Purine analogs as phosphatidylinositol 4-kinase III? inhibitors

Result code in IS VaVaI

<a href="https://www.isvavai.cz/riv?ss=detail&h=RIV%2F60461373%3A22330%2F16%3A43901711" target="_blank" >RIV/60461373:22330/16:43901711 - isvavai.cz</a>

Result on the web

<a href="http://dx.doi.org/10.1016/j.bmcl.2016.04.002" target="_blank" >http://dx.doi.org/10.1016/j.bmcl.2016.04.002</a>

DOI - Digital Object Identifier

<a href="http://dx.doi.org/10.1016/j.bmcl.2016.04.002" target="_blank" >10.1016/j.bmcl.2016.04.002</a>

Result language

angličtina

Original language name

Purine analogs as phosphatidylinositol 4-kinase III? inhibitors

Original language description

We report on an extensive structure-activity relationship study of novel PI4K III beta inhibitors. The purine derivative of the potent screening hit T-00127-HEV1 has served as a suitable starting point for a thorough investigation of positions 8 and 2. While position 8 of the purine scaffold can only bear a small substituent to maintain the inhibitory activity, position 2 is opened for extensive modification and can accommodate even substituted phenyl rings without the loss of PI4K III beta inhibitory activity. These empirical observations nicely correlate with the results of our docking study, which suggests that position 2 directs towards solution and can provide the necessary space for the interaction with remote residues of the enzyme, whereas the cavity around position 8 is strictly limited. The obtained compounds have also been subjected to antiviral screening against a panel of (+) ssRNA viruses. (C) 2016 Published by Elsevier Ltd.

Czech name

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Czech description

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Type

J_x - Unclassified - Peer-reviewed scientific article (Jimp, Jsc and Jost)

CEP classification

CC - Organic chemistry

OECD FORD branch

—

Project

—

Continuities

I - Institucionalni podpora na dlouhodoby koncepcni rozvoj vyzkumne organizace

Publication year

2016

Confidentiality

S - Úplné a pravdivé údaje o projektu nepodléhají ochraně podle zvláštních právních předpisů

Name of the periodical

Bioorganic &amp; Medicinal Chemistry Letters

ISSN

0960-894X

e-ISSN

—

Volume of the periodical

26

Issue of the periodical within the volume

11

Country of publishing house

GB - UNITED KINGDOM

Number of pages

7

Pages from-to

2706-2712

UT code for WoS article

000374988600028

EID of the result in the Scopus database

2-s2.0-84963686126