Focused Sets: SAM/SAH Mimetics

The enzyme co-factor SAM/SAH is thought to be the second most common after ATP, exploited by protein methyltransferases for the transfer of a methyl group.  A number of these enzymes have come to the fore as drug targets through strong interest in the field of epigenetics. This includes histone methyltransferases that have been implicated in various human diseases including liver cancer, leukemia, prostate cancer, lung cancer, drug addiction, mental retardation and maintenance of HIV.  However, there is wide-ranging interest in SAM/SAH-dependent enzymes beyond epigenetics, including in the fields of antibacterials, antivirals, antiparasitics, crop protection and industrial chemical processing. Compounds targeting the SAM/SAH site of these enzymes offer great potential, yet very few such molecules are readily available for the inclusion in screening collections. 

A modular approach has been used by ASINEX to synthesize a library of SAM-SAH mimetics.  We have developed a number of stereo- and enantioselective methods for the synthesis of nucleoside-like core intermediates (e. g.  mimics of adenosine). These unique intermediates have been extensively decorated by various long chain amines, acids and amino acids to yield an array of >3000  final compounds .

Download SAM/SAH Mimetics SDF file (2961 compounds, version Mar.2016).

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