Abstract:
:The novel hydroxamates containing purine scaffold were designed, synthesized and screened for their biological activities as histone deacetylase (HDAC) inhibitors. Some of them exhibited excellent acti-HDACs activities and antiproliferative activities, the most promising compound was 7m'. Western blot analysis indicated the compounds 7f', 7l', 7m', 7o' could increase histone H3 acetylation levels in HCT116 and K562 cell lines, and 7m' increased the level of acetyl histone H3 in a dose-dependent manner, which is similar to the behavior of suberoylanilide hydroxamic acid (SAHA). Molecular docking study revealed that the conformation of 7m' in the active site of HDAC2 was similar to positive drug SAHA, which were oriented with the hydroxamic acid towards the catalytic center and formed metal binding with zinc ion.
journal_name
Chem Pharm Bull (Tokyo)journal_title
Chemical & pharmaceutical bulletinauthors
Xu Z,Yang Y,Mai X,Liu B,Xiong Y,Feng L,Liao Y,Zhang Y,Wang H,Ouyang L,Liu Sdoi
10.1248/cpb.c17-00997subject
Has Abstractpub_date
2018-01-01 00:00:00pages
439-451issue
4eissn
0009-2363issn
1347-5223journal_volume
66pub_type
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