title: Antileishmanial activity evaluation of bis-lawsone analogs and DNA topoisomerase-I inhibition studies.
abstract: For the development of potent novel antileishmanial agents, 3,3'-(arylmethylene)bis(2-hydroxynaphthalene-1,4 dione) derivatives were synthesized from lawsone and evaluated for cytotoxicity on Leishmania donovani promastigotes as well as on leishmanial DNA topoisomerase-I. Enzyme inhibition studies were conducted with simultaneous and preincubation conditions. Total inhibition is compared to camptothecin (CPT), which was taken as positive control on both the systems of enzyme inhibition. The range of activity varied from 37.5 to 70 µM in simultaneous assay and 13-16 µM in preincubation assay. Furthermore, when evaluated against L. donovani promastigotes, the synthesized compounds exhibited the activity ranging from 2 to 14 µM. The results revealed that all the compounds exhibit promising antileishmanial activity.
authors.affiliation: Department of Chemistry, School of Science and Humanities, Karunya University , Coimbatore , India .
authors.forename: Garima
authors.initials: G
authors.lastname: Sharma
authors.forename: Sayan
authors.initials: S
authors.lastname: Chowdhury
authors.forename: Suman
authors.initials: S
authors.lastname: Sinha
authors.forename: Hemanta K
authors.initials: HK
authors.lastname: Majumder
authors.forename: S Vasanth
authors.initials: SV
authors.lastname: Kumar
mesh_terms: D000981:Antiprotozoal Agents / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*; D004264:DNA Topoisomerases, Type I / Q000378:metabolism*; D004278:DNA, Superhelical / Q000187:drug effects; D004587:Electrophoresis, Agar Gel; D020128:Inhibitory Concentration 50; D007893:Leishmania donovani / Q000187:drug effects* / Q000201:enzymology; D015394:Molecular Structure; D009285:Naphthoquinones / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*; D021261:Parasitic Sensitivity Tests; D010957:Plasmids; D059004:Topoisomerase I Inhibitors / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*
chemical_list: D000981:Antiprotozoal Agents; D004278:DNA, Superhelical; D009285:Naphthoquinones; D059004:Topoisomerase I Inhibitors; D004264:DNA Topoisomerases, Type I; C005090:lawsone