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5-membered cyclic hydroxamic acids as HDAC inhibitors.

Journal of enzyme inhibition and medicinal chemistry (2014-06-19)
Ilze Mutule, Diana Borovika, Elina Rozenberga, Nadezhda Romanchikova, Raivis Zalubovskis, Irina Shestakova, Peteris Trapencieris
ABSTRACT

The new histone deacylases inhibitors (HDACi) were synthesized in the class of 5-membered cyclic hydroxamic acids (5-CHA), showing medium size CHA as a new Zn-binding group. New reaction sequence was proposed for the synthesis of 5-membered alkylidene-cyclic-hydroxamic acids starting from butyrolactone. Compound 10c showed low µM activity on HeLa cell extracts. From these results, cyclic hydroxamic acids will be further investigated to find more potent compounds.

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Mercury, electronic grade, 99.9999% trace metals basis
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Mercury, ≥99.99% trace metals basis
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Mercury, ACS reagent, 99.9995% trace metals basis