novel allosteric site: synthesis, in vitro characterization, and X-ray crystallography

…, AM Mathiowetz, LD McClure, NB Nestor…

Index: Wright, Stephen W.; Carlo, Anthony A.; Carty, Maynard D.; Danley, Dennis E.; Hageman, David L.; Karam, George A.; Levy, Carolyn B.; Mansour, Mahmoud N.; Mathiowetz, Alan M.; McClure, Lester D.; Nestor, Nestor B.; McPherson, R. Kirk; Pandit, Jayvardhan; Pustilnik, Leslie R.; Schulte, Gayle K.; Soeller, Walter C.; Treadway, Judith L.; Wan, Ing-Kae; Bauer, Paul H. Journal of Medicinal Chemistry, 2002 , vol. 45, # 18 p. 3865 - 3877

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Citation Number: 84

Abstract

The synthesis and in vitro structure-activity relationships (SAR) of a novel series of anilinoquinazolines as allosteric inhibitors of fructose-1, 6-bisphosphatase (F16Bpase) are reported. The compounds have a different SAR as inhibitors of F16Bpase than anilinoquinazolines previously reported. Selective inhibition of F16Bpase can be attained through the addition of appropriate polar functional groups at the quinazoline 2-position, ...