Preparation and optimization of new 4-(2-(indolin-1-yl)-2-oxoethyl)-2- morpholinothiazole-5-carboxylic acid and amide derivatives as potent and selective PI3Kβ inhibitors

Victor Certal, Frank Halley, Angela Virone-Oddos, Bruno Filoche-Rommé, Jean Christophe Carry, Florence Gruss-Leleu, Luc Bertin, Houlfa Guizani, Fabienne Pilorge, Patrick Richepin, Andreas Karlsson, Véronique Charrier, Pierre Yves Abecassis, Loic Vincent, Jean Paul Nicolas, Christoph Lengauer, Carlos Garcia-Echeverria, Laurent Schio

Research output: Contribution to journalArticlepeer-review

Abstract

In our continuous efforts to identify and develop novel targeted cancer treatments, a new morpholino-thiazole scaffold active against PI3Kβ has been identified. This Letter reports the optimization of this compound class to develop PI3Kβ isoform-selective inhibitors with suitable pharmacological properties.

Original languageEnglish (US)
Pages (from-to)1506-1510
Number of pages5
JournalBioorganic and Medicinal Chemistry Letters
Volume24
Issue number6
DOIs
StatePublished - Mar 15 2014
Externally publishedYes

Keywords

  • pAKT
  • PI3Kβ
  • PTEN
  • Thiazole

ASJC Scopus subject areas

  • Biochemistry
  • Clinical Biochemistry
  • Molecular Biology
  • Molecular Medicine
  • Organic Chemistry
  • Drug Discovery
  • Pharmaceutical Science

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