Identification of Clinical Candidate M2698, a Dual p70S6K and Akt Inhibitor, for Treatment of PAM Pathway-Altered Cancers.


Journal

Journal of medicinal chemistry
ISSN: 1520-4804
Titre abrégé: J Med Chem
Pays: United States
ID NLM: 9716531

Informations de publication

Date de publication:
14 10 2021
Historique:
pubmed: 2 10 2021
medline: 16 2 2022
entrez: 1 10 2021
Statut: ppublish

Résumé

Herein, we report the discovery of a novel class of quinazoline carboxamides as dual p70S6k/Akt inhibitors for the treatment of tumors driven by alterations to the PI3K/Akt/mTOR (PAM) pathway. Through the screening of in-house proprietary kinase library, 4-benzylamino-quinazoline-8-carboxylic acid amide

Identifiants

pubmed: 34596404
doi: 10.1021/acs.jmedchem.1c01087
doi:

Substances chimiques

MTOR protein, human EC 2.7.1.1
Phosphatidylinositol 3-Kinases EC 2.7.1.-
Protein Kinase Inhibitors 0
Proto-Oncogene Proteins c-akt EC 2.7.11.1
Ribosomal Protein S6 Kinases, 70-kDa EC 2.7.11.1
TOR Serine-Threonine Kinases EC 2.7.11.1
M2698 0

Types de publication

Journal Article

Langues

eng

Sous-ensembles de citation

IM

Pagination

14603-14619

Auteurs

Lizbeth DeSelm (L)

Discovery Technologies, Medicinal Chemistry, EMD Serono Research & Development Institute, Inc., Billerica, Massachusetts 01821, United States.

Bayard Huck (B)

Discovery Technologies, Medicinal Chemistry, EMD Serono Research & Development Institute, Inc., Billerica, Massachusetts 01821, United States.

Ruoxi Lan (R)

Discovery Technologies, Medicinal Chemistry, EMD Serono Research & Development Institute, Inc., Billerica, Massachusetts 01821, United States.

Constantin Neagu (C)

Discovery Technologies, Medicinal Chemistry, EMD Serono Research & Development Institute, Inc., Billerica, Massachusetts 01821, United States.

Justin Potnick (J)

Discovery Technologies, Medicinal Chemistry, EMD Serono Research & Development Institute, Inc., Billerica, Massachusetts 01821, United States.

Yufang Xiao (Y)

Discovery Technologies, Medicinal Chemistry, EMD Serono Research & Development Institute, Inc., Billerica, Massachusetts 01821, United States.

Xiaoling Chen (X)

Discovery Technologies, Medicinal Chemistry, EMD Serono Research & Development Institute, Inc., Billerica, Massachusetts 01821, United States.

Reinaldo Jones (R)

Discovery Technologies, Medicinal Chemistry, EMD Serono Research & Development Institute, Inc., Billerica, Massachusetts 01821, United States.

Thomas E Richardson (TE)

SCYNEXIS, Inc., 1 Evertrust Plaza, 13th Floor, Jersey City, New Jersey 07302, United States.

Brian H Heasley (BH)

SCYNEXIS, Inc., 1 Evertrust Plaza, 13th Floor, Jersey City, New Jersey 07302, United States.

Thomas Haxell (T)

SCYNEXIS, Inc., 1 Evertrust Plaza, 13th Floor, Jersey City, New Jersey 07302, United States.

Joseph Moore (J)

SCYNEXIS, Inc., 1 Evertrust Plaza, 13th Floor, Jersey City, New Jersey 07302, United States.

Hui Tian (H)

Discovery Technologies, Medicinal Chemistry, EMD Serono Research & Development Institute, Inc., Billerica, Massachusetts 01821, United States.

Katrin Georgi (K)

Discovery Technologies, Medicinal Chemistry, EMD Serono Research & Development Institute, Inc., Billerica, Massachusetts 01821, United States.

Felix Rohdich (F)

Discovery Technologies, Medicinal Chemistry, EMD Serono Research & Development Institute, Inc., Billerica, Massachusetts 01821, United States.

Amanda Sutton (A)

Discovery Technologies, Medicinal Chemistry, EMD Serono Research & Development Institute, Inc., Billerica, Massachusetts 01821, United States.

Theresa Johnson (T)

Discovery Technologies, Medicinal Chemistry, EMD Serono Research & Development Institute, Inc., Billerica, Massachusetts 01821, United States.

Igor Mochalkin (I)

Discovery Technologies, Medicinal Chemistry, EMD Serono Research & Development Institute, Inc., Billerica, Massachusetts 01821, United States.

Jennifer Jackson (J)

Discovery Technologies, Medicinal Chemistry, EMD Serono Research & Development Institute, Inc., Billerica, Massachusetts 01821, United States.

Jing Lin (J)

Discovery Technologies, Medicinal Chemistry, EMD Serono Research & Development Institute, Inc., Billerica, Massachusetts 01821, United States.

Lindsey Crowley (L)

Discovery Technologies, Medicinal Chemistry, EMD Serono Research & Development Institute, Inc., Billerica, Massachusetts 01821, United States.

Andreas Machl (A)

Discovery Technologies, Medicinal Chemistry, EMD Serono Research & Development Institute, Inc., Billerica, Massachusetts 01821, United States.

Anderson Clark (A)

Discovery Technologies, Medicinal Chemistry, EMD Serono Research & Development Institute, Inc., Billerica, Massachusetts 01821, United States.

Erik Wilker (E)

Discovery Technologies, Medicinal Chemistry, EMD Serono Research & Development Institute, Inc., Billerica, Massachusetts 01821, United States.

Brian Sherer (B)

Discovery Technologies, Medicinal Chemistry, EMD Serono Research & Development Institute, Inc., Billerica, Massachusetts 01821, United States.

Andreas Goutopoulos (A)

Discovery Technologies, Medicinal Chemistry, EMD Serono Research & Development Institute, Inc., Billerica, Massachusetts 01821, United States.

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Classifications MeSH