title: 4-anilinoquinoline triazines: a novel class of hybrid antimalarial agents.
abstract: A novel class of hybrid 4-anilinoquinoline triazines have been synthesized and evaluated in vitro for their antimalarial activity against CQ-sensitive 3D7 strain of P. falciparum as well as for their cytotoxicity toward VERO cell line. Five compounds (19, 20, 23, 41 and 45) exhibited the antimalarial potency superior to CQ. Compounds 14 and 16 were found to be orally active at a dose of 100 mg/kg×4 days against CQ-resistant strain of P. yoelii. Inhibition of β-hematin formation assay and molecular docking study has been conducted in order to gain insight into the mechanism of action of proposed targets for the 4-anilinoquinoline and triazine moiety of the hybrid compounds.
authors.affiliation: Division of Medicinal & Process Chemistry, Central Drug Research Institute, Lucknow 226001, India.
authors.forename: Ashok
authors.initials: A
authors.lastname: Kumar
authors.forename: Kumkum
authors.initials: K
authors.lastname: Srivastava
authors.forename: S Raja
authors.initials: SR
authors.lastname: Kumar
authors.forename: M I
authors.initials: MI
authors.lastname: Siddiqi
authors.forename: Sunil K
authors.initials: SK
authors.lastname: Puri
authors.forename: Jitendra K
authors.initials: JK
authors.lastname: Sexana
authors.forename: Prem M S
authors.initials: PM
authors.lastname: Chauhan
mesh_terms: D000818:Animals; D000962:Antimalarials / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*; D049109:Cell Proliferation / Q000187:drug effects; D002522:Chlorocebus aethiops; D006420:Hemeproteins / Q000037:antagonists & inhibitors; D008288:Malaria / Q000188:drug therapy*; D051379:Mice; D008958:Models, Molecular; D015394:Molecular Structure; D021261:Parasitic Sensitivity Tests; D010963:Plasmodium falciparum / Q000187:drug effects*; D011804:Quinolines / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*; D013237:Stereoisomerism; D013329:Structure-Activity Relationship; D014227:Triazines / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*; D014709:Vero Cells
chemical_list: D000962:Antimalarials; D006420:Hemeproteins; D011804:Quinolines; D014227:Triazines; C020753:hemozoin