2. Academic Validation
  3. Discovery of a novel tricyclic 4H-thiazolo[5',4':4,5]pyrano[2,3-c]pyridine-2-amino scaffold and its application in a PI3Kα inhibitor with high PI3K isoform selectivity and potent cellular activity

Discovery of a novel tricyclic 4H-thiazolo[5',4':4,5]pyrano[2,3-c]pyridine-2-amino scaffold and its application in a PI3Kα inhibitor with high PI3K isoform selectivity and potent cellular activity

  • Bioorg Med Chem Lett. 2015 Sep 1;25(17):3582-4. doi: 10.1016/j.bmcl.2015.06.077.
Marc Gerspacher 1,  Robin A Fairhurst 2,  Robert Mah 2,  Esther Roehn-Carnemolla 2,  Pascal Furet 2,  Christine Fritsch 2,  Daniel A Guthy 2
Affiliations

Affiliations

  • 1 Novartis Institutes for BioMedical Research, Novartis Pharma AG, WKL-136.4.84, CH-4002 Basel, Switzerland. Electronic address: marc.gerspacher@novartis.com.
  • 2 Novartis Institutes for BioMedical Research, Novartis Pharma AG, WKL-136.4.84, CH-4002 Basel, Switzerland.
PMID: 26164189 DOI: 10.1016/j.bmcl.2015.06.077
Abstract

A novel, previously undescribed 4H-thiazolo[5',4':4,5]pyrano[2,3-c]pyridine tricyclic scaffold has been discovered. The application of this novel chemotype leading to a potent and selective prototype PI3Kα Inhibitor with favorable physicochemical and PK-properties is described.

Keywords

4H-Thiazolo[5′,4′:4,5]pyrano[2,3-c]pyridine-2-amino derivative; Oncology; Phosphatidylinositol-3-kinase (PI3K); Selective PI3Kα Inhibitor.

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