Discovery of new tranylcypromine derivatives as highly potent LSD1 inhibitors.

Cell Line, Tumor Dose-Response Relationship, Drug Drug Discovery Enzyme Inhibitors / chemical synthesis Histone Demethylases / antagonists & inhibitors Humans Molecular Structure Structure-Activity Relationship Tranylcypromine / analogs & derivatives
Gastric cancer Histone demethylase LSD1 inhibitor Tranylcypromine

Journal

Bioorganic & medicinal chemistry letters
ISSN: 1464-3405
Titre abrégé: Bioorg Med Chem Lett
Pays: England
ID NLM: 9107377

Informations de publication

Date de publication:
01 06 2021
Historique:
received: 22 12 2020
revised: 14 03 2021
accepted: 19 03 2021
pubmed: 30 3 2021
medline: 18 9 2021
entrez: 29 3 2021
Statut: ppublish

Résumé

Tranylcypromine (TCP)-based structural modifications lead to the discovery of new LSD1 inhibitors, of which compounds 26b and 29b effectively inhibit LSD1 with the IC

Identifiants

DOI: 10.1016/j.bmcl.2021.127993 PMID: 33775841
pubmed: 33775841
pii: S0960-894X(21)00219-5
doi: 10.1016/j.bmcl.2021.127993
pii:
doi:

Substances chimiques

Enzyme Inhibitors 0
Tranylcypromine 3E3V44J4Z9
Histone Demethylases EC 1.14.11.-
KDM1A protein, human EC 1.5.-

Types de publication

Journal Article Research Support, Non-U.S. Gov't

Langues

eng

Sous-ensembles de citation

IM

Pagination

127993

Informations de copyright

Copyright © 2021 Elsevier Ltd. All rights reserved.

Auteurs

Ming-Jie Huang (MJ)

Green Catalysis Center, and College of Chemistry, Zhengzhou University, Zhengzhou 450001, China.

Jia-Wen Guo (JW)

Green Catalysis Center, and College of Chemistry, Zhengzhou University, Zhengzhou 450001, China.

Yun-Dong Fu (YD)

Green Catalysis Center, and College of Chemistry, Zhengzhou University, Zhengzhou 450001, China.

Ya-Zhen You (YZ)

Green Catalysis Center, and College of Chemistry, Zhengzhou University, Zhengzhou 450001, China.

Wen-Yu Xu (WY)

Green Catalysis Center, and College of Chemistry, Zhengzhou University, Zhengzhou 450001, China.

Ting-Yu Song (TY)

Green Catalysis Center, and College of Chemistry, Zhengzhou University, Zhengzhou 450001, China.

Ran Li (R)

Green Catalysis Center, and College of Chemistry, Zhengzhou University, Zhengzhou 450001, China.

Zi-Tong Chen (ZT)

Green Catalysis Center, and College of Chemistry, Zhengzhou University, Zhengzhou 450001, China.

Li-Hua Huang (LH)

Green Catalysis Center, and College of Chemistry, Zhengzhou University, Zhengzhou 450001, China. Electronic address: hlh606@zzu.edu.cn.

Hong-Min Liu (HM)

School of Pharmaceutical Sciences, Zhengzhou University, Zhengzhou 450001, China. Electronic address: liuhm@zzu.edu.cn.

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Classifications MeSH

questionsmedicales.fr › Cellules › Cellules cultivées › Cellules cancéreuses en culture › Lignée cellulaire tumorale › Discovery of new tranylcypromine derivatives...
questionsmedicales.fr › Phénomènes physiologiques › Phénomènes pharmacologiques et toxicologiques › Phénomènes toxicologiques › Relation dose-effet des médicaments › Discovery of new tranylcypromine derivatives...
questionsmedicales.fr › Techniques d'investigation › Développement de médicament › Découverte de médicament › Discovery of new tranylcypromine derivatives...
questionsmedicales.fr › Actions chimiques et utilisations › Actions pharmacologiques › Mécanismes moléculaires de l'action pharmacologique › Antienzymes › Discovery of new tranylcypromine derivatives...
questionsmedicales.fr › Enzymes et coenzymes › Enzymes › Oxidoreductases › Oxidoreductases acting on CH-NH group donors › Oxidoreductases, (N-demethylating) › Histone Demethylases › Discovery of new tranylcypromine derivatives...
questionsmedicales.fr › Eucaryotes › Animaux › Chordés › Vertébrés › Mammifères › Eutheria › Primates › Haplorhini › Catarrhini › Hominidae › Humains › Discovery of new tranylcypromine derivatives...
questionsmedicales.fr › Phénomènes chimiques › Structure moléculaire › Discovery of new tranylcypromine derivatives...
questionsmedicales.fr › Phénomènes physiologiques › Phénomènes pharmacologiques et toxicologiques › Phénomènes pharmacologiques › Relation structure-activité › Discovery of new tranylcypromine derivatives...
questionsmedicales.fr › Composés chimiques organiques › Amines › Propylamines › Tranylcypromine › Discovery of new tranylcypromine derivatives...