Quinoxaline chemistry. Part XVII. Methyl [4-(substituted 2-quinoxalinyloxy) phenyl] acetates and ethyl N-([4-(substituted 2-quinoxalinyloxy) phenyl] acetyl) glutamates analogs of methotrexate: synthesis and evaluation of in vitro anticancer activity.
Fourteen out of 21 quinoxaline derivatives described in the present paper were selected at NCI for evaluation of their in vitro anticancer activity. Preliminary screening showed that some derivatives exhibited a moderate to strong growth inhibition activity on various tumor panel cell lines between 10(-5) and 10(-4) M concentrations. Interesting selectivities were also recorded between 10(-8) and 10(-6) M for the compounds 9 and 13.
Dipartimento Farmaco Chimico Tossicologico, Università di Sassari, via Muroni 23A, Sassari 07100, Italy.
Sandra
S
Piras
Mario
M
Loriga
Giuseppe
G
Paglietti
D000964:Antimetabolites, Antineoplastic / Q000138:chemical synthesis* / Q000494:pharmacology*; D002455:Cell Division / Q000187:drug effects; D045744:Cell Line, Tumor; D004354:Drug Screening Assays, Antitumor; D006801:Humans; D007202:Indicators and Reagents; D009682:Magnetic Resonance Spectroscopy; D008727:Methotrexate / Q000031:analogs & derivatives* / Q000138:chemical synthesis* / Q000494:pharmacology; D011810:Quinoxalines / Q000138:chemical synthesis* / Q000494:pharmacology*; D013055:Spectrophotometry, Infrared; D013056:Spectrophotometry, Ultraviolet
D000964:Antimetabolites, Antineoplastic; D007202:Indicators and Reagents; D011810:Quinoxalines; D008727:Methotrexate