Discovery of a Thiadiazole–Pyridazine-Based Allosteric Glutaminase 1 Inhibitor Series That Demonstrates Oral Bioavailability and Activity in Tumor Xenograft Models

Author:

Finlay M. Raymond V.1ORCID,Anderton Mark1,Bailey Andrew1,Boyd Scott1,Brookfield Joanna2,Cairnduff Ceri2,Charles Mark2,Cheasty Anne2,Critchlow Susan E.1,Culshaw Janet1,Ekwuru Tennyson2,Hollingsworth Ian1,Jones Neil2,Leroux Fred2,Littleson Mairi1ORCID,McCarron Hollie2,McKelvie Jennifer2,Mooney Lorraine1,Nissink J. Willem M.1ORCID,Perkins David1,Powell Steve1,Quesada Mar Jimenez2,Raubo Piotr1,Sabin Verity2,Smith James2,Smith Peter D.1ORCID,Stark Andrew1,Ting Attilla1,Wang Peng3,Wilson Zena1,Winter-Holt Jon J.1,Wood J. Matthew1,Wrigley Gail L.1,Yu Guoqing3,Zhang Peng3

Affiliation:

1. Oncology, IMED Biotech Unit, AstraZeneca, 310, Cambridge Science Park, Milton Road, Cambridge CB4 0FZ, United Kingdom

2. Cancer Research UK, Therapeutic Discovery Laboratories, Jonas Webb Building, Babraham Research Campus, Cambridge CB22 3AT, United Kingdom

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

Publisher

American Chemical Society (ACS)

Subject

Drug Discovery,Molecular Medicine

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