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J Enzyme Inhib Med Chem. 2014 Aug;29(4):555-62. doi: 10.3109/14756366.2013.827675. Epub 2013 Sep 9.

Quinolone-based HDAC inhibitors.

Author information

1
Department of Medicinal Chemistry and.

Abstract

HDAC inhibitors emerged as promising drug candidates in combating wide variety of cancers. At present, two of the compounds SAHA and Romidepsin were approved by FDA for cutaneous T-cell lymphoma and many are in various clinical phases. A new quinolone cap structure was explored with hydroxamic acid as zinc-binding group (ZBG). The pan HDAC inhibitory and antiproliferative activities against three human cancer cell lines HCT-116 (colon), NCI-H460 (lung) and U251 (glioblastoma) of the compounds (4a-4w) were evaluated. Introduction of heterocyclic amines in CAP region increased the enzyme inhibitory and antiproliferative activities and few of the compounds tested are metabolically stable in both MLM and HLM.

KEYWORDS:

Anticancer activity; HDAC inhibition; quinolone

PMID:
25019596
DOI:
10.3109/14756366.2013.827675
[Indexed for MEDLINE]

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