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207 results on '"DATTOLO G"'

29. 1-Methyl-3H-pyrazolo[1,2-a]benzo[1,2,3,4]tetrazin-3-ones. Design, Synthesis, and Biological Activity of New Antitumor Agents

Author

Almerico, A. M., Mingoia, F., Diana, P., Barraja, P., Lauria, A., Montalbano, A., Cirrincione, G., and Dattolo, G.

Abstract

1-Methylpyrazolo[1,2-a]benzo[1,2,3,4]tetrazin-3-ones 4, synthesized in good to excellent yields, were designed as novel alkylating agents because of their peculiar chemical behavior. All derivatives showed antiproliferative activity against more than 50 types of tumor cell lines with GI50 reaching sub-micromolar values. SAR studies revealed that the presence of a chlorine atom is well-tolerated in both positions 8 and 9, whereas in the case of the methyl group, switching from the 8 to the 9 position gives rise to the most active compound of the series, 4g, either for the number of cell lines inhibited and for selectivity against leukaemia and renal cancer subpanels. COMPARE and 3D-MIND computations indicate, for compounds 4, an activity profile analogous to rifamycins and cytidine analogues.

Published
2005

30. Synthesis and antiproliferative activity of [1,2,4] triazino[4,3-a]indoles

Author

Barraja, P., Diana, P., Antonino Lauria, Montalbano, A., Almerico, A. M., Dattolo, G., Cirrincione, G., BARRAJA P, DIANA P, LAURIA A, MONTALBANO A, ALMERICO AM, DATTOLO G, and CIRRINCIONE G

Subjects
antiproliferative activity, Indoles, Triazines, Cell Line, Tumor, Neoplasms, 2-diazoindole, triazinoindole, Humans, Antineoplastic Agents, Drug Screening Assays, Antitumor, Settore CHIM/08 - Chimica Farmaceutica
Abstract

A series of [1, 2, 4triazino[4,3-a]indoles was prepared in good yield by reacting 2-diazo-3-ethoxycarbonylindole with methylene active compounds. Derivatives of the title ring system were tested against a panel of 60 human tumor cell lines, and showed inhibitory activity against a wide range of cancer cell lines at micromolar concentration.

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