Search

Your search keyword '"Arshad Siddiqui M"' showing total 2 results
Start Over Author "Arshad Siddiqui M" Topic pyrazines
2 results on '"Arshad Siddiqui M"'

1. Potency switch between CHK1 and MK2: discovery of imidazo[1,2-a]pyrazine- and imidazo[1,2-c]pyrimidine-based kinase inhibitors.

Author

Meng Z, Ciavarri JP, McRiner A, Zhao Y, Zhao L, Reddy PA, Zhang X, Fischmann TO, Whitehurst C, and Arshad Siddiqui M

Subjects
Checkpoint Kinase 1, Dose-Response Relationship, Drug, Humans, Imidazoles chemical synthesis, Imidazoles chemistry, Intracellular Signaling Peptides and Proteins metabolism, Models, Molecular, Molecular Structure, Protein Kinase Inhibitors chemical synthesis, Protein Kinase Inhibitors chemistry, Protein Serine-Threonine Kinases metabolism, Pyrazines chemical synthesis, Pyrazines chemistry, Pyrimidines chemical synthesis, Pyrimidines chemistry, Structure-Activity Relationship, Drug Discovery, Imidazoles pharmacology, Intracellular Signaling Peptides and Proteins antagonists & inhibitors, Protein Kinase Inhibitors pharmacology, Protein Kinases metabolism, Protein Serine-Threonine Kinases antagonists & inhibitors, Pyrazines pharmacology, Pyrimidines pharmacology
Abstract

Chemistry has been developed to access both imidazo[1,2-a]pyrazines and imidazo[1,2-c]pyrimidines. Small structural modifications in both series led to a switch of potency between two kinases involved in mediating cell cycle checkpoint control, CHK1 and MK2., (Copyright © 2013 Elsevier Ltd. All rights reserved.)

Published
2013
Full Text
View/download PDF

2. Discovery of novel imidazo[1,2-a]pyrazin-8-amines as Brk/PTK6 inhibitors.

Author

Zeng H, Belanger DB, Curran PJ, Shipps GW Jr, Miao H, Bracken JB, Arshad Siddiqui M, Malkowski M, and Wang Y

Subjects
Adaptor Proteins, Signal Transducing metabolism, Animals, Aurora Kinases, Breast Neoplasms drug therapy, Breast Neoplasms genetics, Computer Simulation, DNA-Binding Proteins metabolism, Dasatinib, Dose-Response Relationship, Drug, Drug Design, Drug Discovery, Drug Screening Assays, Antitumor, Female, Humans, Imidazoles chemistry, Imidazoles pharmacokinetics, Inhibitory Concentration 50, Melanocytes physiology, Mice, Molecular Targeted Therapy, Neoplasm Proteins genetics, Oncogenes, Phenotype, Protein Kinase Inhibitors chemistry, Protein Kinase Inhibitors pharmacokinetics, Protein Serine-Threonine Kinases antagonists & inhibitors, Protein-Tyrosine Kinases genetics, Proto-Oncogenes, Pyrazines chemistry, Pyrazines pharmacokinetics, Pyrimidines metabolism, RNA-Binding Proteins metabolism, Structure-Activity Relationship, Thiazoles metabolism, Breast Neoplasms enzymology, Imidazoles chemical synthesis, Imidazoles pharmacology, Neoplasm Proteins antagonists & inhibitors, Protein Kinase Inhibitors chemical synthesis, Protein Kinase Inhibitors pharmacology, Protein-Tyrosine Kinases antagonists & inhibitors, Pyrazines chemical synthesis, Pyrazines pharmacology
Abstract

A series of substituted imidazo[1,2-a]pyrazin-8-amines were discovered as novel breast tumor kinase (Brk)/protein tyrosine kinase 6 (PTK6) inhibitors. Tool compounds with low-nanomolar Brk inhibition activity, high selectivity towards other kinases and desirable DMPK properties were achieved to enable the exploration of Brk as an oncology target., (Copyright © 2011 Elsevier Ltd. All rights reserved.)

Published
2011
Full Text
View/download PDF

Catalog

Books, media, physical & digital resources
See catalog results