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

Sandra Piras; Mario Loriga; Giuseppe Paglietti

doi:10.1016/j.farmac.2003.11.014

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

Farmaco. 2004 Mar;59(3):185-94. doi: 10.1016/j.farmac.2003.11.014.

Authors

Sandra Piras¹, Mario Loriga, Giuseppe Paglietti

Affiliation

¹ Dipartimento Farmaco Chimico Tossicologico, Università di Sassari, via Muroni 23A, Sassari 07100, Italy.

PMID: 14987981
DOI: 10.1016/j.farmac.2003.11.014

Abstract

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.

MeSH terms

Antimetabolites, Antineoplastic / chemical synthesis*
Antimetabolites, Antineoplastic / pharmacology*
Cell Division / drug effects
Cell Line, Tumor
Drug Screening Assays, Antitumor
Humans
Indicators and Reagents
Magnetic Resonance Spectroscopy
Methotrexate / analogs & derivatives*
Methotrexate / chemical synthesis*
Methotrexate / pharmacology
Quinoxalines / chemical synthesis*
Quinoxalines / pharmacology*
Spectrophotometry, Infrared
Spectrophotometry, Ultraviolet

Substances

Antimetabolites, Antineoplastic
Indicators and Reagents
Quinoxalines
Methotrexate