Discovery of ARD-69 as a highly potent proteolysis targeting chimera (PROTAC) degrader of androgen receptor (AR) for the treatment of prostate cancer X Han, C Wang, C Qin, W Xiang, E Fernandez-Salas, CY Yang, M Wang, ... Journal of medicinal chemistry 62 (2), 941-964, 2019 | 331 | 2019 |
Discovery of highly potent and efficient PROTAC degraders of androgen receptor (AR) by employing weak binding affinity VHL E3 ligase ligands X Han, L Zhao, W Xiang, C Qin, B Miao, T Xu, M Wang, CY Yang, ... Journal of medicinal chemistry 62 (24), 11218-11231, 2019 | 173 | 2019 |
Design, synthesis, and biological evaluation of novel conformationally constrained inhibitors targeting epidermal growth factor receptor threonine790→ methionine790 mutant S Chang, L Zhang, S Xu, J Luo, X Lu, Z Zhang, T Xu, Y Liu, Z Tu, Y Xu, ... Journal of Medicinal Chemistry 55 (6), 2711-2723, 2012 | 138 | 2012 |
Copper-Catalyzed Tandem Reactions of 1-(2-Iodoary)-2-yn-1-ones with Isocyanides for the Synthesis of 4-Oxo-indeno[1,2-b]pyrroles Q Cai, F Zhou, T Xu, L Fu, K Ding Organic Letters 13 (2), 340-343, 2011 | 93 | 2011 |
Design of the first‐in‐class, highly potent irreversible inhibitor targeting the menin‐MLL protein–protein interaction S Xu, A Aguilar, T Xu, K Zheng, L Huang, J Stuckey, K Chinnaswamy, ... Angewandte Chemie 130 (6), 1617-1621, 2018 | 59 | 2018 |
Engineered bioorthogonal POLY-PROTAC nanoparticles for tumour-specific protein degradation and precise cancer therapy J Gao, B Hou, Q Zhu, L Yang, X Jiang, Z Zou, X Li, T Xu, M Zheng, ... Nature Communications 13 (1), 4318, 2022 | 54 | 2022 |
Discovery of the first-in-class agonist-based SOS1 PROTACs effective in human cancer cells harboring various KRAS mutations C Zhou, Z Fan, Z Zhou, Y Li, R Cui, C Liu, G Zhou, X Diao, H Jiang, ... Journal of medicinal chemistry 65 (5), 3923-3942, 2022 | 43 | 2022 |
C5-substituted pyrido [2, 3-d] pyrimidin-7-ones as highly specific kinase inhibitors targeting the clinical resistance-related EGFR T790M mutant T Xu, T Peng, X Ren, L Zhang, L Yu, J Luo, Z Zhang, Z Tu, L Tong, ... MedChemComm 6 (9), 1693-1697, 2015 | 40 | 2015 |
Pyrimido[4,5‐d]pyrimidin‐4(1H)‐one Derivatives as Selective Inhibitors of EGFR Threonine790 to Methionine790 (T790M) Mutants T Xu, L Zhang, S Xu, CY Yang, J Luo, F Ding, X Lu, Y Liu, Z Tu, S Li, D Pei, ... Angewandte Chemie International Edition 52 (32), 8387-8390, 2013 | 35 | 2013 |
Design, Synthesis, and Biological Evaluation of 2-Oxo-3,4-dihydropyrimido[4,5-d]pyrimidinyl Derivatives as New Irreversible Epidermal Growth Factor Receptor … S Xu, T Xu, L Zhang, Z Zhang, J Luo, Y Liu, X Lu, Z Tu, X Ren, K Ding Journal of medicinal chemistry 56 (21), 8803-8813, 2013 | 33 | 2013 |
A structure-guided optimization of pyrido [2, 3-d] pyrimidin-7-ones as selective inhibitors of EGFRL858R/T790M mutant with improved pharmacokinetic properties L Yu, M Huang, T Xu, L Tong, X Yan, Z Zhang, Y Xu, C Yun, H Xie, K Ding, ... European journal of medicinal chemistry 126, 1107-1117, 2017 | 32 | 2017 |
Discovery of M-808 as a Highly Potent, Covalent, Small-Molecule Inhibitor of the Menin–MLL Interaction with Strong In Vivo Antitumor Activity S Xu, A Aguilar, L Huang, T Xu, K Zheng, D McEachern, S Przybranowski, ... Journal of medicinal chemistry 63 (9), 4997-5010, 2020 | 26 | 2020 |
Design, synthesis, and biological evaluation of novel EGFR PROTACs targeting Del19/T790M/C797S mutation H Zhang, R Xie, H Ai-Furas, Y Li, Q Wu, J Li, F Xu, T Xu ACS Medicinal Chemistry Letters 13 (2), 278-283, 2022 | 24 | 2022 |
Structure-based discovery of M-89 as a highly potent inhibitor of the menin-mixed lineage leukemia (Menin-MLL) protein–protein interaction A Aguilar, K Zheng, T Xu, S Xu, L Huang, E Fernandez-Salas, L Liu, ... Journal of medicinal chemistry 62 (13), 6015-6034, 2019 | 24 | 2019 |
Discovery of ARD-2051 as a potent and orally efficacious proteolysis targeting chimera (PROTAC) degrader of androgen receptor for the treatment of advanced prostate cancer X Han, L Zhao, W Xiang, B Miao, C Qin, M Wang, T Xu, D McEachern, ... Journal of Medicinal Chemistry 66 (13), 8822-8843, 2023 | 14 | 2023 |
Discovery of a potent, cooperative, and selective SOS1 PROTAC ZZ151 with in vivo antitumor efficacy in KRAS-mutant cancers Z Zhou, G Zhou, C Zhou, Z Fan, R Cui, Y Li, R Li, Y Gu, H Li, Z Ge, X Cai, ... Journal of medicinal chemistry 66 (6), 4197-4214, 2023 | 14 | 2023 |
Stimuli-activatable PROTACs for precise protein degradation and cancer therapy J Gao, L Yang, S Lei, F Zhou, H Nie, B Peng, T Xu, X Chen, X Yang, ... Science bulletin, 2023 | 12 | 2023 |
Design, Synthesis, and Bioevaluation of Pyrido[2,3-d]pyrimidin-7-ones as Potent SOS1 Inhibitors M Liu, G Zhou, W Su, Y Gu, M Gao, K Wang, R Huo, Y Li, Z Zhou, K Chen, ... ACS Medicinal Chemistry Letters 14 (2), 183-190, 2023 | 7 | 2023 |
Discovery of ARD-1676 as a Highly Potent and Orally Efficacious AR PROTAC Degrader with a Broad Activity against AR Mutants for the Treatment of AR+ Human Prostate Cancer W Xiang, L Zhao, X Han, T Xu, S Kregel, M Wang, B Miao, C Qin, M Wang, ... Journal of Medicinal Chemistry 66 (18), 13280-13303, 2023 | 6 | 2023 |
Design, synthesis and structure-activity relationship studies of pyrido [2, 3-d] pyrimidin-7-ones as potent Janus Kinase 3 (JAK3) covalent inhibitors W Su, Z Chen, M Liu, R He, C Liu, R Li, M Gao, M Zheng, Z Tu, Z Zhang, ... Bioorganic & Medicinal Chemistry Letters 64, 128680, 2022 | 6 | 2022 |