Title

Trithiocarbonates as a novel class of HDAC inhibitors: SAR studies, isoenzyme selectivity, and pharmacological profiles.

Journal

Journal of medicinal chemistry

Volume

51

Issue

None

Pages

3985-4001

Date

2008-07-10

Authors

Beckers T | Burkhardt C | Ciossek T | Dehmel F | Fettis K | Julius H | Maier T | Stengel T | Weinbrenner S | Wieland H

Highly potent, substrate competitive HDAC6 selective inhibitors were identified (12ac:IC 50 = 65 nM and K i = 110 nM). Trithiocarbonate analogues with an aminoquinoline-substituted pyridinyl-thienoacetyl cap demonstrate a cytotoxicity profile and potency comparable to that of suberoylanilide hydroxamic acid (SAHA) as an approved cancer drug.

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