首页|Discovery and evaluation of 1H-pyrrolo[2,3-b]pyridine based selective and reversible small molecule BTK inhibitors for the treatment of rheumatoid arthritis

Discovery and evaluation of 1H-pyrrolo[2,3-b]pyridine based selective and reversible small molecule BTK inhibitors for the treatment of rheumatoid arthritis

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  • NSTL
  • Elsevier
In a pursuit to identify reversible and selective BTK inhibitors, two series based on 7H-pyrrolo[2,3-d] pyrimidine and 1H-pyrrolo[2,3-b]pyridine as the hinge binding core, have been identified. Structure activity relationship (SAR) exploration led to identification of two advanced lead molecules, 11 and 13, which demonstrated desired BTK inhibitory potency in different cellular assays, excellent selectivity in a panel of 50 diverse kinases, favorable in vivo PK properties in mice and anti-arthritic effect in a mouse model of CIA. (C) 2017 Elsevier Ltd. All rights reserved.

BTKReversible1H-Pyrrolo[23-b]pyridineHuman whole bloodKinase selectivityAutoimmune diseasesRheumatoid arthritis

Thakkar, Mahesh、Kaduskar, Rahul、Mengawade, Tanaji、Naik, Keshav、Salunkhe, Videsh、Bhalerao, Amit、Kurhade, Santosh、Mavinahalli, Jagadeesh、Jain, Vaibhav、Petla, Rajkanth、Avaragolla, Satheesh、Ray, Swagatam、Rouduri, Sreekanth、Dhanave, Avinash、Bhuniya, Debnath、De, Siddhartha、Pathade, Vishal、Tambe, Ashwini、Raje, Amol A.、Madgula, Vamsi、Joshi, Sachin、Nadeem, Ahmed、Bala, Madhu、Umrani, Dhananjay、Hariharan, Narayanan、Kulkarni, Bheemashankar、Mookhtiar, Kasim A.

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Advinus Therapeut Ltd, Drug Discovery Unit, Plot 9,Phase 1,Rajiv Gandhi InfoTech Pk, Pune 411057

2017

10.1016/j.bmcl.2017.02.026

Bioorganic and Medicinal Chemistry Letters

Bioorganic and Medicinal Chemistry Letters

ISSN：0960-894X
年,卷(期)：2017.27(8)
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