Synthesis, Characterization, and In Silico Studies of Novel Spirooxindole Derivatives as Ecto-5'-Nucleotidase Inhibitors.

ABSTRACT: Ecto-5'-nucleotidase (ecto-5'-NT, CD73) inhibitors are promising drug candidates for cancer therapy. Traditional efforts used to inhibit the ecto-5'-nucleotidase have involved antibody therapy or development of small molecule inhibitors that can mimic the acidic and ionizable structure of adenosine 5'-monophosphate (AMP). Herein, we report an efficient, environment friendly route for the synthesis of non-nucleotide based small molecules, i.e., substituted spirooxindole derivatives 9a-9l and investigated their inhibitory potential on human and rat recombinant ecto-5'-nucleotidase isozymes. These attempts have resulted in the identification of compound 9f (IC₅₀ = 0.15 ± 0.02 μM) inhibitor on h-ecto-5'-NT which showed 280-fold higher inhibition and compo

SUBMITTER: Ashraf A 

PROVIDER: S-EPMC7734640 | biostudies-literature | 2020 Dec

REPOSITORIES: biostudies-literature