Synthesis and biological activity of aminophthalazines and aminopyridazines as novel inhibitors of PGE 2 production in cells

…, J Dietrich, S Chappeta, B Smith, V Gokhale…

Index: Medda, Federico; Sells, Earlphia; Chang, Hui-Hua; Dietrich, Justin; Chappeta, Shashi; Smith, Breland; Gokhale, Vijay; Meuillet, Emmanuelle J.; Hulme, Christopher Bioorganic and Medicinal Chemistry Letters, 2013 , vol. 23, # 2 p. 528 - 531

Full Text: HTML

Citation Number: 5

Abstract

This Letter reports the synthesis and biological evaluation of a collection of aminophthalazines as a novel class of compounds capable of reducing production of PGE2 in HCA-7 human adenocarcinoma cells. A total of 28 analogs were synthesized, assayed for PGE2 reduction, and selected active compounds were evaluated for inhibitory activity against COX-2 in a cell free assay. Compound 2xxiv (R1= H, R2= p-CH3O) exhibited the ...