Discovery of Quinazoline-2,4(1

Animals Antineoplastic Agents / blood Crystallography, X-Ray Dogs Drug Discovery Humans Mice Molecular Structure Piperazines / chemistry Poly (ADP-Ribose) Polymerase-1 / antagonists & inhibitors Poly(ADP-ribose) Polymerase Inhibitors / blood Poly(ADP-ribose) Polymerases Quinazolines / chemistry Rats Structure-Activity Relationship Xenograft Model Antitumor Assays

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:
25 11 2021
Historique:
pubmed: 9 11 2021
medline: 29 1 2022
entrez: 8 11 2021
Statut: ppublish

Résumé

Inhibiting PARP-1/2 offered an important arsenal for cancer treatments via interfering with DNA repair of cancer cells. Novel PARP-1/2 inhibitors were designed by capitalizing on methyl- or ethyl-substituted piperizine ring to capture the characteristics of adenine-ribose binding site (AD site), and their unique binding features were revealed by the cocrystal structures of compounds

Identifiants

DOI: 10.1021/acs.jmedchem.1c01522 PMID: 34748333
pubmed: 34748333
doi: 10.1021/acs.jmedchem.1c01522
doi:

Substances chimiques

Antineoplastic Agents 0
Piperazines 0
Poly(ADP-ribose) Polymerase Inhibitors 0
Quinazolines 0
PARP1 protein, human EC 2.4.2.30
PARP2 protein, human EC 2.4.2.30
Poly (ADP-Ribose) Polymerase-1 EC 2.4.2.30
Poly(ADP-ribose) Polymerases EC 2.4.2.30

Types de publication

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

Langues

eng

Sous-ensembles de citation

IM

Pagination

16711-16730

Auteurs

Jie Zhou (J)

Beijing Key Laboratory of Active Substances Discovery and Druggability Evaluation, Institute of Materia Medica, Chinese Academy of Medical Sciences and Peking Union Medical College, Beijing 100050, China.

Ming Ji (M)

Department of Pharmacology, Institute of Materia Medica, Chinese Academy of Medical Sciences and Peking Union Medical College, Beijing 100050, China.
State Key Laboratory of Bioactive Substances and Functions of Natural Medicines, Institute of Materia Medica, Chinese Academy of Medical Sciences and Peking Union Medical College, Beijing 100050, China.

Xiaoyu Wang (X)

Beijing Key Laboratory of Active Substances Discovery and Druggability Evaluation, Institute of Materia Medica, Chinese Academy of Medical Sciences and Peking Union Medical College, Beijing 100050, China.

Hailong Zhao (H)

Beijing Key Laboratory of Active Substances Discovery and Druggability Evaluation, Institute of Materia Medica, Chinese Academy of Medical Sciences and Peking Union Medical College, Beijing 100050, China.

Ran Cao (R)

Beijing Key Laboratory of Active Substances Discovery and Druggability Evaluation, Institute of Materia Medica, Chinese Academy of Medical Sciences and Peking Union Medical College, Beijing 100050, China.

Jing Jin (J)

Department of Pharmacology, Institute of Materia Medica, Chinese Academy of Medical Sciences and Peking Union Medical College, Beijing 100050, China.
State Key Laboratory of Bioactive Substances and Functions of Natural Medicines, Institute of Materia Medica, Chinese Academy of Medical Sciences and Peking Union Medical College, Beijing 100050, China.

Yan Li (Y)

Beijing Key Laboratory of Non-Clinical Drug Metabolism and PK/PD Study, Institute of Materia Medica, Chinese Academy of Medical Sciences and Peking Union Medical College, Beijing 100050, China.

Xianhong Chen (X)

Beijing Key Laboratory of Non-Clinical Drug Metabolism and PK/PD Study, Institute of Materia Medica, Chinese Academy of Medical Sciences and Peking Union Medical College, Beijing 100050, China.
Beijing Collab Pharma Co., Ltd, Beijing 102600, China.

Li Sheng (L)

Beijing Key Laboratory of Non-Clinical Drug Metabolism and PK/PD Study, Institute of Materia Medica, Chinese Academy of Medical Sciences and Peking Union Medical College, Beijing 100050, China.

Xiaoguang Chen (X)

Department of Pharmacology, Institute of Materia Medica, Chinese Academy of Medical Sciences and Peking Union Medical College, Beijing 100050, China.
State Key Laboratory of Bioactive Substances and Functions of Natural Medicines, Institute of Materia Medica, Chinese Academy of Medical Sciences and Peking Union Medical College, Beijing 100050, China.

Bailing Xu (B)

Beijing Key Laboratory of Active Substances Discovery and Druggability Evaluation, Institute of Materia Medica, Chinese Academy of Medical Sciences and Peking Union Medical College, Beijing 100050, China.
ORCID: 0000-0003-2633-0887

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Classifications MeSH

questionsmedicales.fr › Eucaryotes › Animaux › Discovery of Quinazoline-2,4(1
questionsmedicales.fr › Actions chimiques et utilisations › Actions pharmacologiques › Utilisations thérapeutiques › Antinéoplasiques › Discovery of Quinazoline-2,4(1
questionsmedicales.fr › Techniques d'investigation › Techniques de chimie analytique › Cristallographie aux rayons X › Discovery of Quinazoline-2,4(1
questionsmedicales.fr › Eucaryotes › Animaux › Chordés › Vertébrés › Mammifères › Eutheria › Carnivora › Pinnipedia › Canidae › Chiens › Discovery of Quinazoline-2,4(1
questionsmedicales.fr › Techniques d'investigation › Développement de médicament › Découverte de médicament › Discovery of Quinazoline-2,4(1
questionsmedicales.fr › Eucaryotes › Animaux › Chordés › Vertébrés › Mammifères › Eutheria › Primates › Haplorhini › Catarrhini › Hominidae › Humains › Discovery of Quinazoline-2,4(1
questionsmedicales.fr › Eucaryotes › Animaux › Chordés › Vertébrés › Mammifères › Eutheria › Rodentia › Muridae › Murinae › Souris › Discovery of Quinazoline-2,4(1
questionsmedicales.fr › Phénomènes chimiques › Structure moléculaire › Discovery of Quinazoline-2,4(1
questionsmedicales.fr › Composés hétérocycliques › Composés hétéromonocycliques › Pipérazines › Discovery of Quinazoline-2,4(1
questionsmedicales.fr › Enzymes et coenzymes › Enzymes › Transferases › Glycosyltransferase › Pentosyltransferases › ADP ribose transferases › Poly(ADP-ribose) polymerases › Poly (ADP-Ribose) polymerase-1 › Discovery of Quinazoline-2,4(1
questionsmedicales.fr › Actions chimiques et utilisations › Actions pharmacologiques › Utilisations thérapeutiques › Antinéoplasiques › Inhibiteurs de poly(ADP-ribose) polymérases › Discovery of Quinazoline-2,4(1
questionsmedicales.fr › Enzymes et coenzymes › Enzymes › Transferases › Glycosyltransferase › Pentosyltransferases › ADP ribose transferases › Poly(ADP-ribose) polymerases › Discovery of Quinazoline-2,4(1
questionsmedicales.fr › Composés hétérocycliques › Composés hétérocycliques à cycles fusionnés › Composés hétérobicycliques › Quinazolines › Discovery of Quinazoline-2,4(1
questionsmedicales.fr › Eucaryotes › Animaux › Chordés › Vertébrés › Mammifères › Eutheria › Rodentia › Muridae › Murinae › Rats › Discovery of Quinazoline-2,4(1
questionsmedicales.fr › Phénomènes physiologiques › Phénomènes pharmacologiques et toxicologiques › Phénomènes pharmacologiques › Relation structure-activité › Discovery of Quinazoline-2,4(1
questionsmedicales.fr › Techniques d'investigation › Transplantation tumorale › Tests d'activité antitumorale sur modèle de xénogreffe › Discovery of Quinazoline-2,4(1