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Cover Feature: Development of Novel Inhibitors for Histone Methyltransferase SET7/9 based on Cyproheptadine (ChemMedChem 15/2018)
Author(s) -
Hirano Tomoya,
Fujiwara Takashi,
Niwa Hideaki,
Hirano Michitake,
Ohira Kasumi,
Okazaki Yusuke,
Sato Shin,
Umehara Takashi,
Maemoto Yuki,
Ito Akihiro,
Yoshida Minoru,
Kagechika Hiroyuki
Publication year - 2018
Publication title -
chemmedchem
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.817
H-Index - 100
eISSN - 1860-7187
pISSN - 1860-7179
DOI - 10.1002/cmdc.201800495
Subject(s) - cyproheptadine , chemistry , antagonist , acetamide , pharmacology , methyltransferase , receptor , serotonin , stereochemistry , biochemistry , methylation , medicine , organic chemistry , gene
The Cover Feature shows the inhibitor of histone methyltransferase SET7/9 based on a novel scaffold, cyproheptadine, which is used clinically as a serotonin receptor antagonist or histamine receptor antagonist. Among its derivatives, a compound bearing a 2‐hydroxy group showed the most potent activity, while a 3‐hydroxy group or other hydrophilic functional groups such as acetamide decreased the activity. Structural analysis clarified a rationale for the improved potency only by tightly restricted location and type of hydrophilic group. These results are helpful for further structure‐based development of SET7/9 inhibitors. More information can be found in the Full Paper by Tomoya Hirano et al. on page 1530 in Issue 15, 2018 (DOI: 10.1002/cmdc.201800233).