XU Heng
Principal Investigator
Prof. Xu Heng obtained his B.S. degree in chemistry from Nanjing University in 1998 and his PhD degree from the University of Texas at Arlington in 2005. After postdoctoral research at National Institutes of Health/National Cancer Institute USA, he joined GSK R&D China in 2008, where he worked as a senior scientist on small molecule drug discovery projects in the CNS field. In 2011, he joined PKU Care Pharmaceutical R&D Center as vice president to lead the research efforts in innovative drug discovery and development. In 2015, he started his academic career as a principle investigator at the Institute of Materia Medica and his research interests include small molecule drug design and development; drug discovery based on PROTAC technology; light-controlled drug design and discovery.
1. Design, Synthesis and Biological Evaluation of a Novel Photocaged PI3K Inhibitor toward Precise Cancer Treatment. J. Med. Chem. 2021, 64, 7331-7340.
2. A novel PI3K inhibitor XH30 suppresses orthotopic glioblastoma growth and brain metastasis in mice models. Acta Pharmaceutica Sinica B. https://doi.org/10.1016/j.apsb.2021.05.019.
3. Discovery of New Thieno[2,3-d]pyrimidine and Thiazolo[5,4-d]pyrimidine Derivatives as Orally Active Phosphoinositide 3-Kinase Inhibitors. Bioorg. Med. Chem. 2021, 29, 115890.
4. A novel orally active microtubule destabilizing agent S-40 targets the colchicine-binding site and shows potent antitumor activity. Cancer Lett. 2020, 495, 22-32.
5. Cp*RhIII-catalyzed sulfonamide directed ortho arene C–H carbenoid functionalization with pyridotriazoles. Org. Lett. , 2020, 22, 772-775.
6. CXCR2 antagonism promotes oligodendrocyte precursor cell differentiation and enhances remyelination in a mouse model of multiple sclerosis. Neurobiol. Dis. 2020, 134, 104630.
7. Discovery of 4-Methyl Quinazoline Based PI3K Inhibitors for the Potential Treatment of Idiopathic Pulmonary Fibrosis. J. Med. Chem. 2019, 62, 8873-8879.
8. Design, Synthesis and Biological Evaluation of 4-Methyl Quinazoline Derivatives as Anticancer Agents Simultaneously Targeting Phosphoinositide 3-Kinases and Histone Deacetylases. J. Med. Chem. 2019, 62, 6992-7014.
9. Switching the site-selectivity of C–H activation in aryl sulfonamides containing strongly coordinating N-heterocycles. Chem. Sci. 2019, 10, 8744-8751.
10. Rhodium(III)-catalyzed sulfonamide directed ortho C–H carbenoid functionalization via metal carbene migratory insertion. Chem.Commun. 2019, 55, 2027-2030.
11. Discovery and Optimization of 2-Amino-4-methylquinazoline Derivatives as Highly Potent Phosphatidylinositol 3-kinase Inhibitors for Cancer Treatment. J. Med. Chem. 2018, 61, 6087–6109.
12. Rhodium(III)-catalyzed directed amidation of unactivated C(sp3)–H bonds to afford 1,2-amino alcohol derivatives. Chem.Commun. 2018, 54, 11096-11099.
13. Discovery of new thienopyrimidine derivatives as potent and orally efficacious phosphoinositide 3-kinase inhibitors. Bioorg. Med. Chem. 2018, 26, 637-646.
14. Discovery of CNS Penetrant CXCR2 Antagonists for the Potential Treatment of CNS Demyelinating Disorders. ACS Med. Chem. Lett. 2016, 7, 397-402.
15. Discovery of a novel thienopyrimidine series as highly potent and selective PI3K inhibitors. ACS Med. Chem. Lett. 2015, 6, 434-438.
