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• W2578762335 abstract "The clinical validation of histone deacetylase inhibition as a cancer therapeutic modality has stimulated interest in the development of new generation of potent and tumor selective histone deacetylase inhibitors (HDACi). With the goal of selective delivery of the HDACi to melanoma cells, we incorporated the benzamide, a high affinity melanin-binding template, into the design of HDACi to generate a new series of compounds 10a-b and 11a-b which display high potency towards HDAC1 and HDAC6. However, these compounds have attenuated antiproliferative activities relative to the untargeted HDACi. An alternative strategy furnished compound 14, a prodrug bearing the benzamide template linked via a labile bond to a hydroxamate-based HDACi. This pro-drug compound showed promising antiproliferative activity and warrant further study." @default.
• W2578762335 created "2017-01-26" @default.
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• W2578762335 creator A5058348150 @default.
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• W2578762335 date "2017-02-01" @default.
• W2578762335 modified "2023-10-17" @default.
• W2578762335 title "Design, synthesis and evaluation of antiproliferative activity of melanoma-targeted histone deacetylase inhibitors" @default.
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• W2578762335 doi "https://doi.org/10.1016/j.bmcl.2017.01.044" @default.
• W2578762335 hasPubMedCentralId "https://www.ncbi.nlm.nih.gov/pmc/articles/5314971" @default.
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