title: Facile synthesis of antimalarial 1,2-disubstituted 4-quinolones from 1,3-bisaryl-monothio-1,3-diketones.
abstract: A new strategy was developed to synthesize 1,2-disubstituted 4-quinolones in good yield starting from 1,3-bisaryl-monothio-1,3-diketone substrates. The synthesized compounds were evaluated for antimalarial activity using Plasmodium falciparum strains. All compounds, except for two, showed good activity. Of these, seven compounds exhibited an excellent antimalarial activity (IC50, <2 μM). More importantly, all seven compounds were equally effective in inhibiting the growth of both chloroquine-sensitive and chloroquine-resistant strains. The cytotoxicity assessment using carcinoma and non-carcinoma human cell lines revealed that almost all synthesized compounds were minimally cytotoxic (IC50, >50 μM).
authors.affiliation: Department of Studies in Chemistry, University of Mysore, Manasagangothri, Mysore 570006, India. mpsadashiva@gmail.com rangappaks@yahoo.com.
authors.forename: Ajjampura C
authors.initials: AC
authors.lastname: Vinayaka
authors.forename: Maralinganadoddi P
authors.initials: MP
authors.lastname: Sadashiva
authors.forename: Xianzhu
authors.initials: X
authors.lastname: Wu
authors.forename: Sergei S
authors.initials: SS
authors.lastname: Biryukov
authors.forename: José A
authors.initials: JA
authors.lastname: Stoute
authors.forename: Kanchugarakoppal S
authors.initials: KS
authors.lastname: Rangappa
authors.forename: D Channe
authors.initials: DC
authors.lastname: Gowda
mesh_terms: D042462:4-Quinolones / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*; D000962:Antimalarials / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*; D002460:Cell Line; D045744:Cell Line, Tumor; D006801:Humans; D016778:Malaria, Falciparum / Q000188:drug therapy*; D010963:Plasmodium falciparum / Q000187:drug effects*
chemical_list: D042462:4-Quinolones; D000962:Antimalarials