Deuteration versus ethylation - strategies to improve the metabolic fate of an ¹⁸F-labeled celecoxib derivative.

ABSTRACT: The inducible isoenzyme cyclooxygenase-2 (COX-2) is closely associated with chemo-/radioresistance and poor prognosis of solid tumors. Therefore, COX-2 represents an attractive target for functional characterization of tumors by positron emission tomography (PET). In this study, the celecoxib derivative 3-([¹⁸F]fluoromethyl)-1-[4-(methylsulfonyl)phenyl]-5-(p-tolyl)-1H-pyrazole ([¹⁸F]5a) was chosen as a lead compound having a reported high COX-2 inhibitory potency and a potentially low carbonic anhydrase binding tendency. The respective deuterated analog [D₂,¹⁸F]5a and the fluoroethyl-substituted derivative [¹⁸F]5b were selected to study the influence of these modifications with respect to COX inhibition potency in vitr

SUBMITTER: Laube M 

PROVIDER: S-EPMC9057277 | biostudies-literature | 2020 Oct

REPOSITORIES: biostudies-literature