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New thiouracil derivatives as histone deacetylase inhibitors and apoptosis inducers: design, synthesis and anticancer evaluation. | LitMetric

AI Article Synopsis

Article Abstract

Histone deacetylase (HDAC) inhibitors have good contributions in cancer management. To introduce new active HDAC inhibitors. Design and synthesis of 16 thiouracil derivatives with deep biological and computational investigation. Compounds , , , , and showed the highest antiproliferative effects against MCF7, HepG2 and HCT116 cell lines. Compound exhibited the highest activities against HDAC1 and HDAC4. Compound arrested the cell cycle of HCT116 cells at G0-G1 with significant apoptotic effect. In addition, treatment with compound was associated with a significant increase in the levels of caspase-3 and caspase-8. The docking studies gave good insight about the binding patterns of the synthesized compounds against HDAC1. Compound has a promising anticancer activity targeting HDAC.

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Source
http://dx.doi.org/10.4155/fmc-2023-0106DOI Listing

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