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

doi:10.1016/j.bmcl.2014.02.004

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 journal › Article › peer-review

4 Scopus citations

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 language	English (US)
Pages (from-to)	1506-1510
Number of pages	5
Journal	Bioorganic and Medicinal Chemistry Letters
Volume	24
Issue number	6
DOIs	https://doi.org/10.1016/j.bmcl.2014.02.004
State	Published - Mar 15 2014
Externally published	Yes

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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10.1016/j.bmcl.2014.02.004

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Certal, V., Halley, F., Virone-Oddos, A., Filoche-Rommé, B., Carry, J. C., Gruss-Leleu, F., Bertin, L., Guizani, H., Pilorge, F., Richepin, P., Karlsson, A., Charrier, V., Abecassis, P. Y., Vincent, L., Nicolas, J. P., Lengauer, C., Garcia-Echeverria, C., & Schio, L. (2014). 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. Bioorganic and Medicinal Chemistry Letters, 24(6), 1506-1510. https://doi.org/10.1016/j.bmcl.2014.02.004

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. / Certal, Victor; Halley, Frank; Virone-Oddos, Angela et al.

In: Bioorganic and Medicinal Chemistry Letters, Vol. 24, No. 6, 15.03.2014, p. 1506-1510.

Research output: Contribution to journal › Article › peer-review

Certal, V, Halley, F, Virone-Oddos, A, Filoche-Rommé, B, Carry, JC, Gruss-Leleu, F, Bertin, L, Guizani, H, Pilorge, F, Richepin, P, Karlsson, A, Charrier, V, Abecassis, PY, Vincent, L, Nicolas, JP, Lengauer, C, Garcia-Echeverria, C & Schio, L 2014, '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', Bioorganic and Medicinal Chemistry Letters, vol. 24, no. 6, pp. 1506-1510. https://doi.org/10.1016/j.bmcl.2014.02.004

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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.",

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AU - Halley, Frank

AU - Virone-Oddos, Angela

AU - Filoche-Rommé, Bruno

AU - Carry, Jean Christophe

AU - Gruss-Leleu, Florence

AU - Bertin, Luc

AU - Guizani, Houlfa

AU - Pilorge, Fabienne

AU - Richepin, Patrick

AU - Karlsson, Andreas

AU - Charrier, Véronique

AU - Abecassis, Pierre Yves

AU - Vincent, Loic

AU - Nicolas, Jean Paul

AU - Lengauer, Christoph

AU - Garcia-Echeverria, Carlos

AU - Schio, Laurent

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KW - PI3Kβ

KW - PTEN

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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

Abstract

Keywords

ASJC Scopus subject areas

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