Pyrazole[3,4-d]pyrimidine derivatives loaded into halloysite as potential CDK inhibitors

Giampaolo Barone, Viviana Barra, Aldo Di Leonardo, Marina Massaro, Serena Riela, Fabrizio Lo Celso, Patrizia Cancemi, Cesar Viseras Iborra, Giancarlo Grossi, Fabrizio Lo Celso, Silvia Schenone

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1 Citation (Scopus)

Abstract

Uncontrolled cell proliferation is a hallmark of cancer as a result of rapid and deregulated progression through the cell cycle. The inhibition of cyclin-dependent kinases (CDKs) activities is a promising therapeutic strategy to block cell cycle of tumor cells. In this work we reported a new example of nanocomposites based on halloysite nanotubes (HNTs)/pyrazolo[3,4-d]pyrimidine derivatives (Si306 and Si113) as anticancer agents and CDK inhibitors. HNTs/Si306 and HNTs/Si113 nanocomposites were synthesized and characterized. The release kinetics were also investigated. Antitumoral activity was evaluated on three cancer cell lines (HeLa, MDA-MB-231 and HCT116) and the effects on cell cycle arrest in HCT116 cells were evaluated. Finally, molecular dynamics simulations were performed of the complexes between Si113 or Si306 and the active site of both CDK 1 and 2.
Original languageEnglish
Pages (from-to)1-10
Number of pages10
JournalInternational Journal of Pharmaceutics
Volume599
Publication statusPublished - 2021

All Science Journal Classification (ASJC) codes

  • Pharmaceutical Science

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