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2 results on '"Tyurin B"'

1. Identification of 3-amido-4-anilinoquinolines as potent and selective inhibitors of CSF-1R kinase.

Author

Scott DA, Balliet CL, Cook DJ, Davies AM, Gero TW, Omer CA, Poondru S, Theoclitou ME, Tyurin B, and Zinda MJ

Subjects
Administration, Oral, Animals, Antineoplastic Agents chemical synthesis, Antineoplastic Agents chemistry, Drug Design, Humans, Inhibitory Concentration 50, Kinetics, Models, Chemical, Protein Kinase Inhibitors chemical synthesis, Protein Kinase Inhibitors chemistry, Rats, Chemistry, Pharmaceutical methods, Neoplasms drug therapy, Quinolines chemistry, Quinolines pharmacokinetics, Receptor, Macrophage Colony-Stimulating Factor antagonists & inhibitors, Receptor, Macrophage Colony-Stimulating Factor chemistry
Abstract

3-amido-4-anilinoquinolines are potent and highly selective inhibitors of CSF-1R. Their synthesis and SAR is reported, along with initial efforts to optimize the physical properties and PK through modifications at the quinoline 6- and 7-positions.

Published
2009
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2. 3-amido-4-anilinoquinolines as CSF-1R kinase inhibitors 2: Optimization of the PK profile.

Author

Scott DA, Bell KJ, Campbell CT, Cook DJ, Dakin LA, Del Valle DJ, Drew L, Gero TW, Hattersley MM, Omer CA, Tyurin B, and Zheng X

Subjects
Amines chemistry, Animals, Antineoplastic Agents chemical synthesis, Antineoplastic Agents chemistry, ERG1 Potassium Channel, Ether-A-Go-Go Potassium Channels metabolism, Humans, Inhibitory Concentration 50, Kinetics, Mice, Models, Chemical, Protein Kinase Inhibitors chemical synthesis, Protein Kinase Inhibitors chemistry, Rats, Chemistry, Pharmaceutical methods, Neoplasms drug therapy, Quinolines chemistry, Quinolines pharmacokinetics, Receptor, Macrophage Colony-Stimulating Factor antagonists & inhibitors, Receptor, Macrophage Colony-Stimulating Factor chemistry
Abstract

The optimization of compounds from the 3-amido-4-anilinoquinolines series of CSF-1R kinase inhibitors is described. The series has excellent activity and kinase selectivity. Excellent physical properties and rodent PK profiles were achieved through the introduction of cyclic amines at the quinoline 6-position. Compounds with good activity in a mouse PD model measuring inhibition of pCSF-1R were identified.

Published
2009
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