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3. Effects of interleukin-1 beta and interleukin-2 on amino acids levels in mouse cortex and hippocampus

Author

Zonta N, Mauro Bianchi, Alberto E. Panerai, and P. Ferrario

Subjects
Male, medicine.medical_specialty, Glutamic Acid, Mice, Inbred Strains, Hippocampal formation, Biology, Hippocampus, gamma-Aminobutyric acid, Mice, Internal medicine, Aspartic acid, medicine, Animals, Amino Acids, Beta (finance), gamma-Aminobutyric Acid, chemistry.chemical_classification, Cerebral Cortex, General Neuroscience, Interleukin, Glutamic acid, Amino acid, Glutamine, Endocrinology, chemistry, Interleukin-2, Injections, Intraperitoneal, medicine.drug, Interleukin-1
Abstract

We measured the levels of glutamine, aspartic acid, glutamic acid and GABA in cortex and hippocampus of mice acutely treated with i.p. human recombinant interleukin-2 (IL-2) or human recombinant interleukin-1 beta (IL-1 beta). Administration of IL-2 (5.0 micrograms kg-1) induced a slight but statistically significant increase in glutamine concentrations in both brain areas, while similar administration of IL-1 beta (20 micrograms kg-1) significantly reduced the hippocampal levels of glutamine, glutamic acid and GABA. Our data suggest that brain amino acid pathways are involved in the central modifications induced by IL-1 beta.

Published
1995

4. Design, synthesis and structure-activity relationship of 2-(3',4',5'-trimethoxybenzoyl)-benzo[b]furan derivatives as a novel class of inhibitors of tubulin polymerization

Author

Stefania Grimaudo, Nicola Zonta, Ernest Hamel, Carlota Lopez Cara, Andrea Brancale, Maria Rosaria Pipitone, Olga Cruz-Lopez, Pier Giovanni Baraldi, Manlio Tolomeo, Maria Dora Carrion, Romeo Romagnoli, Jan Balzarini, Antonietta Di Cristina, Romagnoli, R, Baraldi, PG, Carrion, MD, Cara, CL, Cruz-Lopez, O, Tolomeo, M, Grimaudo, S, Di Cristina, A, Pipitone, RM, Balzarini, J, Zonta, N, Brancale, A, and Hamel, E

Subjects
structure-activity, Stereochemistry, Clinical Biochemistry, Pharmaceutical Science, Antineoplastic Agents, macromolecular substances, Biochemistry, Chemical synthesis, Article, Structure-Activity Relationship, chemistry.chemical_compound, benzo[b]furans, Microtubule, Cell Line, Tumor, Furan, Drug Discovery, Humans, Structure–activity relationship, Molecular Biology, Benzofurans, Cell Proliferation, Binding Sites, Dose-Response Relationship, Drug, biology, Chemistry, Tubulin Modulators, Cell growth, Cell Cycle, Organic Chemistry, Small molecule, tubulin polymerization, Tubulin, Drug Design, biology.protein, Molecular Medicine, Protein Multimerization, Colchicine
Abstract

The biological importance of microtubules in mitosis and cell division makes them an interesting target for the development of anticancer agents. Small molecules such as benzo[b]furans are attractive as inhibitors of tubulin polymerization. Thus, a new class of inhibitors of tubulin polymerization based on the 2-(3′,4′,5′-trimethoxybenzoyl)-benzo[b]furan molecular skeleton, with electron-donating (Me, OMe or OH) or electron-withdrawing (F, Cl and Br) substituents on the benzene ring, was synthesized and evaluated for antiproliferative activity, inhibition of tubulin polymerization and cell cycle effects. Adding a methyl group at the C-3 position resulted in increased activity. The most promising compound in this series was 2-(3′,4′,5′-trimethoxybenzoyl)-3-methyl-6-ethoxy-benzo[b]furan, which inhibits cancer cell growth at nanomolar concentrations and interacts strongly with tubulin by binding to the colchicine site.

Published
2009

5. Synthesis and Biological Evaluation of 1-Methyl-2-(3',4',5'-trimethoxybenzoyl)-3-aminoindoles as a New Class of Antimitotic Agents and Tubulin Inhibitors

Author

Hsing Pang Hsieh, Taradas Sarkar, Nicola Zonta, Pier Giovanni Baraldi, Stefania Grimaudo, Romeo Romagnoli, Mojgan Aghazadeh Tabrizi, Manlio Tolomeo, Andrea Brancale, Jan Balzarini, Carlota Lopez Cara, Maria Dora Carrion, Olga Cruz-Lopez, Ernest Hamel, Delia Preti, Antonella Di Cristina, ROMAGNOLI R, BARALDI PG, SARKAR T, CARRION MD, CARA CL, CRUZ-LOPEZ O, PRETI D, TABRIZI MA, TOLOMEO M, GRIMAUDO S, DI CRISTINA A, ZONTA N, BALZARINI J, BRANCALE A, HSIEH HP, and HAMEL E

Subjects
Models, Molecular, Indoles, Stereochemistry, Alkylation, Antimitotic Agents, Chemical synthesis, Mice, Structure-Activity Relationship, Biopolymers, Tubulin, Cell Line, Tumor, Drug Discovery, Structure–activity relationship, Animals, Humans, Indole test, Binding Sites, biology, Tubulin Modulators, Chemistry, Biological activity, biology.protein, Molecular Medicine, Antimitotic Agent, Drug Screening Assays, Antitumor, Colchicine, Protein Binding
Abstract

The 2-(3,4,5-trimethoxybenzoyl)-2-aminoindole nucleus was used as the fundamental structure for the synthesis of compounds modified with respect to positions C-4 to C-7 with different moieties (chloro, methyl, or methoxy). Additional structural variations concerned the indole nitrogen, which was alkylated with small alkyl groups such as methyl or ethyl. We have identified 1-methyl-2-(3,4,5-trimethoxybenzoyl)-3-amino-7-methoxyindole as a new highly potent antiproliferative agent that targets tubulin at the colchicine binding site and leads to apoptotic cell death.

Published
2008

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