Quinoxaline chemistry. Part 7. 2-[aminobenzoates]- and 2-[aminobenzoylglutamate]-quinoxalines as classical antifolate agents. Synthesis and evaluation of in vitro anticancer, anti-HIV and antifungal activity.
Thirty-three quinoxalines bearing an aminobenzoyl or aminobenzoylglutamate group on position 2 and various substituents on position 3,6,7 of the heterocycle were prepared in order to evaluate in vitro anticancer activity. Preliminary screening performed at NCI 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(-6) M. Among the series examined one compound (29) which was the most active also exhibited both in vitro anti-HIV protection and antifungal activity while in other two (31, 37) the antifungal activity was prevailing.
Loriga
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Istituto di Chimica Farmaceutica, Università di Sassari.
Piras
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Sanna
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Paglietti
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D062365:Aminobenzoates / Q000737:chemistry / Q000494:pharmacology*; D019380:Anti-HIV Agents / Q000737:chemistry / Q000494:pharmacology*; D000935:Antifungal Agents / Q000737:chemistry / Q000494:pharmacology*; D000970:Antineoplastic Agents / Q000737:chemistry / Q000494:pharmacology*; D002176:Candida albicans / Q000187:drug effects; D004354:Drug Screening Assays, Antitumor; D005493:Folic Acid Antagonists / Q000737:chemistry / Q000494:pharmacology*; D005971:Glutamates / Q000737:chemistry / Q000494:pharmacology*; D006678:HIV / Q000187:drug effects; D006801:Humans; D008826:Microbial Sensitivity Tests; D015394:Molecular Structure; D011810:Quinoxalines / Q000737:chemistry / Q000494:pharmacology*; D014407:Tumor Cells, Cultured
D062365:Aminobenzoates; D019380:Anti-HIV Agents; D000935:Antifungal Agents; D000970:Antineoplastic Agents; D005493:Folic Acid Antagonists; D005971:Glutamates; D011810:Quinoxalines; C011398:4-aminobenzoylglutamic acid