title: Chalcone-benzoxaborole hybrid molecules as potent antitrypanosomal agents.
abstract: We report the novel chalcone-benzoxaborole hybrids and their structure-activity relationship against Trypanosoma brucei  parasites. The 4-NH(2) derivative 29 and 3-OMe derivative 43 were found to have excellent potency. The synergistic 4-NH(2)-3-OMe compound 49 showed an IC(50) of 0.010 μg/mL and resulted in 100% survival and zero parasitemia in a murine infection model, which represents one of the most potent compounds discovered to date from the benzoxaborole class that inhibit  T. brucei  growth.
authors.affiliation: School of Pharmacy, Shanghai Jiao Tong University, 200240, Shanghai, China.
authors.forename: Zhitao
authors.initials: Z
authors.lastname: Qiao
authors.forename: Qi
authors.initials: Q
authors.lastname: Wang
authors.forename: Fenglong
authors.initials: F
authors.lastname: Zhang
authors.forename: Zhongli
authors.initials: Z
authors.lastname: Wang
authors.forename: Tana
authors.initials: T
authors.lastname: Bowling
authors.forename: Bakela
authors.initials: B
authors.lastname: Nare
authors.forename: Robert T
authors.initials: RT
authors.lastname: Jacobs
authors.forename: Jiong
authors.initials: J
authors.lastname: Zhang
authors.forename: Dazhong
authors.initials: D
authors.lastname: Ding
authors.forename: Yangang
authors.initials: Y
authors.lastname: Liu
authors.forename: Huchen
authors.initials: H
authors.lastname: Zhou
mesh_terms: D000818:Animals; D001896:Boron Compounds / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology; D045744:Cell Line, Tumor; D047188:Chalcones / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology; D020128:Inhibitory Concentration 50; D051379:Mice; D021261:Parasitic Sensitivity Tests; D013329:Structure-Activity Relationship; D014344:Trypanocidal Agents / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology; D014346:Trypanosoma brucei brucei / Q000187:drug effects*; D014353:Trypanosomiasis, African / Q000188:drug therapy
chemical_list: D001896:Boron Compounds; D047188:Chalcones; D014344:Trypanocidal Agents