2. Academic Validation
  3. 3-arylamino and 3-alkoxy-nor-beta-lapachone derivatives: synthesis and cytotoxicity against cancer cell lines

3-arylamino and 3-alkoxy-nor-beta-lapachone derivatives: synthesis and cytotoxicity against cancer cell lines

  • J Med Chem. 2010 Jan 14;53(1):504-8. doi: 10.1021/jm900865m.
Eufrânio N da Silva Jr 1,  Clara F de Deus,  Bruno C Cavalcanti,  Cláudia Pessoa,  Letícia V Costa-Lotufo,  Raquel C Montenegro,  Manoel O de Moraes,  Maria do Carmo F R Pinto,  Carlos A de Simone,  Vitor F Ferreira,  Marilia O F Goulart,  Carlos Kleber Z Andrade,  Antônio V Pinto
Affiliations

Affiliation

  • 1 Instituto de Quimica, Universidade de Brasilia, 70910-970 Brasilia, DF, Brazil.
PMID: 19947600 DOI: 10.1021/jm900865m
Abstract

Several 3-arylamino and 3-alkoxy-nor-beta-lapachone derivatives were synthesized in moderate to high yields and found to be highly potent against Cancer cells SF295 (central nervous system), HCT8 (colon), MDA-MB435 (melanoma), and HL60 (leukemia), with IC(50) below 2 microM. The arylamino para-nitro and the 2,4-dimethoxy substituted naphthoquinones showed the best cytoxicity profile, while the ortho-nitro and the 2,4-dimethoxy substituted ones were more selective than doxorubicin and similar to the precursor lapachones, thus emerging as promising new lead compounds in Anticancer drug development.

Figures