Structure-Based Drug Design of Novel Triaminotriazine Derivatives as Orally Bioavailable IDH2<sup>R140Q</sup> Inhibitors with High Selectivity and Reduced hERG Inhibitory Activity for the Treatment of Acute Myeloid Leukemia-Reference-Cited by-同舟云学术

Structure-Based Drug Design of Novel Triaminotriazine Derivatives as Orally Bioavailable IDH2^R140Q Inhibitors with High Selectivity and Reduced hERG Inhibitory Activity for the Treatment of Acute Myeloid Leukemia

Published:2023-09-14 Issue:18 Volume:66 Page:12894-12910
ISSN:0022-2623
Container-title:Journal of Medicinal Chemistry
language:en
Short-container-title:J. Med. Chem.

Author:

Wei Qingyun¹²,Yao Kun³,Yang Jie¹²,Zhou Qian¹²,Liu Pengyu³,Chen Jiao¹²,Liu Haipeng³,Lai Yisheng³^ORCID,Cao Peng¹⁴^ORCID

Affiliation:

1. Jiangsu Provincial Medical Innovation Center, Affiliated Hospital of Integrated Traditional Chinese and Western Medicine, Nanjing University of Chinese Medicine, Nanjing 210028, China

2. Jiangsu Province Academy of Traditional Chinese Medicine, Nanjing 210028, China

3. State Key Laboratory of Natural Medicines, Jiangsu Key Laboratory of Drug Discovery for Metabolic Diseases, Center of Drug Discovery, China Pharmaceutical University, Nanjing 210009, China

4. School of Pharmacy, Nanjing University of Chinese Medicine, Nanjing 210023, China

Funder

National Science Fund for Distinguished Young Scholars

National Natural Science Foundation of China

Jiangsu Provincial Medical Innovation Center

Publisher

American Chemical Society (ACS)

Subject

Drug Discovery,Molecular Medicine

Link

https://pubs.acs.org/doi/pdf/10.1021/acs.jmedchem.3c00835

Reference46 articles.

1. NCCN Guidelines Insights: Acute Myeloid Leukemia, Version 2.2021

2. Advances in acute myeloid leukemia

3. Isocitrate Dehydrogenase 1 and 2 Mutations in Cancer: Alterations at a Crossroads of Cellular Metabolism

4. The Common Feature of Leukemia-Associated IDH1 and IDH2 Mutations Is a Neomorphic Enzyme Activity Converting α-Ketoglutarate to 2-Hydroxyglutarate

5. The implications of IDH mutations for cancer development and therapy

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