出版刊物
Ubiquitin-conjugating enzyme UbcH10 promotes gastric cancer growth and is a potential biomarker for gastric cancer Oncology Reports.,2016, 36(2): 779-86 |
Chemically Diverse Group I p21-Activated Kinase (PAK) Inhibitors Impart Acute Cardiovascular Toxicity with a Narrow Therapeutic Window J. Med. Chem., 2016, 59 (11), 5520–5541. |
Identification of GNE-131: A potent and selective hNaV1.7 inhibitor for the treatment of pain National Medicinal Chemistry Symposium, 2016, Jun. 26-29, Chicago |
Optimization of isoxazoline amide benzoxaboroles for identification of a development candidate as an oral long acting animal ectoparasiticide Bioorganic & Medicinal Chemistry Letters 26 (2016) 3182–3186 |
Identification of Novel EZH2 Inhibitors through Pharmacophore-based Virtual Screening and Biological Assays Bioorganic & Medicinal Chemistry Letters. 2016, 26, 3813–3817 |
Identification of Novel Disruptor of Telomeric Silencing 1-Like (DOT1L) Inhibitors through Structure-Based Virtual Screening and Biological Assays J. Chem. Inf. Model. 2016, 56 (3), 527–534 |
Design and Discovery of new pyrimidine coupled nitrogen aromatic rings as chelating groups of JMJD3 Inhibitor Bioorg Med Chem Lett. 2016, 26(3), 721-725 |
Discovery of novel inhibitors targeting menin-mixed lineage leukemia (MLL) interface using pharmacophore- and docking-based virtual screening Journal of Chemical Information and Modeling. ahead of print |
Fragment-Based Drug Discovery of 2‑Thiazolidinones as BRD4 Inhibitors: 2. Structure-Based Optimization J. Med. Chem. 2015, 58, 1281−1297 |
Mutant IDH is sufficient to initiate enchondromatosis in mice PNAS. ( in process) |
From Ergolines to Indoles: Improved Inhibitors of the Human H3 Receptor for the Treatment of Narcolepsy ChemMedChem. 2015 Feb;10(2):266-75. |
Neuroactive Steroids.1.Positive Allosteric Modulators of the (γ-Aminobutyric Acid)A Receptor: Structure-Activity Relationships of Heterocyclic Substitution at C-21 J. Med. Chem. 2015, 58, 3500-3511. |
人源性胃癌移植瘤模型的建立及其评价 实验动物与比较医学. 34:259-65 |
Discovery of A-971432, An Orally Bioavailable Selective Sphingosine-1-Phosphate Receptor 5 (S1P5) Agonist for the Potential Treatment of Neurodegenerative Disorders J. Med. Chem., 2015, 58 (23), 9154–9170 |
Leveraging the Pre-DFG Residue Thr-406 To Obtain High Kinase Selectivity in an Aminopyrazole-Type PAK1 Inhibitor Series ACS Med. Chem. Lett., 2015, 6 (6), 711–715 |
Design of Selective PAK1 Inhibitor G-5555: Improving Properties by Employing an Unorthodox Low-pK a Polar Moiety ACS Med. Chem. Lett., 2015, 6 (12), 1241–1246. |
SUBSTITUTED BENZAMIDES AND METHODS OF USE THEREOF WO/2015/078374 |
Discovery of imidazo[1,5-a]pyridines and -pyrimidines as potent and selective RORc inverse agonists Bioorganic & Medicinal Chemistry Letters 2015 (25), 2907–2912 |
Neuroactive Steroids.1.Positive Allosteric Modulators of the (γ-Aminobutyric Acid)A Receptor: Structure-Activity Relationships of Heterocyclic Substitution at C-21 J. Med. Chem. 2015, 58, 3500-3511. |
Discovery of an orally bioavailable isoxazoline benzoxaborole (AN8030) as a long acting animal ectoparasiticide Bioorganic & Medicinal Chemistry Letters 25 (2015) 5589–5593 |
Discovery and Optimization of Novel, Selective Histone Methyltransferase SET7 Inhibitors by Pharmacophore- and Docking-Based Virtual Screening J. Med. Chem. 2015, 58, 8166−8181 |
Identifying Novel Selective Non-Nucleoside DNA Methyltransferase 1 Inhibitors through Docking-Based Virtual Screening J. Med. Chem. 2014, 57, 9028−9041 |
Virtual screening and biological evaluation of novel small molecular inhibitors against protein arginine methyltransferase 1 (PRMT1) Org. Biomol. Chem., 2014, 12, 9665–9673 |
Ergoline-derived inverse agonists of the human h3 receptor for the treatment of narcolepsy ChemMedChem. 2014 Aug;9(8):1683-96 |
Establishment and Characterization of 7 Novel Hepatocellular Carcinoma Cell Lines from Patient-Derived Tumor Xenografts Plos One. 9(1): e85308 |
Steric and Electronic Factors Influence Regio-isomeric Thiazole Formations Between Substituted Benzothioamides and Ethyl Bromopyruvate J. Heterocyclic. Chem. 2014, 51, 1137−1146 |
Novel synthesis of isoxazoline indolizine amides for potential application to tropical diseases Tetrahedron Letters, Volume 55, 2014, Pages 1936–1938 |
Vortioxetine disinhibits pyramidal cell function and enhances synaptic plasticity in the rat hippocampus. J Psychopharmacol. 2014 Oct;28(10):891-902. |
Targeted Inhibition of Mutant IDH2 in Leukemia Cells Induces Cellular Differentiation Science,2013, 340(6132),622-6 |
人源性食管癌移植瘤模型的建立、评价及其应用的初步研究 实验动物与比较医学: 33(1) |
HZ08 reverse the aneuploidy-induced cisplatin-resistance in Gastric cancer by modulating the p53 pathway. European Journal of Pharmacology. 720(1-3): 84-97 |
食管癌动物模型的建立 上海师范大学学报(自然科学版). 42(4): 398-404 |
Small Molecule Activation of PKM2 in Cancer Cells Induces Serine Auxotrophy Chem. Biol. 2012, 19(9), 1187-98 |
Intrinsic gemcitabine resistance in a novel pancreatic cancer cell line is associated with cancer stem cell-like phenotype. Int J Oncol. 40 (3): 798-806 |
Identification of NME5 as a contributor to innate resistance to gemcitabine in pancreatic cancer cells. FEBS J. 279(7): 1261-73 |
Transactivation of the human NME5 gene by Sp1 in pancreatic cancer cells. Gene. 503(2): 200-7 |
Full-length human glutaminase in complex with an allosteric inhibitor Biochem. 2011, 50(50), 10764 -70 |
INHIBITORS OF AKT ACTIVITY WO/2011/130921 |
Differential Aspartate Usage Identifies a Subset of Cancer Cells Particularly Cell Reports 17, 876–890, October 11, 2016 |
Discovery of AG-120 (Ivosidenib): A First-in-Class Mutant IDH1 Inhibitor for the Treatment of IDH1 Mutant Cancers ACS Med Chem Lett. 2018 Jan 19;9(4):300-305. |
AG-348 enhances pyruvate kinase activity in red blood cells from patients with pyruvate kinase deficiency Blood. 2017 Sep 14;130(11):1347-1356. |
AG-221, a First-in-Class Therapy Targeting Acute Myeloid Leukemia Harboring Oncogenic IDH2 Mutations Cancer Discov. 2017 May;7(5):478-493. |
Mtb PKNA/PKNB Dual Inhibition Provides Selectivity Advantages for Inhibitor Design To Minimize Host Kinase Interactions ACS Med Chem Lett. 2017 Nov 28;8(12):1224-1229. |
A small molecule activator of Nav1.1 channels increases fast-spiking interneuron excitability and GABAergic transmission in vitro and has anti-convulsive effects in vivo European Journal of Neuroscience, Vol. 46, pp. 1887–1896, 2017 |
First Selective Small Molecule Inhibitor of FGFR4 for the Treatment of Hepatocellular Carcinomas with an Activated FGFR4 Signaling Pathway Cancer Discov. 2015 Apr;5(4):424-37. |
H3B-6527 Is a Potent and Selective Inhibitor of FGFR4 in FGF19-Driven Hepatocellular Carcinoma Cancer Res. 2017 Dec 15;77(24):6999-7013. |
Precision Targeted Therapy with BLU-667 for RET -Driven Cancers “Cancer Discovery (July 1 2018 8 (7) 836-849; DOI:10.1158/2159-8290.CD-18-0338)” |
“Durable tumor regression in genetically altered malignant rhabdoid tumors by inhibition of methyltransferase EZH2” PNAS | May 7, 2013 | vol. 110 | no. 19 | 7923 |
EZH2 inhibition by tazemetostat results in altered dependency on B-cell activation signaling in DLBCL AACR August 23, 2017; DOI: 10.1158/1535-7163.MCT-16-0840 |
Identification of a CARM1 Inhibitor with Potent In Vitro and In Vivo Activity in Preclinical Models of Multiple Myeloma SCIEntIfIC Reports | (2017) 7:17993 | DOI:10.1038/s41598-017-18446-z |
Selective Killing of SMARCA2- and SMARCA4- deficient Small Cell Carcinoma of the Ovary, Hypercalcemic Type Cells by Inhibition of EZH2: In Vitro and In Vivo Preclinical Models AACR Mol Cancer Ther; 16(5) May 2017 |
“Synergistic Anti-Tumor Activity of EZH2 Inhibitors and Glucocorticoid Receptor Agonists in Models of Germinal Center Non-Hodgkin Lymphomas” PLOS ONE| DOI:10.1371/journal.pone.0111840 December 10, 2014 |
Patent Application Publication US 2016/0303135 A1 |
Discovery of the First Potent Inhibitors of Mutant IDH1 That Lower Tumor 2-HG in VivoACS Med. Chem. Lett. 3, 10, 850-855 |
Pyrimidine hydroxyl amide compounds as protein deacetylase inhibitors and methods of use thereof. WO2011307115 |
ANALOGS OF CELASTROL WO2017070615A1 |
“Discovery of A‑971432, An Orally Bioavailable Selective Sphingosine-1-Phosphate Receptor 5 (S1P5) Agonist for the Potential Treatment of Neurodegenerative Disorders” J. Med. Chem. 2015, 58, 9154-9170 |
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一种山环素的制备方法 CN103387511B |
一种3-氯-5,6,7,8-四氢异喹啉的制备方法 201810781489.9 |
一种4-溴甲基-2-三甲基硅乙炔苯基-1-磺酰氟的制备方法 201810781490.1 |
一种5-氨甲基-哌啶-2-酮的制备方法 201810785216.1 |
Mtb PKNA/PKNB Dual Inhibition Provides Selectivity Advantages for Inhibitor Design To Minimize Host Kinase Interactions ACS Med. Chem. Lett. 2017, 8, 1224-1229 |