Journal
BIOORGANIC & MEDICINAL CHEMISTRY
Volume 25, Issue 17, Pages 4579-4594Publisher
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmc.2017.06.032
Keywords
Methyltransferase inhibitor; Cycloalkyl substituted analogue; Natural product; Sinefungin
Funding
- National Health and Family Planning Commission of China [2012ZX09304-011, 2013ZX09401003-005, 2013ZX09507001, 2013ZX09507-002, 2014ZX09507002-001]
- National Natural Science Foundation of China [21302202]
- Shanghai Science and Technology Development Fund [15DZ2291600]
- Thousand Talents Program in China
Ask authors/readers for more resources
A series of cycloalkyl substituted analogues of the natural product sinefungin lacking the amino-acid moiety was designed and synthesized. Two stereoisomers (6-R and 6-S) were separated and their bioactivities examined against EHMT1/2. Of which, compound 14d showed an inhibitory activity against EHMT1/2 (88.9%, IC50 = 21.8 mu M for EHMT1 and 77.6%, IC50 = 39.6 mu M for EHMT2, respectively) similar to that of sinefungin (100.0%, IC50 = 28.4 mu M for EHMT1 and 79.5%, IC50 = 30.1 mu M for EHMT2, respectively). Further studies against other methyltransferases such as PRMT1 showed no activity except that 12d displayed about 20% inhibition. (C) 2017 Elsevier Ltd. All rights reserved.
Authors
I am an author on this paper
Click your name to claim this paper and add it to your profile.
Reviews
Recommended
No Data Available
Share Paper
