Journal article
Discovery of HDAC6-Selective Inhibitor NN-390 with in Vitro Efficacy in Group 3 Medulloblastoma
Abstract
Histone deacetylase 6 (HDAC6) has been targeted in clinical studies for anticancer effects due to its role in oncogenic transformation and metastasis. Through a second-generation structure-activity relationship (SAR) study, the design, and biological evaluation of the selective HDAC6 inhibitor NN-390 is reported. With nanomolar HDAC6 potency, >200-550-fold selectivity for HDAC6 in analogous HDAC isoform functional assays, potent intracellular …
Authors
Nawar N; Bukhari S; Adile AA; Suk Y; Manaswiyoungkul P; Toutah K; Olaoye OO; Raouf YS; Sedighi A; Garcha HK
Journal
Journal of Medicinal Chemistry, Vol. 65, No. 4, pp. 3193–3217
Publisher
American Chemical Society (ACS)
Publication Date
February 24, 2022
DOI
10.1021/acs.jmedchem.1c01585
ISSN
0022-2623