Optimization of an Imidazo[1,2-a]pyridine Series to Afford Highly Selective Type I1/2 Dual Mer/Axl Kinase Inhibitors with In Vivo Efficacy-Reference-Cited by-同舟云学术

Optimization of an Imidazo[1,2-a]pyridine Series to Afford Highly Selective Type I1/2 Dual Mer/Axl Kinase Inhibitors with In Vivo Efficacy

Published:2021-09-03 Issue:18 Volume:64 Page:13524-13539
ISSN:0022-2623
Container-title:Journal of Medicinal Chemistry
language:en
Short-container-title:J. Med. Chem.

Author:

McCoull William¹^ORCID,Boyd Scott¹,Brown Martin R.²,Coen Muireann³,Collingwood Olga¹,Davies Nichola L.¹,Doherty Ann³,Fairley Gary¹,Goldberg Kristin¹,Hardaker Elizabeth¹,He Guang⁴,Hennessy Edward J.⁵,Hopcroft Philip²,Hodgson George²,Jackson Anne²,Jiang Xiefeng⁴,Karmokar Ankur⁶,Lainé Anne-Laure⁷,Lindsay Nicola¹,Mao Yumeng¹,Markandu Roshini¹,McMurray Lindsay¹,McLean Neville¹,Mooney Lorraine⁶,Musgrove Helen⁶,Nissink J. Willem M.¹^ORCID,Pflug Alexander²,Reddy Venkatesh Pilla³,Rawlins Philip B.²,Rivers Emma²,Schimpl Marianne²^ORCID,Smith Graham F.³,Tentarelli Sharon⁵^ORCID,Travers Jon¹,Troup Robert I.¹,Walton Josephine¹,Wang Cheng⁴,Wilkinson Stephen¹,Williamson Beth¹,Winter-Holt Jon¹,Yang Dejian⁴,Zheng Yuting⁴,Zhu Qianxiu⁴,Smith Paul D.¹

Affiliation:

1. Oncology R&D, AstraZeneca, Cambridge CB4 0WG, U.K.

2. Discovery Sciences, R&D, AstraZeneca, Cambridge CB4 0WG, U.K.

3. Clinical Pharmacology & Safety Sciences, BioPharmaceuticals R&D, AstraZeneca, Cambridge CB4 0WG, U.K.

4. Pharmaron Beijing Co., Ltd., 6 Taihe Road BDA, Beijing 100176, P. R. China

5. Oncology R&D, AstraZeneca, Gatehouse Park, Waltham, Massachusetts 02451, United States

6. Oncology R&D, AstraZeneca, Mereside, Alderley Park, Macclesfield SK10 4TG, U.K.

7. Pharmaceutical Sciences, BioPharmaceuticals R&D, AstraZeneca, Cambridge CB4 0WG, U.K.

Publisher

American Chemical Society (ACS)

Subject

Drug Discovery,Molecular Medicine

Link

https://pubs.acs.org/doi/pdf/10.1021/acs.jmedchem.1c00920

Reference27 articles.

1. The TAM family: phosphatidylserine-sensing receptor tyrosine kinases gone awry in cancer

2. TAM-ing T cells in the tumor microenvironment: implications for TAM receptor targeting

3. TAM receptor tyrosine kinases as emerging targets of innate immune checkpoint blockade for cancer therapy

4. Axl and Mertk Receptors Cooperate to Promote Breast Cancer Progression by Combined Oncogenic Signaling and Evasion of Host Antitumor Immunity

5. Targeting Tyro3, Axl and MerTK (TAM receptors): implications for macrophages in the tumor microenvironment

Cited by 18 articles. 订阅此论文施引文献订阅此论文施引文献，注册后可以免费订阅5篇论文的施引文献，订阅后可以查看论文全部施引文献

1. Hit me with your best shot: Integrated hit discovery for the next generation of drug targets;Drug Discovery Today;2024-10

2. Building Block-Centric Approach to DNA-Encoded Library Design;Journal of Chemical Information and Modeling;2024-06-11

3. Recent discovery and development of AXL inhibitors as antitumor agents;European Journal of Medicinal Chemistry;2024-06

4. Kinase Inhibitors and Kinase-Targeted Cancer Therapies: Recent Advances and Future Perspectives;International Journal of Molecular Sciences;2024-05-17

5. Discovery of Novel Macrocyclic MERTK/AXL Dual Inhibitors;Journal of Medicinal Chemistry;2024-04-01