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Issue 11, 2015
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Discovery of fluoroquinolone derivatives as potent, selective inhibitors of PI3Kγ

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Abstract

Phosphoinositide 3-kinase (PI3K) is an attractive target to potentially treat a range of disease states as illustrated by more than 15 inhibitors now in clinical trials. We disclose herein the discovery of a new class of fluoroquinolone derivatives having improved potency toward PI3K. The activity of compound A3 as an inhibitor of PI3K was further investigated in human tumor cells. Notably, compound A3 with potent inhibitory activity was less toxic. By computational docking studies, it was predicted that, like CAL-101, a known small inhibitor of PI3K, compound A3 was tightly embedded into the ATP binding pocket with H bonds and π–cation interactions.

Graphical abstract: Discovery of fluoroquinolone derivatives as potent, selective inhibitors of PI3Kγ

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Submitted
27 Aug 2015
Accepted
28 Sep 2015
First published
29 Sep 2015

Med. Chem. Commun., 2015,6, 2029-2035
Article type
Concise Article

Discovery of fluoroquinolone derivatives as potent, selective inhibitors of PI3Kγ

S. Sha, H. Han, F. Gao, T. Liu, Z. Li, C. Xu, W. Zhong and H. Zhu, Med. Chem. Commun., 2015, 6, 2029
DOI: 10.1039/C5MD00364D

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