Zuomei Li

TL;DR: The exploration of the 14 A internal cavity adjacent to the enzyme catalytic site led to the design and synthesis of compound 4 with the unusual bis(aryl)-type pharmacophore, which resulted in optimization to potent, selective, nonhydroxamic acid HDAC inhibitors.

TL;DR: A series of sulfonamide hydroxamic acids and anilides synthesized and studied as histone deacetylase (HDAC) inhibitors selectively inhibit proliferation, cause cell cycle blocks, and induce apoptosis in human cancer cells but not in normal cells.

TL;DR: Novel, chiral 3,4-dihydroquinoxalin-2(1H)-one and piperazine-2,5-dione aryl hydroxamates showing selectivity (up to 40-fold) for human HDAC6 over other class I/IIa HDACs suggests new possibilities for use of chiral compounds in selective HDAC isoform inhibition.

TL;DR: The results suggest that sulfonamide anilides are novel HDAC inhibitors and may be useful as antiproliferative agents in cancer chemotherapy.