Journal
ACS MEDICINAL CHEMISTRY LETTERS
Volume 9, Issue 2, Pages 149-154Publisher
AMER CHEMICAL SOC
DOI: 10.1021/acsmedchemlett.7b00504
Keywords
histone deacetylase inhibitors; belinostat; MCF-7 xenograft; boron-containing prodrugs; biocompatibility
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Funding
- NIH-NIMHD [2G12MD007595]
- Louisiana Cancer Research Consortium
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Despite promising therapeutic utilities for treatment of hematological malignancies, histone deacetylase inhibitor (HDACi) drugs have not proven as effective in the treatment of solid tumors. To expand the clinical indications of HDACi drugs, we developed novel boron-containing prodrugs of belinostat (2), one of which efficiently releases active 2 through a cascade of reactions in cell culture and demonstrates activities comparable to 2 against a panel of cancer cell lines. Importantly, prodrug 7 is more efficacious than belinostat in vivo, not only inhibiting the growth of tumor but also reducing tumor volumes in an MCF-7 xenograft tumor model owing to its superior biocompatibility, which suggests its clinical potential in the treatment of solid tumors.
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