title: Synthesis of a series of novel 2,4,5-trisubstituted selenazole compounds as potential PLTP inhibitors.
abstract: Based on a homology-modeled structure of PLTP and characteristic structural features of reported cholesteryl ester transfer protein (CETP) inhibitors, we designed and synthesized a novel series of 2,4,5-trisubstituted selenazole compounds. Biological evaluation reveals that compounds 12 and 17 exhibit favorable PLTP activity, and their IC(50)s are 8 microM and 10 microM, respectively.
authors.affiliation: Laboratory of Computer-Aided Drug Design & Discovery, Beijing Institute of Pharmacology and Toxicology, Beijing, PR China.
authors.forename: Cui
authors.initials: C
authors.lastname: Ling
authors.forename: Zhibing
authors.initials: Z
authors.lastname: Zheng
authors.forename: Xian Cheng
authors.initials: XC
authors.lastname: Jiang
authors.forename: Wu
authors.initials: W
authors.lastname: Zhong
authors.forename: Song
authors.initials: S
authors.lastname: Li
mesh_terms: D001393:Azoles / Q000737:chemistry*; D004353:Drug Evaluation, Preclinical; D020128:Inhibitory Concentration 50; D049294:Phospholipid Transfer Proteins / Q000037:antagonists & inhibitors*; D018036:Selenium Compounds / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*
chemical_list: D001393:Azoles; D049294:Phospholipid Transfer Proteins; D018036:Selenium Compounds