title: New developments in diketo-containing inhibitors of HIV-1 integrase.
abstract: HIV-1 integrase is one of the three enzymes, which are critical for viral replication. It catalyzes the integration of the HIV genome into the cellular chromosome. Since there is no known human homolog to integrase, its inhibition is one of the most promising novel drug targets for anti-retroviral therapy with potential advantage over existing therapies. To date, numerous compounds with diverse structural features have been reported as integrase inhibitors, among which the diketo-containing inhibitors of HIV-1 integrase represent a major lead for anti-HIV drug development. The discovery of diketo acids plays an important role in validating integrase as a legitimate target for treatment of AIDS. In this review, we summarize several drug candidates in clinical trials and new diketo-containing inhibitors of HIV-1 integrase discovered recently.
authors.affiliation: College of Pharmacy, Shandong University, Jinan, Shandong, PR China. guisenzhao@sdu.edu.cn
authors.forename: Guisen
authors.initials: G
authors.lastname: Zhao
authors.forename: Chao
authors.initials: C
authors.lastname: Wang
authors.forename: Chuan
authors.initials: C
authors.lastname: Liu
authors.forename: Hongxiang
authors.initials: H
authors.lastname: Lou
mesh_terms: D000163:Acquired Immunodeficiency Syndrome / Q000188:drug therapy; D002986:Clinical Trials as Topic; D015195:Drug Design; D019427:HIV Integrase / Q000187:drug effects*; D019428:HIV Integrase Inhibitors / Q000737:chemistry* / Q000494:pharmacology / Q000627:therapeutic use; D006571:Heterocyclic Compounds / Q000737:chemistry / Q000494:pharmacology / Q000627:therapeutic use; D006801:Humans; D007651:Keto Acids / Q000737:chemistry* / Q000494:pharmacology / Q000627:therapeutic use; D013329:Structure-Activity Relationship
chemical_list: D019428:HIV Integrase Inhibitors; D006571:Heterocyclic Compounds; D007651:Keto Acids; D019427:HIV Integrase