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Discovery of cinnoline derivatives as potent PI3K inhibitors with antiproliferative activity.
- Source :
-
Bioorganic & medicinal chemistry letters [Bioorg Med Chem Lett] 2021 Sep 15; Vol. 48, pp. 128271. Date of Electronic Publication: 2021 Jul 17. - Publication Year :
- 2021
-
Abstract
- Cinnoline is a potential pharmacophore which has rarely been reported for uses as PI3K inhibitors. In this study, a series of cinnoline derivatives were developed as PI3K inhibitors and evaluated for enzymatic and cellular activities. Most compounds displayed nanomolar inhibitory activities against PI3Ks, among which 25 displayed high LLE and micromolar inhibitory potency against three human tumor cell lines (IC <subscript>50</subscript>  = 0.264 μM, 2.04 μM, 1.14 μM).<br /> (Copyright © 2021 Elsevier Ltd. All rights reserved.)
- Subjects :
- Antineoplastic Agents chemical synthesis
Antineoplastic Agents chemistry
Cell Line, Tumor
Cell Proliferation drug effects
Dose-Response Relationship, Drug
Drug Screening Assays, Antitumor
Heterocyclic Compounds, 2-Ring chemical synthesis
Heterocyclic Compounds, 2-Ring chemistry
Humans
Molecular Structure
Phosphoinositide-3 Kinase Inhibitors chemical synthesis
Phosphoinositide-3 Kinase Inhibitors chemistry
Structure-Activity Relationship
Antineoplastic Agents pharmacology
Drug Discovery
Heterocyclic Compounds, 2-Ring pharmacology
Phosphatidylinositol 3-Kinases metabolism
Phosphoinositide-3 Kinase Inhibitors pharmacology
Subjects
Details
- Language :
- English
- ISSN :
- 1464-3405
- Volume :
- 48
- Database :
- MEDLINE
- Journal :
- Bioorganic & medicinal chemistry letters
- Publication Type :
- Academic Journal
- Accession number :
- 34284105
- Full Text :
- https://doi.org/10.1016/j.bmcl.2021.128271