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128. 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

130. Derivatives of the New Ring System Indolo[1,2-c]benzo[1,2,3]triazine with Potent Antitumor and Antimicrobial Activity

Author

Cirrincione, G., Almerico, A. M., Barraja, P., Diana, P., Lauria, A., Passannanti, A., Musiu, C., Pani, A., Murtas, P., Minnei, C., Marongiu, M. E., and Colla, P. La

Abstract

Derivatives of the new ring system indolo[1,2-c]benzo[1,2,3]triazine 5 were synthesized by diazotization of substituted 2-(2-aminophenyl)indoles followed by an intramolecular coupling reaction of the diazonium group with the indole nitrogen. To obtain the indolobenzotriazine system it was necessary to protect the 3 position of the indole nucleus to avoid cyclization into the indolo[3,2-c]cinnoline system 4. Indolobenzotriazines 5a−g were evaluated in vitro for antitumor activity against a panel of leukemia-, lymphoma-, carcinoma-, and neuroblastoma-derived cell lines. Some compounds inhibited the proliferation of T and B cell lines at submicromolar concentrations, whereas their activity against solid tumor cell lines was in the micromolar range. When evaluated for their antifungal potential 5a,d inhibited some of the fungi tested, although at concentrations very close to those inhibiting the proliferation of human cells. On the contrary, all indolobenzotriazines proved fairly potent and selective inhibitors of Streptococcus and Staphylococcus. In particular 5b,c,g were up to 80 times more potent than the reference drug streptomycin and inhibited the growth of the above Gram-positive bacteria at concentrations far lower than those cytotoxic for animal cells.

Published
1999

132. 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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