Adamantane-Substituted Purines and Their β-Cyclodextrin Complexes: Synthesis and Biological Activity.

ABSTRACT: Cyclin-dependent kinases (CDKs) play an important role in the cell-division cycle. Synthetic inhibitors of CDKs are based on 2,6,9-trisubstituted purines and are developed as potential anticancer drugs; however, they have low solubility in water. In this study, we proved that the pharmaco-chemical properties of purine-based inhibitors can be improved by appropriate substitution with the adamantane moiety. We prepared ten new purine derivatives with adamantane skeletons that were linked at position 6 using phenylene spacers of variable geometry and polarity. We demonstrated that the adamantane skeleton does not compromise the biological activity, and some of the new purines displayed even higher inhibition activity towards CDK2/cyclin E than the parental compounds. These findings were suppo

SUBMITTER: Rouchal M 

PROVIDER: S-EPMC8657435 | biostudies-literature | 2021 Nov

REPOSITORIES: biostudies-literature