Pham-The Hai

TL;DR: It was found that the N-hydroxypropenamides (10a-d) were the most potent, both in term of HDAC inhibition and cytotoxicity, which was found to have high quantitative correlation with experimental results.

TL;DR: Biological evaluation showed that these benzamides potently inhibited HDAC2 with IC50 values in sub-micromolar range, and docking experiments indicated that the compounds tightly bound toHDAC2 at the active binding site with binding affinities much higher than that of SAHA.

TL;DR: Detailed investigation on the estimation of absorption, distribution, metabolism, excretion, and toxicity (ADMET) suggested that compounds 4g, 6c, and 6g, while showing potent HDAC2 inhibitory activity and cytotoxicity, also potentially displayed ADMET characteristics desirable to be expected as promising anticancer drug candidates.

TL;DR: Biological evaluation showed that these hydroxamic acids potently inhibited HDAC2 with IC50 values in submicromolar range and up to tenfold (compound 3j) better than that of SAHA (also known as suberoylanilidehydroxamic acid).

TL;DR: Additional cytotoxic evaluation of the compounds against three human cancer cell lines revealed that five compounds, including 5g, exhibited strong cytotoxicity, and 5g was the most potent one with IC 50 values as low as 0.65 μM, even more potent than adriamycin, a positive control.