Synthesis and cytotoxicity of novel pyrido[1,2-e]purines on multidrug resistant human MCF7 cells

• Published in: Pharmazie Vol. 54; no. 12; pp. 876 - 878
• Main Authors: Pinguet, F, Mavel, S, Galtier, C, Gueiffier, A
• Format: Journal Article
• Language: English
• Published: ESCHBORN GOVI-VERLAG GMBH 01.12.1999
• Subjects: Antibiotics, Antineoplastic - pharmacology; Antibodies, Monoclonal - pharmacology; Antineoplastic Agents - chemical synthesis; Antineoplastic Agents - pharmacology; ATP-Binding Cassette, Sub-Family B, Member 1 - metabolism; Cell Line; Chemistry; Chemistry, Medicinal; Chemistry, Multidisciplinary; Coloring Agents; Doxorubicin - pharmacology; Drug Resistance, Multiple - genetics; Humans; Life Sciences & Biomedicine; Pharmacology & Pharmacy; Physical Sciences; Purines - chemical synthesis; Purines - pharmacology; Science & Technology; Tetrazolium Salts; Thiazoles; Tumor Cells, Cultured; ANTINEOPLASTIC AGENTS; GAMMA-CARBOLINES; IMIDAZO<1,2-A>PYRIDINES
• ISSN: 0031-7144

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 (TC50: 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.