Ontology highlight
ABSTRACT:
SUBMITTER: Dutour R
PROVIDER: S-EPMC5683706 | biostudies-literature | 2017 Nov
REPOSITORIES: biostudies-literature
Dutour Raphaël R Cortés-Benítez Francisco F Roy Jenny J Poirier Donald D
ACS medicinal chemistry letters 20171011 11
Inhibition of cytochrome P450 (CYP) 1B1 is a promising therapeutic strategy, as such an inhibitor could modulate the bioactivation of procarcinogens while reducing drug resistance. Based on docking studies, the synthesis of 12 estra-1,3,5(10)-triene derivatives containing a pyridin-3-/4-yl moiety at position C2, C3, or C4 was performed, and we measured their inhibitory activity on CYP1B1 using the ethoxyresorufin-<i>O</i>-deethylase (EROD) assay. The position of the nitrogen atom in the aromatic ...[more]