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3 results on '"Han, Cheolkyu"'

1. Synthesis and biological evaluation of N-(3-fluorobenzyl)-4-(1-(methyl-d3)-1H-indazol-5-yl)-5-(6-methylpyridin-2-yl)-1H-imidazol-2-amine as a novel, potent ALK5 receptor inhibitor

Author

Kang, Byung-Nam, primary, Kang, Hong-Jun, additional, Kim, Sunjoo, additional, Lee, Jungwoo, additional, Lee, Jinwoo, additional, Jeong, Hee-Jin, additional, Jeon, Seeun, additional, Shin, Youngdo, additional, Yoon, Cheolhwan, additional, Han, Cheolkyu, additional, Seo, Jeongbeob, additional, and Yun, Jaesook, additional

Published
2023
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3. Synthesis and biological evaluation of N-(3-fluorobenzyl)-4-(1-(methyl-d 3 )-1H-indazol-5-yl)-5-(6-methylpyridin-2-yl)-1H-imidazol-2-amine as a novel, potent ALK5 receptor inhibitor.

Author

Kang BN, Kang HJ, Kim S, Lee J, Lee J, Jeong HJ, Jeon S, Shin Y, Yoon C, Han C, Seo J, and Yun J

Subjects
Mice, Animals, Receptor, Transforming Growth Factor-beta Type I metabolism, Amines, Indazoles pharmacology, Cytochrome P-450 Enzyme System metabolism, Structure-Activity Relationship, Protein Kinase Inhibitors pharmacology, Protein Serine-Threonine Kinases, Receptors, Transforming Growth Factor beta metabolism
Abstract

Specific inhibition of ALK5 provides a novel method for controlling the development of cancers and fibrotic diseases. In this work, a novel series of N-(3-fluorobenzyl)-4-(1-(methyl-d 3 )-1H-indazol-5-yl)-5-(6-methylpyridin-2-yl)-1H-imidazol-2-amine (11), a potential clinical candidate, was synthesized by strategic incorporation of deuterium at potential metabolic soft spots and identified as ALK5 inhibitors. This compound has a low potential for CYP-mediated drug-drug interactions as a CYP450 inhibitor (IC 50  = >10 μM) and showed potent inhibitory effects in cellular assay (IC 50  = 3.5 ± 0.4 nM). The pharmacokinetic evaluation of 11 in mice demonstrated moderate clearance (29.0 mL/min/kg) and also revealed high oral bioavailability in mice (F = 67.6%)., Competing Interests: Declaration of Competing Interest The authors declare that they have no known competing financial interests or personal relationships that could have appeared to influence the work reported in this paper., (Copyright © 2023 Elsevier Ltd. All rights reserved.)

Published
2023
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