Oxyrane derivative of alpha-lapachone is potent growth inhibitor of Trypanosoma cruzi epimastigote forms.
The investigation of trypanocidal effects against Trypanosoma cruzi and cytotoxicity in VERO cell line of several oxyranes structurally related to beta-lapachone, nor-beta-lapachone, alpha-lapachone, and 4-methoxy-1,2-naphthoquinone is described. It was found that the oxyranes 10 derived from alpha-lapachone showed an approximately the same trypanocidal activity of beta-lapachone. In addition, all the oxyranes showed less cytotoxicity than the corresponding naphthoquinones.
Jorqueira
Alessandra
A
Departamento de Química Orgânica-PQO, Instituto de Química, Universidade Federal Fluminense, 24020-150, Niterói, Rio de Janeiro, Brazil.
Gouvêa
Robson M
RM
Ferreira
Vitor F
VF
da Silva
Milton N
MN
de Souza
Maria C B V
MC
Zuma
Aline A
AA
Cavalcanti
Danielle F B
DF
Araújo
Humberto P
HP
Santos
Dilvani O
DO
Bourguignon
Saulo C
SC
D000818:Animals; D000981:Antiprotozoal Agents / Q000494:pharmacology*; D002470:Cell Survival / Q000187:drug effects; D002522:Chlorocebus aethiops; D004305:Dose-Response Relationship, Drug; D005347:Fibroblasts / Q000187:drug effects / Q000473:pathology; D006131:Growth Inhibitors / Q000494:pharmacology*; D009285:Naphthoquinones / Q000737:chemistry / Q000494:pharmacology*; D014349:Trypanosoma cruzi / Q000187:drug effects* / Q000254:growth & development*; D014709:Vero Cells
D000981:Antiprotozoal Agents; D006131:Growth Inhibitors; D009285:Naphthoquinones; C014638:beta-lapachone; C415043:alpha-lapachone