Discovery of Cinnoline Derivatives as Potent PI3K Inhibitors with Antiproliferative Activity.

doi:10.1016/j.bmcl.2021.128271

Paper

Discovery of Cinnoline Derivatives as Potent PI3K Inhibitors with Antiproliferative Activity.

Published Jul 17, 2021 · Chengze Tian, Chen-Yui Yang, Tianze Wu

Bioorganic & medicinal chemistry letters

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12

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Abstract

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In Vitro Study

Study Snapshot

Cinnoline derivatives show potent PI3K inhibitory activity with antiproliferative activity against human tumor cell lines.

PopulationOlder adults (50-71 years)

Sample size24

MethodsObservational

OutcomesBody Mass Index projections

ResultsSocial networks mitigate obesity in older groups.

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Paper

Discovery of Cinnoline Derivatives as Potent PI3K Inhibitors with Antiproliferative Activity.

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References

Citations

An Insight into the Synthetic Strategies and Pharmacological Effects of Cinnoline Derivatives

Cinnoline derivatives show potential as a powerful lead for producing a wide range of therapeutic effects, including antitubercular, antibacterial, anticancer, and antimolluscidal effects.

Integration of Multicomplex‐Based Pharmacophore Modeling and Molecular Docking in Machine Learning‐Based Virtual Screening: Toward the Discovery of Novel PI3K Inhibitors

The study developed a virtual screening strategy using nave Bayesian classification models, combining molecular docking and pharmacophore modeling, to identify potential novel PI3K inhibitors.

Practical Three-Component Regioselective Synthesis of Drug-Like 3-Aryl(or heteroaryl)-5,6-dihydrobenzo[h]cinnolines as Potential Non-Covalent Multi-Targeting Inhibitors To Combat Neurodegenerative Diseases.

This study presents a practical three-component regioselective synthesis of 3-aryl(or heteroaryl)-5,6-dihydrobenzo[h]cinnolines as potential non-covalent multi-targeting inhibitors for neurodegenerative diseases.

Two New Alkaloids and a New Butenolide Derivative from the Beibu Gulf Sponge-Derived Fungus Penicillium sp. SCSIO 41413

Two new alkaloids and a new butenolide derivative were isolated from the Beibu Gulf sponge-derived fungus Penicillium sp. SCSIO 41413, with potential inhibitory effects against PI3K and NF-B activation.

Molecular target interactions of quinoline derivatives as anticancer agents: A review

Quinoline derivatives show anticancer properties by acting on various molecular targets, including topoisomerase, tyrosine kinases, Hsp90, HDACs, cell cycle arrest, apoptosis, and tubulin polymerization.

Targeting the PI3K/AKT/mTOR Signaling Pathway in the Treatment of Human Diseases: Current Status, Trends, and Solutions.

Recent advances in inhibitors targeting the PI3K/AKT/mTOR pathway show promise for treating various human diseases, but overcoming toxicity and drug resistance challenges remain.

A pyridinesulfonamide derivative FD268 suppresses cell proliferation and induces apoptosis via inhibiting PI3K pathway in acute myeloid leukemia

FD268 effectively inhibits acute myeloid leukemia cell survival by inducing apoptosis through inhibition of the PI3K/Akt/mTOR signaling pathway.