title: Synthesis and cytotoxicity of novel pyrido[1,2-e]purines on multidrug resistant human MCF7 cells.
abstract: The anticancer activity of 4-methylaminopyridol[1,2-e]purine 6a, 4-(piperidin-1-yl)pyrido[1,2-e]purine 7a and their 7-methyl derivatives 6b, 7b was investigated against the human MCF7 cancer cell line in vitro. The sensitive cell line showed a range of sensitivities to 6a, 6b, 7a, 7b (IC50: 1.6 to 7.2 x 10(-4) M) and sensitivity to doxorubicin (IC50: 7.5 x 10(-7) M). A resistant cell line with the multidrug resistant phenotype was sensitive to these derivatives (IC50: 1.8 to 6.7 x 10(-4) M), doxorubicin (IC50: 5 x 10(-5) M) and drug activity seems to be not affected by MDR resistance. Our data show that 6a, 6b, 7a and 7b appear to exert a low cytotoxicity on sensitive and MDR resistant MCF7 human cancer cell lines.
authors.affiliation: Laboratoire d'oncopharmacologie-pharmacie, Centre Régional de Lutte contre le Cancer Val-d'Aurelle-Paul Lamarque, Montpellier, France.
authors.forename: F
authors.initials: F
authors.lastname: Pinguet
authors.forename: S
authors.initials: S
authors.lastname: Mavel
authors.forename: C
authors.initials: C
authors.lastname: Galtier
authors.forename: A
authors.initials: A
authors.lastname: Gueiffier
mesh_terms: D020168:ATP Binding Cassette Transporter, Subfamily B, Member 1 / Q000378:metabolism; D000903:Antibiotics, Antineoplastic / Q000494:pharmacology; D000911:Antibodies, Monoclonal / Q000494:pharmacology; D000970:Antineoplastic Agents / Q000138:chemical synthesis* / Q000494:pharmacology; D002460:Cell Line; D004396:Coloring Agents; D004317:Doxorubicin / Q000494:pharmacology; D018432:Drug Resistance, Multiple / Q000235:genetics*; D006801:Humans; D011687:Purines / Q000138:chemical synthesis* / Q000494:pharmacology; D013778:Tetrazolium Salts; D013844:Thiazoles; D014407:Tumor Cells, Cultured
chemical_list: D020168:ATP Binding Cassette Transporter, Subfamily B, Member 1; D000903:Antibiotics, Antineoplastic; D000911:Antibodies, Monoclonal; D000970:Antineoplastic Agents; D004396:Coloring Agents; D011687:Purines; D013778:Tetrazolium Salts; D013844:Thiazoles; D004317:Doxorubicin; C022616:thiazolyl blue