Molecular explorations of substituted 2-(4-phenylquinolin-2-yl) phenols as phosphoinositide 3-kinase inhibitors and anticancer agents

Purpose Substituted 2-(4-phenylquinolin-2-yl) phenols (PQPDs) emerged as the inhibitors of phosphoinositide 3-kinase (PI3K) and anticancer agents. Method PI3K inhibition was assessed by competitive ELISA. Anticancer activity was evaluated against breast cancer (MCF-7), skin cancer (G-361), and colon...

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Bibliographic Details
Published in:Cancer chemotherapy and pharmacology 2017-02, Vol.79 (2), p.389-397
Main Authors: Alagumuthu, Manikandan, Arumugam, Sivakumar
Format: Article
Language:English
Subjects:
Antineoplastic Agents - pharmacology
Cancer Research
Cell Line, Tumor
Humans
Medicine
Medicine & Public Health
Molecular Docking Simulation
Oncology
Original Article
Pharmacology/Toxicology
Phenols - chemistry
Phenols - pharmacology
Phosphatidylinositol 3-Kinases - antagonists & inhibitors
Structure-Activity Relationship
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Summary:Purpose Substituted 2-(4-phenylquinolin-2-yl) phenols (PQPDs) emerged as the inhibitors of phosphoinositide 3-kinase (PI3K) and anticancer agents. Method PI3K inhibition was assessed by competitive ELISA. Anticancer activity was evaluated against breast cancer (MCF-7), skin cancer (G-361), and colon cancer (HCT 116) cell lines. Results In PI3 Kinase assay, PQPDs 4c, 4d, and 4k were inactive with IC 50  >5 µM. IC 50 for 4a, 4b, 4f–h, and 4j was ≥0.05 µM. Rest PQPDs IC 50 was
ISSN:0344-5704
1432-0843
DOI:10.1007/s00280-016-3227-z