N(1)-Hydroxy-N(8)-ferrocenyloctanediamide, JAHA (7), an organometallic analogue of SAHA containing a ferrocenyl group as a phenyl bioisostere, displays nanomolar inhibition of class I HDACs, excellent selectivity over class IIa HDACs, and anticancer action in intact cells (IC(50) = 2.4 μM, MCF7
A cyclodextrin-capped histone deacetylase inhibitor.
Amin et al.
Biochemical Medicine, 23(11), 3346-3348 (2013)
Synthesis of 1-Aminocyclopropyl-Pentanoic and-Heptanoic Acid Derivatives.
Gensini et al.
Letters in Organic Chemistry, 5(5), 328-331 (2008)
Analytical and bioanalytical chemistry, 394(6), 1679-1685 (2009-06-02)
A fluorescent assay for the evaluation of inhibitors of fatty acid amide hydrolase (FAAH) is described. Microsomes from rat brain served as enzyme source. N-(2-Hydroxyethyl)-4-pyren-1-ylbutanamide was designed and synthesized as novel fluorogenic substrate. For substrate solubilization, Triton X-100 was employed.
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