Publications by authors named "Tianfeng Xu"

10Publications

Discovery of Highly Potent and Efficient PROTAC Degraders of Androgen Receptor (AR) by Employing Weak Binding Affinity VHL E3 Ligase Ligands.

J Med Chem 2019 12 5;62(24):11218-11231. Epub 2019 Dec 5.

School of Pharmaceutical Sciences and Institute of Drug Discovery & Development , Zhengzhou University , Zhengzhou 450001 , China.

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December 2019

Design of the First-in-Class, Highly Potent Irreversible Inhibitor Targeting the Menin-MLL Protein-Protein Interaction.

Angew Chem Int Ed Engl 2018 02 15;57(6):1601-1605. Epub 2018 Jan 15.

Comprehensive Cancer and Departments of Internal Medicine, Pharmacology and Medicinal Chemistry, University of Michigan, 1600 Huron Parkway, Ann Arbor, MI, 48109, USA.

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February 2018

A structure-guided optimization of pyrido[2,3-d]pyrimidin-7-ones as selective inhibitors of EGFR mutant with improved pharmacokinetic properties.

Eur J Med Chem 2017 Jan 3;126:1107-1117. Epub 2016 Dec 3.

School of Pharmacy, Jinan University, No. 601 Huangpu Avenue West, Guangzhou 510632, China. Electronic address:

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January 2017

Design, synthesis, and biological evaluation of 2-oxo-3,4-dihydropyrimido[4,5-d]pyrimidinyl derivatives as new irreversible epidermal growth factor receptor inhibitors with improved pharmacokinetic properties.

J Med Chem 2013 Nov 31;56(21):8803-13. Epub 2013 Oct 31.

Institute of Chemical Biology , Guangzhou Institutes of Biomedicine and Health, Chinese Academy of Sciences , #190 Kaiyuan Avenue, Guangzhou 510530, China.

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November 2013

Pyrimido[4,5-d]pyrimidin-4(1H)-one derivatives as selective inhibitors of EGFR threonine790 to methionine790 (T790M) mutants.

Angew Chem Int Ed Engl 2013 Aug 26;52(32):8387-90. Epub 2013 Jun 26.

Institute of Chemical Biology, Guangzhou Institutes of Biomedicine and Health, Chinese Academy of Sciences, 190 Kaiyuan Avenue, Guangzhou 510530, China.

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August 2013

Design, synthesis, and biological evaluation of novel conformationally constrained inhibitors targeting epidermal growth factor receptor threonine⁷⁹⁰ → methionine⁷⁹⁰ mutant.

J Med Chem 2012 Mar 1;55(6):2711-23. Epub 2012 Mar 1.

Key Laboratory of Regenerative Biology and Institute of Chemical Biology, Guangzhou Institutes of Biomedicine and Health, Chinese Academy of Sciences, #190 Kaiyuan Avenue, Guangzhou 510530, China.

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March 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.

Org Lett 2011 Jan 17;13(2):340-3. Epub 2010 Dec 17.

Key Laboratory of Regenerative Biology and Institue of Chemical Biology, Guangzhou Institutes of Biomedicine and Health, Chinese Academy of Sciences, No. 190 Kaiyuan Avenue, Guangzhou Science Park, Guangzhou, 510530, China.

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January 2011