Dataset Information

Discovery of 2-arylquinazoline derivatives as a new class of ASK1 inhibitors.

ABSTRACT: The development of a new series of apoptosis signal-regulating kinase 1 (ASK1) inhibitors is described. Starting from purine, pyrimidine and quinazoline scaffolds identified by high throughput screening, we used tools of structure-based drug design to develop a series of potent kinase inhibitors, including 2-arylquinazoline derivatives 12 and 23, with submicromolar inhibitory activities against ASK1. Kinetic analysis demonstrated that the 2-arylquinazoline scaffold ASK1 inhibitors described herein are ATP competitive.

SUBMITTER: Monastyrskyi A

PROVIDER: S-EPMC5999544 | biostudies-literature | 2018 Feb

REPOSITORIES: biostudies-literature

ACCESS DATA

Publications

Discovery of 2-arylquinazoline derivatives as a new class of ASK1 inhibitors.

Monastyrskyi Andrii A Bayle Simon S Quereda Victor V Grant Wayne W Cameron Michael M Duckett Derek D Roush William W

Bioorganic & medicinal chemistry letters 20171213 3

The development of a new series of apoptosis signal-regulating kinase 1 (ASK1) inhibitors is described. Starting from purine, pyrimidine and quinazoline scaffolds identified by high throughput screening, we used tools of structure-based drug design to develop a series of potent kinase inhibitors, including 2-arylquinazoline derivatives 12 and 23, with submicromolar inhibitory activities against ASK1. Kinetic analysis demonstrated that the 2-arylquinazoline scaffold ASK1 inhibitors described here ...[more]

PMID: 29277458

Dataset Information

Discovery of 2-arylquinazoline derivatives as a new class of ASK1 inhibitors.

Publications

Discovery of 2-arylquinazoline derivatives as a new class of ASK1 inhibitors.

Similar Datasets

OmicsDI is part of the ELIXIR infrastructure

Similar Datasets

Discovery of Indoline-2-carboxamide Derivatives as a New Class of Brain-Penetrant Inhibitors of Trypanosoma brucei.
| S-EPMC4601051 | biostudies-literature

5-Methoxyquinoline Derivatives as a New Class of EZH2 Inhibitors.
| S-EPMC6272711 | biostudies-literature

Discovery of Indazole Derivatives as a Novel Class of Bacterial Gyrase B Inhibitors.
| S-EPMC4601062 | biostudies-literature

Benzobicyclo[3.2.1]octene Derivatives as a New Class of Cholinesterase Inhibitors.
| S-EPMC7659976 | biostudies-literature

Discovery of [1,2,4]Triazole Derivatives as New Metallo-β-Lactamase Inhibitors.
| S-EPMC6982996 | biostudies-literature

Discovery of CNS-Penetrant Apoptosis Signal-Regulating Kinase 1 (ASK1) Inhibitors.
| S-EPMC7153032 | biostudies-literature

Aloperine and Its Derivatives as a New Class of HIV-1 Entry Inhibitors.
| S-EPMC4789664 | biostudies-literature

Thiophen urea derivatives as a new class of hepatitis C virus entry inhibitors.
| S-EPMC7822064 | biostudies-literature

Discovery of a New Class of Sortase A Transpeptidase Inhibitors to Tackle Gram-Positive Pathogens: 2-(2-Phenylhydrazinylidene)alkanoic Acids and Related Derivatives.
| S-EPMC6273394 | biostudies-literature

Fragment-based discovery of a new class of inhibitors targeting mycobacterial tRNA modification.
| S-EPMC7641325 | biostudies-literature