HUANG Haihong
Principal Investigator
Education
1985−1989 Beijing Normal University, Chemistry, B.S.
1989−1992 Nankai University, Organic Chemistry, M.S.
Professional career
1992−2004 Department of Synthetic Medicinal Chemistry, Institute of Materia Medica. Research Assistant, Assistant and Associate Professor
2009–2010 Department of Chemistry and Biochemistry, University of Delaware. Visiting Scholar
2004–present Department of Synthetic Medicinal Chemistry, Institute of Materia Medica. Professor
Research achievements
As a medicinal chemist with profound new drug research and development experience, Huang Haihong has been in charge of more than 10 new drug projects in different therapeutic areas including rheumatoid arthritis, Mycobacterium Tuberculosis, diabetes, etc., sponsored by the national funds and the Global Alliance for Tuberculosis Drug Development. Her research focus is mainly on the early phase new drug development ranging from new drug design and synthesis, lead optimization, candidate confirmation, preclinical study and clinical development. As a PI, two innovative drugshave been identified and advanced to clinical trials. More than 20 domestic and foreign patents have been granted.
1. Discovery of a Candidate Containing an (S)3,3-Difluoro-1-(4-methylpiperazin-1-yl)-2,3-dihydro1Hinden Scaffold as a Highly Potent Pan-Inhibitor of the BCR-ABL Kinase Including the T315I-Resistant Mutant for the Treatment of Chronic Myeloid Leukemia. J. Med. Chem. , 2021, 64, 7434−7452.
2. Discovery of Novel Thiophene-arylamide Derivatives as DprE1 Inhibitors with Potent Antimycobacterial Activities. J. Med. Chem., 2021, 64, 6241-6261.
3. Identification of Novel Tricyclic Benzo[1,3]oxazinyloxazolidinones as Potent Antibacterial Agents with Excellent Pharmacokinetic Profiles against Drug-Resistant Pathogens. J. Med. Chem., 2021, 64, 3234−3248.
4. The optimization and characterization of functionalized sulfonamides derived from sulfaphenazole against Mycobacterium tuberculosis with reduced CYP 2C9 inhibition. Bioorg. Med. Chem. Lett., 2021, 40, 127924.
5. Discovery of a Conformationally Constrained Oxazolidinone with Improved Safety and Efficacy Profiles for the Treatment of Multidrug-Resistant Tuberculosis. J. Med. Chem., 2020, 63, 9316−9339.
6. The optimization of xanthine derivatives leading to HBK001 hydrochloride as a potent dual ligand targeting DPP-IV and GPR119. Eur. J. Med. Chem., 188(2020) 112017.
7. Efficient and stereoselective one-pot synthesis of benzo[ b ]oxazolo[3,4- d ][1,4]oxazin-1-ones. RSC Adv. , 2020, 10, 24037.
8. Docking- and Pharmacophore-Based Virtual Screening for the Identification of Novel Mycobacterium tuberculosis Protein Tyrosine Phosphatase B (MptpB) Inhibitor with A Thiobarbiturate Scaffold. Bioorganic Chemistry , 2019, 85, 229-239.
9. An efficient and facile access to highly functionalized pyrrole derivatives. Beilstein J. Org. Chem. , 2018, 14, 884-890.
10. Facile and efficient synthesis of quinazoline-2,4(1H,3H)-diones through sequential hydrogenation condensation. Synthetic Communications , 2018, 48(10), 1183-1189.
11. Identification of novel benzothiopyranone compounds against Mycobacterium tuberculosis through scaffold morphing from benzothiazinones. Eur. J. Med. Chem., 2018, 160, 157-170.
12. Discovery of Fluorine-Containing Benzoxazinyl-oxazolidinones for the Treatment of Multidrug Resistant Tuberculosis. ACS Med. Chem. Lett. , 2017, 8, 533-537.
13. Discovery of novel xanthine compounds targeting DPP-IV and GPR119 as anti-diabetic agents. Eur. J. Med. Chem. , 2016, 124, 103-116.
14. A facile and efficient synthesis of 4H-1,3-benzoxazine-4-one with electron-withdrawing group derivatives. Tetrahedron Letters , 2015, 56, 4683-4685.
15. Ti (IV)-catalyzed cascade synthesis of tetrahydrofuro[3,2-d]oxazole from arene-1,4-diones. Org. Biomol. Chem. , 2015，13, 4418-4421.
16. Design, synthesis and evaluation of novel diaryl urea derivatives as potential antitumor agents. Eur. J. Med. Chem. , 2014, 77, 351-360.
17. Design, Synthesis and in vitro Antitumor Evaluation of Novel Diaryl Urea Derivatives Bearing Sulfonamide Moiety. Science China Chemistry, 2013, 56(11), 1564-1572.
18. Iron-catalyzed one-pot synthesis of benzimidazoles from 2-nitroanilines and benzylic alcohols. Tetrahedron Letters, 2013, 54(50), 6934-6936.
19. A facile protocol for N -Cbz protection of amines in PEG-600. Chinese Chemical Letters , 2012, 23, 789-792.
20. Identification of Less Lipophilic Riminophenazine Derivatives for the Treatment of Drug-Resistant Tuberculosis. J. Med. Chem., 2012, 55(19), 8409-8417.
