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. 2009 May 15;19(10):2747-51.
doi: 10.1016/j.bmcl.2009.03.113. Epub 2009 Mar 28.

SAR around (l)-S-adenosyl-l-homocysteine, an inhibitor of human DNA methyltransferase (DNMT) enzymes

Oscar M Saavedra  1 , Ljubomir Isakovic, David B Llewellyn, Lijie Zhan, Naomy Bernstein, Stephen Claridge, Franck Raeppel, Arkadii Vaisburg, Nadine Elowe, Andrea J Petschner, Jubrail Rahil, Norman Beaulieu, A Robert MacLeod, Daniel Delorme, Jeffrey M Besterman, Amal Wahhab
Affiliations

SAR around (l)-S-adenosyl-l-homocysteine, an inhibitor of human DNA methyltransferase (DNMT) enzymes

Oscar M Saavedra et al. Bioorg Med Chem Lett. .

Abstract

The inhibitory activity of base-modified SAH analogues and the specificity of inhibiting human DNMT1 and DNMT3b2 enzymes was explored. The 6-amino group was essential while the 7-N of the adenine ring of SAH could be replaced by CH- without loss of activity against both enzymes. The introduction of small groups at the 2-position of the adenine moiety favors DNMT1 over DNMT3b2 inhibition whereas alkylation of the N(6)-amino moiety favors the inhibition of DNMT3b2 enzyme.

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