Synthesis and Structure-Activity Relationship of Tetra-Substituted Cyclohexyl Diol Inhibitors of Proviral Insertion of Moloney Virus (PIM) Kinases.

Cell Line, Tumor Cyclohexanols / chemical synthesis Humans Microsomes, Liver / metabolism Molecular Docking Simulation Molecular Structure Protein Binding Protein Kinase Inhibitors / chemical synthesis Proto-Oncogene Proteins c-pim-1 / antagonists & inhibitors Structure-Activity Relationship

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:
10 12 2020
Historique:
pubmed: 2 12 2020
medline: 4 2 2021
entrez: 1 12 2020
Statut: ppublish

Résumé

Overexpression of PIM 1, 2, and 3 kinases is frequently observed in many malignancies. Previously, we discovered a potent and selective pan-PIM kinase inhibitor, compound

Identifiants

DOI: 10.1021/acs.jmedchem.0c01279 PMID: 33258605
pubmed: 33258605
doi: 10.1021/acs.jmedchem.0c01279
doi:

Substances chimiques

Cyclohexanols 0
Protein Kinase Inhibitors 0
Proto-Oncogene Proteins c-pim-1 EC 2.7.11.1

Types de publication

Journal Article

Langues

eng

Sous-ensembles de citation

IM

Pagination

14885-14904

Auteurs

Wooseok Han (W)

Novartis Institutes for BioMedical Research, Emeryville, California 94608, United States.
Global Discovery Chemistry, Novartis Institutes for BioMedical Research, Cambridge, Massachusetts 02139, United States.
ORCID: 0000-0002-7567-1883

Yu Ding (Y)

Novartis Institutes for BioMedical Research, Emeryville, California 94608, United States.
BeiGene, Ltd., San Mateo, California 94403, United States.

Zheng Chen (Z)

Novartis Institutes for BioMedical Research, Emeryville, California 94608, United States.
Boston Analytical, Salem, New Hampshire 03079, United States.

John L Langowski (JL)

Novartis Institutes for BioMedical Research, Emeryville, California 94608, United States.
Kite, a Gilead Company, Emeryville, California 94608, United States.

Cornelia Bellamacina (C)

Novartis Institutes for BioMedical Research, Emeryville, California 94608, United States.
Crystallographic Consulting, Berkeley, California 94704, United States.

Alice Rico (A)

Novartis Institutes for BioMedical Research, Emeryville, California 94608, United States.
Exelixis, Alameda, California 94502, United States.

Gisele A Nishiguchi (GA)

Novartis Institutes for BioMedical Research, Emeryville, California 94608, United States.
St. Jude Children's Research Hospital, Memphis, Tennessee 38105, United States.

Jiong Lan (J)

Novartis Institutes for BioMedical Research, Emeryville, California 94608, United States.
Genfleet Therapeutics, Inc., Pudong District, Shanghai 201203, China.

Gordana Atallah (G)

Novartis Institutes for BioMedical Research, Emeryville, California 94608, United States.
Pharmacyclics, an AbbVie Company, Sunnyvale, California 94085, United States.

Mika Lindvall (M)

Novartis Institutes for BioMedical Research, Emeryville, California 94608, United States.
Recursion Pharmaceuticals, Salt Lake City, Utah 84101, United States.

Song Lin (S)

Novartis Institutes for BioMedical Research, Emeryville, California 94608, United States.
Astex Pharmaceuticals Inc., Pleasanton, California 94588, United States.

Richard Zang (R)

Novartis Institutes for BioMedical Research, Emeryville, California 94608, United States.
Global Blood Therapeutics, South San Francisco, California 94080, United States.

Paul Feucht (P)

Novartis Institutes for BioMedical Research, Emeryville, California 94608, United States.

Tatiana Zavorotinskaya (T)

Novartis Institutes for BioMedical Research, Emeryville, California 94608, United States.
ORIC Pharmaceuticals, South San Francisco, California 94080, United States.

Yumin Dai (Y)

Novartis Institutes for BioMedical Research, Emeryville, California 94608, United States.
Bristol Myers Squibb, Redwood City, California 94158, United States.

Pablo Garcia (P)

Novartis Institutes for BioMedical Research, Emeryville, California 94608, United States.
Circle Pharma, Inc., South San Francisco, California 94080, United States.

Matthew T Burger (MT)

Novartis Institutes for BioMedical Research, Emeryville, California 94608, United States.
Novartis Institutes for BioMedical Research, Cambridge, Massachusetts 02139, United States.

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Classifications MeSH

questionsmedicales.fr › Cellules › Cellules cultivées › Cellules cancéreuses en culture › Lignée cellulaire tumorale › Synthesis and Structure-Activity Relationship...
questionsmedicales.fr › Lipides › Alcools gras › Hexanols › Cyclohexanols › Synthesis and Structure-Activity Relationship...
questionsmedicales.fr › Eucaryotes › Animaux › Chordés › Vertébrés › Mammifères › Eutheria › Primates › Haplorhini › Catarrhini › Hominidae › Humains › Synthesis and Structure-Activity Relationship...
questionsmedicales.fr › Cellules › Structures cellulaires › Fractions subcellulaires › Microsomes › Microsomes du foie › Synthesis and Structure-Activity Relationship...
questionsmedicales.fr › Sciences de l'information › Méthodologies informatiques › Simulation numérique › Simulation de docking moléculaire › Synthesis and Structure-Activity Relationship...
questionsmedicales.fr › Phénomènes chimiques › Structure moléculaire › Synthesis and Structure-Activity Relationship...
questionsmedicales.fr › Métabolisme › Liaison aux protéines › Synthesis and Structure-Activity Relationship...
questionsmedicales.fr › Actions chimiques et utilisations › Actions pharmacologiques › Mécanismes moléculaires de l'action pharmacologique › Antienzymes › Inhibiteurs de protéines kinases › Synthesis and Structure-Activity Relationship...
questionsmedicales.fr › Acides aminés, peptides et protéines › Protéines › Protéines tumorales › Protéines oncogènes › Protéines proto-oncogènes › Protéines proto-oncogènes c-pim-1 › Synthesis and Structure-Activity Relationship...
questionsmedicales.fr › Phénomènes physiologiques › Phénomènes pharmacologiques et toxicologiques › Phénomènes pharmacologiques › Relation structure-activité › Synthesis and Structure-Activity Relationship...