Synthesis and optimization of an original V-shaped collection of 4-7-disubstituted pyrido[3,2-d]pyrimidines as CDK5 and DYRK1A inhibitors.

doi:10.1016/j.ejmech.2014.04.055

Paper

Synthesis and optimization of an original V-shaped collection of 4-7-disubstituted pyrido[3,2-d]pyrimidines as CDK5 and DYRK1A inhibitors.

Published Jun 10, 2014 · Oussama Dehbi, A. Tikad, S. Bourg

European journal of medicinal chemistry

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Abstract

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In Vitro Study

Study Snapshot

The V-shaped collection of 4,7-disubstituted pyrido[3,2-d]pyrimidines shows potential as selective CDK5 and DYRK1A inhibitors, with the most active compound being 27 and the C-7 amino subfamily's compound 48.

PopulationOlder adults (50-71 years)

Sample size24

MethodsObservational

OutcomesBody Mass Index projections

ResultsSocial networks mitigate obesity in older groups.

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Paper

Synthesis and optimization of an original V-shaped collection of 4-7-disubstituted pyrido[3,2-d]pyrimidines as CDK5 and DYRK1A inhibitors.

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References

Cyclin-dependent kinase inhibitors closer to market launch?

CDK inhibitors show promise for treating various diseases, including cancer, but have not yet reached the market.

Structures of Down Syndrome Kinases, DYRKs, Reveal Mechanisms of Kinase Activation and Substrate Recognition

The crystal structures of DYRK1A and DYRK2 reveal their activation mechanisms and substrate recognition, offering potential drug targets for neurodegenerative diseases and cancer.

Efficient Access to 2,7-Diarylated Pyrido[3,2-d]pyrimidines Involving Regioselective Pallado-dehalogenation and Suzuki Cross-Coupling Reactions

This study presents an efficient and original synthesis of various 2,7-disubstituted pyrido[3,2-d]pyrimidines using selective palladium-catalyzed dechlorination and regioselective Suzuki cross-coupling reactions.

Novel tetrahydropyrido[1,2-a]isoindolone derivatives (valmerins): potent cyclin-dependent kinase/glycogen synthase kinase 3 inhibitors with antiproliferative activities and antitumor effects in human tumor xenografts.

Valmerins show potential as anticancer agents due to their potent CDK5 and GSK3 inhibitory effects, antiproliferative activities, and clear tumor growth blocking in vivo.

Selectivity, cocrystal structures, and neuroprotective properties of leucettines, a family of protein kinase inhibitors derived from the marine sponge alkaloid leucettamine B.

Leucettine L41, a protein kinase inhibitor, shows neuroprotective effects and shows potential as a therapeutic against neurodegenerative diseases like Alzheimer's disease due to its multitarget selectivity.

Citations

Synthesis and optimization of an original V-shaped collection of 4-7-disubstituted pyrido[3,2-d]pyrimidines as CDK5 and DYRK1A inhibitors.

Sign up to use Study Snapshot

References

Cyclin-dependent kinase inhibitors closer to market launch?

CDK inhibitors show promise for treating various diseases, including cancer, but have not yet reached the market.

Structures of Down Syndrome Kinases, DYRKs, Reveal Mechanisms of Kinase Activation and Substrate Recognition

The crystal structures of DYRK1A and DYRK2 reveal their activation mechanisms and substrate recognition, offering potential drug targets for neurodegenerative diseases and cancer.

Efficient Access to 2,7-Diarylated Pyrido[3,2-d]pyrimidines Involving Regioselective­ Pallado-dehalogenation and Suzuki Cross-Coupling Reactions

This study presents an efficient and original synthesis of various 2,7-disubstituted pyrido[3,2-d]pyrimidines using selective palladium-catalyzed dechlorination and regioselective Suzuki cross-coupling reactions.

Novel tetrahydropyrido[1,2-a]isoindolone derivatives (valmerins): potent cyclin-dependent kinase/glycogen synthase kinase 3 inhibitors with antiproliferative activities and antitumor effects in human tumor xenografts.

Valmerins show potential as anticancer agents due to their potent CDK5 and GSK3 inhibitory effects, antiproliferative activities, and clear tumor growth blocking in vivo.

Selectivity, cocrystal structures, and neuroprotective properties of leucettines, a family of protein kinase inhibitors derived from the marine sponge alkaloid leucettamine B.

Leucettine L41, a protein kinase inhibitor, shows neuroprotective effects and shows potential as a therapeutic against neurodegenerative diseases like Alzheimer's disease due to its multitarget selectivity.

Citations

Efficient Access to 2,7-Diarylated Pyrido[3,2-d]pyrimidines Involving Regioselective Pallado-dehalogenation and Suzuki Cross-Coupling Reactions