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Discovery of Pyrazolopyrimidine Derivatives as Novel Dual Inhibitors of BTK and PI3K?.

ABSTRACT: The aberrant activation of B-cells has been implicated in several types of cancers and hematological disorders. BTK and PI3K? are kinases responsible for B-cell signal transduction, and inhibitors of these enzymes have demonstrated clinical benefit in certain types of lymphoma. Simultaneous inhibition of these pathways could result in more robust responses or overcome resistance as observed in single agent use. We report a series of novel compounds that have low nanomolar potency against both BTK and PI3K? as well as acceptable PK properties that could be useful in the development of treatments against B-cell related diseases.

SUBMITTER: Pujala B

PROVIDER: S-EPMC5150666 | biostudies-literature | 2016 Dec

REPOSITORIES: biostudies-literature

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Discovery of Pyrazolopyrimidine Derivatives as Novel Dual Inhibitors of BTK and PI3Kδ.

Pujala Brahmam B Agarwal Anil K AK Middya Sandip S Banerjee Monali M Surya Arjun A Nayak Anjan K AK Gupta Ashu A Khare Sweta S Guguloth Rambabu R Randive Nitin A NA Shinde Bharat U BU Thakur Anamika A Patel Dhananjay I DI Raja Mohd M Green Michael J MJ Alfaro Jennifer J Avila Patricio P Pérez de Arce Felipe F Almirez Ramona G RG Kanno Stacy S Bernales Sebastián S Hung David T DT Chakravarty Sarvajit S McCullagh Emma E Quinn Kevin P KP Rai Roopa R Pham Son M SM

ACS medicinal chemistry letters 20161028 12

The aberrant activation of B-cells has been implicated in several types of cancers and hematological disorders. BTK and PI3Kδ are kinases responsible for B-cell signal transduction, and inhibitors of these enzymes have demonstrated clinical benefit in certain types of lymphoma. Simultaneous inhibition of these pathways could result in more robust responses or overcome resistance as observed in single agent use. We report a series of novel compounds that have low nanomolar potency against both BT ...[more]

PMID: 27994757

Dataset Information

Discovery of Pyrazolopyrimidine Derivatives as Novel Dual Inhibitors of BTK and PI3K?.

Publications

Discovery of Pyrazolopyrimidine Derivatives as Novel Dual Inhibitors of BTK and PI3Kδ.

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