Quinoxaline chemistry. Part 4. 2(R)-anilinoquinoxalines as nonclassical antifolate agents. Synthesis, structure elucidation and evaluation of in vitro anticancer activity

Thirty-five quinoxalines bearing a substituted aniline group on position 2 and various substituents on positions 3,6,7 and 8 were prepared in order to evaluate in vitro anticancer activity. Structural elucidation of some isomeric quinoxalinones formed by ring closure of 4-substituted-1,2-diaminobenz...

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Bibliographic Details
Published inFarmaco (Società chimica italiana : 1989) Vol. 50; no. 5; p. 289
Main Authors Loriga, M, Fiore, M, Sanna, P, Paglietti, G
Format Journal Article
LanguageEnglish
Published France 01.05.1995
Subjects
Aniline Compounds - chemistry
Drug Screening Assays, Antitumor
Folic Acid Antagonists - chemical synthesis
Folic Acid Antagonists - chemistry
Folic Acid Antagonists - pharmacology
Humans
Molecular Structure
Quinoxalines - chemical synthesis
Quinoxalines - chemistry
Quinoxalines - pharmacology
Tumor Cells, Cultured
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Summary:Thirty-five quinoxalines bearing a substituted aniline group on position 2 and various substituents on positions 3,6,7 and 8 were prepared in order to evaluate in vitro anticancer activity. Structural elucidation of some isomeric quinoxalinones formed by ring closure of 4-substituted-1,2-diaminobenzenes with dicarbonyl compounds was achieved by comparison with one isomer coming from an unambiguous independent route. Preliminary in vitro screening at NCI showed that many compounds exhibited a moderate to strong growth inhibition activity on various cell lines between 10(-5) and 10(-4) molar concentrations.
ISSN:0014-827X
1879-0569