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Beilstein J. Org. Chem. 2022, 18, 837–844, doi:10.3762/bjoc.18.84
Graphical Abstract
Figure 1: FDA-approved HDAC inhibitors with a hydroxamic acid moiety.
Scheme 1: Synthesis of compounds 3–18. Reagents and conditions: (a) ethyl 2-bromoethanoate, TBAB, TEA, 50–60 ...
Scheme 2: Synthesis of compounds 20–31. Reagents and conditions: (a) ethyl 2-bromoethanoate (for 22) (or ethy...
Figure 2: The conformational and tautomeric forms of hydroxamic acids according to [36].
Figure 3: Fragment of the 1H NMR spectrum in DMSO-d6 of compound 12.
Beilstein J. Org. Chem. 2013, 9, 81–88, doi:10.3762/bjoc.9.11
Figure 1: FDA approved HDAC inhibitors for the treatment of CTCL.
Scheme 1: SAR of psammaplin A against zinc-dependant HDACs. Adapted from Baud et al. [20].
Scheme 2: Synthesis of 7–9. Conditions: (i) HCl·H2NOMe, pyridine, rt, 12 h; (ii) EDC, NHS, dioxane, rt, 3 h; ...
Scheme 3: Top: Generation of the fluorescent adduct 11 after reaction of probe 10 with thiols. Bottom left: F...
Figure 2: rHDAC1 was incubated with a predetermined IC50 concentration of 7 (left) and 9 (right) for 1–60 min...