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

Brahmam Pujala, Anil K. Agarwal, Sandip Middya, Monali Banerjee, Arjun Surya, Anjan K. Nayak, Ashu Gupta, Sweta Khare, Rambabu Guguloth, Nitin A. Randive, Bharat U. Shinde, Anamika Thakur, Dhananjay I. Patel, Mohd Raja, Michael J. Green, Jennifer Alfaro, Patricio Avila, Felipe Pérez de Arce, Ramona G. Almirez, Stacy KannoSebastián Bernales, David T. Hung, Sarvajit Chakravarty, Emma McCullagh, Kevin P. Quinn, Roopa Rai, Son M. Pham

Resultado de la investigación: Contribución a una revistaArtículorevisión exhaustiva

11 Citas (Scopus)

Resumen

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 BTK and PI3Kδ as well as acceptable PK properties that could be useful in the development of treatments against B-cell related diseases.

Idioma originalInglés
Páginas (desde-hasta)1161-1166
Número de páginas6
PublicaciónACS Medicinal Chemistry Letters
Volumen7
N.º12
DOI
EstadoPublicada - 8 dic 2016
Publicado de forma externa

Áreas temáticas de ASJC Scopus

  • Bioquímica
  • Descubrimiento de medicamentos
  • Química orgánica

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