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Your search keyword '"Bollini, M"' showing total 2 results
Start Over Author "Bollini, M" Journal bioorganic medicinal chemistry
2 results on '"Bollini, M"'

1. New potent imidazoisoquinolinone derivatives as anti-Trypanosoma cruzi agents: biological evaluation and structure-activity relationships.

Author

Bollini M, Casal JJ, Alvarez DE, Boiani L, González M, Cerecetto H, and Bruno AM

Subjects
Animals, Chagas Disease drug therapy, Dose-Response Relationship, Drug, Glutathione chemistry, Glutathione metabolism, HeLa Cells, Humans, Imidazoles metabolism, Imidazoles toxicity, Isoquinolines metabolism, Isoquinolines toxicity, Models, Molecular, Oxidation-Reduction drug effects, Quantitative Structure-Activity Relationship, Trypanocidal Agents metabolism, Trypanocidal Agents pharmacology, Trypanocidal Agents toxicity, DNA, Protozoan metabolism, Imidazoles chemistry, Imidazoles pharmacology, Isoquinolines chemistry, Isoquinolines pharmacology, Trypanocidal Agents chemical synthesis, Trypanosoma cruzi drug effects
Abstract

A series of novel benzoimidazo and N-aryl-5-oxo-imidazo[1,2-b]isoquinoline-10-carbothioamides was developed. All the compounds were evaluated for their in vitro action against the epimastigote form of Trypanosoma cruzi. Four of them showed higher activity than Nifurtimox. Their unspecific cytotoxicity was evaluated using HeLa and L6 cells, being non-toxic at concentrations at least 15 and 200 times higher than that of T. cruzi IC(50.) To gain insight into the mechanism of action, their DNA binding properties and reactivity with glutathione were studied, and QSAR study was performed.

Published
2009
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2. Design, synthesis, and antitumor activity of new bis-aminomethylnaphthalenes.

Author

Bollini M, Casal JJ, and Bruno AM

Subjects
Amination, Animals, Antineoplastic Agents chemistry, Binding Sites, Cattle, Cell Cycle drug effects, Cell Line, Tumor, Cell Proliferation drug effects, DNA chemistry, DNA drug effects, DNA Fragmentation drug effects, Drug Screening Assays, Antitumor, Flow Cytometry methods, Humans, Molecular Structure, Naphthalenes chemistry, Spectrophotometry, Ultraviolet methods, Stereoisomerism, Structure-Activity Relationship, Time Factors, Antineoplastic Agents chemical synthesis, Antineoplastic Agents pharmacology, Drug Design, Naphthalenes chemical synthesis, Naphthalenes pharmacology
Abstract

A new series of bis-aminomethylnaphthalenes were synthesized in satisfactory overall yield, through a simple synthetic strategy using reductive amination. The DNA binding properties of these compounds have been examined and compared to those of reference drugs using an UV spectroscopy method. The compounds were evaluated for their in vitro anticancer activity and some of them were studied in vivo. Compound 15 exhibited remarkable antitumor activity and represents a novel template for anticancer chemotherapy and can serve as a new lead compound.

Published
2008
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