Quinoxaline chemistry. Part 5. 2-(R)-benzylaminoquinoxalines as nonclassical antifolate agents. Synthesis and evaluation of in vitro anticancer activity

Thirty-one quinoxalines bearing a substituted benzylamino group on position 2 and various substituents on position 3,6,7 and 8 of the heterocycle were prepared in order to evaluate in vitro anticancer activity. Preliminary screening performed at NCI on twenty-two compounds showed that most derivativ...

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Bibliographic Details
Published inFarmaco (Società chimica italiana : 1989) Vol. 51; no. 8-9; p. 559
Main Authors Loriga, M, Fiore, M, Sanna, P, Paglietti, G
Format Journal Article
LanguageEnglish
Published France 01.08.1996
Subjects
Antineoplastic Agents - chemical synthesis
Antineoplastic Agents - pharmacology
Folic Acid Antagonists - chemical synthesis
Folic Acid Antagonists - pharmacology
Humans
Quinoxalines - chemical synthesis
Quinoxalines - pharmacology
Structure-Activity Relationship
Tumor Cells, Cultured
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Summary:Thirty-one quinoxalines bearing a substituted benzylamino group on position 2 and various substituents on position 3,6,7 and 8 of the heterocycle were prepared in order to evaluate in vitro anticancer activity. Preliminary screening performed at NCI on twenty-two compounds showed that most derivatives exhibited a moderate to strong growth inhibition activity on various tumor panel cell lines between 10(-5) and 10(-4) molar concentrations. Interesting selectivities were also recorded between 10(-8) and 10(-5) M.
ISSN:0014-827X