Synthesis of nitroaromatic compounds as potential anticancer agents.
Twenty-seven nitrated and non-nitrated compounds have been synthesized and tested for their growth inhibitory activity on three human cancer cells lines. Fourteen compounds were able to inhibit more than 50% of the growth of at least one of the cancer cell lines and five compounds exhibited high antiproliferative activity on human cancer cell lines (IC50 < 8.5 μM). The cytotoxicity of the compounds on Vero cell line was established in vitro to evaluate the selectivity. All active compounds have a good leaving group (bromide or chloride) at the benzylic position, indicating that the mechanism of action of these compounds is related to their alkylating properties. Two compounds (3 and 24) were selected for further studies in mice with Ehrlich solid tumors and display significant antitumor effects in vivo.
Marcela Silva
MS
Lopes
Camila Filizzola
CF
de Andrade Sena
Bruno Leonardo
BL
Silva
Cristina Maria
CM
de Souza
Jonas Pereira
JP
Ramos
Geovanni Dantas
GD
Cassali
Elaine Maria
EM
de Souza-Fagundes
Ricardo Jose
RJ
Alves
Mônica Cristina
MC
de Oliveira
Department of Pharmaceutical Products, Pharmacy Faculty, Federal University of Minas Gerais, Belo Horizonte, Minas Gerais, Brazil. renatabo@farmacia.ufmg.br.
Renata Barbosa
RB
de Oliveira
D000818:Animals; D000970:Antineoplastic Agents / Q000737:chemistry* / Q000494:pharmacology*; D002460:Cell Line; D045744:Cell Line, Tumor; D049109:Cell Proliferation / Q000187:drug effects; D002522:Chlorocebus aethiops; D004354:Drug Screening Assays, Antitumor / Q000379:methods; D005260:Female; D018922:HL-60 Cells; D006801:Humans; D019169:Jurkat Cells; D061986:MCF-7 Cells; D051379:Mice; D009574:Nitro Compounds / Q000737:chemistry* / Q000494:pharmacology*; D014709:Vero Cells
D000970:Antineoplastic Agents; D009574:Nitro Compounds