dc.contributor.author |
Sundriyal, Sandeep |
|
dc.date.accessioned |
2024-01-17T04:58:03Z |
|
dc.date.available |
2024-01-17T04:58:03Z |
|
dc.date.issued |
2014-08 |
|
dc.identifier.uri |
https://pubs.rsc.org/en/content/articlehtml/2014/md/c4md00274a |
|
dc.identifier.uri |
http://dspace.bits-pilani.ac.in:8080/jspui/xmlui/handle/123456789/13854 |
|
dc.description.abstract |
G9a is a histone lysine methyltransferase (HKMT) involved in epigenetic regulation via the installation of histone methylation marks. 6,7-Dimethoxyquinazoline analogues, such as BIX-01294, are established as potent, substrate competitive inhibitors of G9a. With an objective to identify novel chemotypes for substrate competitive inhibitors of G9a, we have designed and synthesised a range of heterocyclic scaffolds, and investigated their ability to inhibit G9a. These studies have led to improved understanding of the key pharmacophoric features of BIX-01294 and the identification of a new core quinoline inhibitory scaffold, which retains excellent potency and high selectivity. Molecular docking was carried out to explain the observed in vitro data. |
en_US |
dc.language.iso |
en |
en_US |
dc.publisher |
RSC |
en_US |
dc.subject |
Pharmacy |
en_US |
dc.subject |
7-dimethoxyquinoline |
en_US |
dc.subject |
Histone lysine methyltransferase (HKMT) |
en_US |
dc.title |
Identification of 2,4-diamino-6,7-dimethoxyquinoline derivatives as G9a inhibitor |
en_US |
dc.type |
Article |
en_US |