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Tianfeng Xu
Tianfeng Xu
Verified email at umich.edu
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Year
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
3302019
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
1732019
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
1382012
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
932011
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
592018
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
542022
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
432022
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
402015
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
352013
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
332013
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
322017
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
262020
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
242019
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
232022
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
142023
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
142023
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
122023
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
72023
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
62022
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
52023
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