Journal
INTERNATIONAL JOURNAL OF PHARMACEUTICS
Volume 599, Issue -, Pages -Publisher
ELSEVIER
DOI: 10.1016/j.ijpharm.2021.120281
Keywords
Halloysite; Pyrazolo[3,4-d]pyrimidine derivatives; Nanocomposites; CDK inhibitors
Categories
Funding
- University of Palermo
- PON AIM: Attrazione e Mobilit`a Internazionale project [1808223]
- AIRC project [23725]
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The study reported a new example of nanocomposites based on HNTs/Si306 and HNTs/Si113 as anticancer agents and CDK inhibitors, and evaluated their inhibitory effects on different cancer cell lines as well as their impact on the cell cycle of HCT116 cells through experiments.
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.
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