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A series of pyrido-pyrimidin-4-ones, incorporating purine/pyrimidine scaffolds, were prepared by a succession of standard reactions and tested for the inhibition of 4 isoforms of the phosphatidylinositol 3-kinase (PI3K) class I, that is, the α, β, δ and γ PI3Ks. Compounds with activity, from the nanomolar to the micromolar, against isoform PI3Kδ were detected, and have been assayed in vivo with the human B cells proliferation assay, stimulated by anti-IgM or IL-4, showing remarkable activity. The patent claims a very promising new class of PI3Kδ inhibitors with selectivity for the δ-class enzymes, involved in a variety of diseases, such as, but not limited to, cancer, autoimmune disease and allergy. The chemotype claimed in the patent is new, and a large chemical diversity was generated by standard chemical processes. The biological activity and selectivity of these enzyme inhibitors seem to be very good.
Università degli Studi di Firenze, Laboratorio di Chimica Bioinorganica, Rm. 188, Via della Lastruccia 3, I-50019 Sesto Fiorentino (Firenze), Italy email@example.com.
This article was published in the following journal.
Name: Expert opinion on therapeutic patents
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