0

Hydroxamates of Para-Aminobenzoic Acid as Selective Inhibitors of HDAC8

Umasankar Kulandaivelu, Laxmi Manasa Chilakamari, Surender Singh Jadav, Tadikonda Rama Rao, K N Jayaveera, Boyapati Shireesha, Alexander-Thomas Hauser, Johanna Senger, Martin Marek, Christophe Romier, Manfred Jung, etc.

Bioorg Chem. 2014 Dec;57:116-120.

PMID: 25462986

Abstract:

A series of hydroxamates (4a-4l) were prepared from p-aminobenzoic acid to inhibit HDAC8. The idea is to substitute rigid aromatic ring in place of less rigid piperazine ring of hydroxamates reported earlier by our group. It is expected to increase potency retaining the selectivity. Result obtained suggested that the modifications carried out retained the selectivity towards HDAC8 isoform and increasing the potency in very few cases. Increase in potency is also associated with variation in cap aryl region. Two compounds (4f &4l) were found to inhibit HDAC8 at concentrations (IC50) less than 20μM.

Chemicals Related in the Paper:

Catalog Number Product Name Structure CAS Number Price
AP150130-B Aminobenzoic acid Aminobenzoic acid 150-13-0 Price
qrcode