Jia Zhou, PhD
Department of Pharmacology and Toxicology
Phone: (409) 772-9748
Fax: (409) 772-9648
BSc, 1991, Central China Normal University, Wuhan, China (Chemistry)
MSc, 1994, Nankai University, Tianjin, China (Organic Chemistry)
PhD, 1997, Nankai University, Tianjin, China (Organic Chemistry)
Postdoctoral Fellow, 1999-2001, Department of Chemistry, University of Virginia
Postdoctoral Fellow, 2001-2003, Drug Discovery Program, Georgetown University Medical Center
Residential School on Medicinal Chemistry, 2009, Drew University, Madison, NJ
My research interests are broadly based on the interface of synthetic organic chemistry and medicinal chemistry, and in particular on the drug discovery of bioactive molecules to probe biological systems or act as potential therapeutic agents in neuroscience, cancer/inflammation, infectious diseases, and other human conditions. With this general idea in mind, and in active collaboration with other biologists and pharmacologists, my group is dedicated to establish a strong and creative research program that applies state-of-the-art chemical approaches to biological problems impacting diagnosis, prevention and treatment of human diseases.
One of our current efforts is focused on design and synthesis of small molecules for probing function and development of pharmacological tools for understanding the workings of the brain and that of novel therapies for central nervous system (CNS) disorders such as drug abuse and addiction, depression, schizophrenia, pain, and neurodegenerative diseases. The proposed projects in this area include the identification, characterization and optimization of allosteric modulators, bitopic ligands, and inverse agonists of 5-HT2C receptor, neuromedin U receptor 2 (NMUR2) ligands, as well as AMPA receptor positive allosteric modulators for preventing neuroapoptosis and opioid use disorder pharmacotherapy. We are also working on the discovery of dopamine D1 biased ligands, orphan GPCR (oGPCR) including GPR52 ligands, DeltaFosB inhibitors, neurexin modulators, and FGF14/Nav1.6 channel complex protein-protein interaction inhibitors as CNS probes and potential therapeutics.Another line of research development centers on the establishment of novel chemical libraries aiming at mechanism-based or lead compound-based drug discovery for cancer/inflammation, particularly by targeting Bcl-2 family proteins and apoptosis pathways, transcription factors as well as epigenetic therapy with the aid of molecular docking and chemical synthesis. Specifically, we are developing Bax activators, BH4 domain antagonists of Bcl2, Survivin inhibitors, orally bioavailable STAT3 inhibitors, glycolysis inhibitors, AP-1 inhibitors, KLF5 inhibitors, KRAS plasma membrane localization inhibitors, cystathionine-β-synthase (CBS) inhibitors, SIRT6 activators, TRIM28 inhibitors, CDK9 inhibitors, MYC inhibitors, PRMT5 inhibitors, BRD4 inhibitors and relevant protein degraders as a new class of preventive/therapeutic agents for various human cancers including brain tumors, breast cancer, lung cancer, head/neck cancer, colorectal cancer, gastric cancer, prostate cancer, and pancreatic cancer as well as inflammation (e.g. airway remodeling and inflammatory bowel diseases).
Our research efforts on developing chemical probes include design and synthesis of small molecules targeting EPAC, which are exchange proteins directly activated by cAMP including cAMP-regulated guanine nucleotide exchange factors. These EPAC inhibitors together with other mechanism-based therapeutics have also demonstrated as promising therapeutics for a variety of indications including infectious diseases. Utilizing structure-based and fragment-based drug design by collaborating with viral research biologists, we are developing novel small molecules as therapeutic candidates targeting viral proteins such as dengue viral NS4B, flavivirus NS2B-NS3 protease and RNA-dependent RNA polymerase (RdRp). Meanwhile, we are also developing novel target-based small molecules as therapeutics to epigenetically silencing HIV or latency reversing agents for HIV eradication or HIV/TB co-infection. Last but not least, we are also working on natural product-inspired diversity-oriented synthesis that may lead to exciting potentials for discovery of novel targets and drug candidates.
- E. A. Wold, E. J. Garcia, C. T. Wild, J. M. Miszkiel, C. A. Soto, J. Chen, K. Pazdrak, R. G. Fox, N. C. Anastasio, K. A. Cunningham, J. Zhou. Discovery of 4-Phenylpiperidine-2-Carboxamide Analogues as Serotonin 5-HT2C Receptor Positive Allosteric Modulators with Enhanced Drug-Like Properties. J. Med. Chem. 2020, In press. DOI: 10.1021/acs.jmedchem.9b01953. PMID: 32567857
- Z. Liu, H. Chen, P. Wang, Y. Li, E. A. Wold, P. G. Leonard, S. Joseph, A. R. Brasier, B. Tian, J. Zhou. Discovery of Orally Bioavailable Chromone Derivatives as Potent and Selective BRD4 Inhibitors: Scaffolding Hopping, Optimization and Pharmacological Evaluation. J. Med. Chem. 2020, 63 (10), 5242-5256. PMID: 32255647. [Journal Cover Article]
- Y. Li, Z. Liu, G. Aglyamova, J. Chen, H. Chen, M. Bhandari, M. A. White, G. Rudenko, J. Zhou. Discovery of phenanthridine analogues as novel chemical probes disrupting the binding of DNA to ΔFosB homodimers and ΔFosB/JunD heterodimers. Bioorg. Med. Chem. Lett., 2020, 30 (16), 127300. https://doi.org/10.1016/j.bmcl.2020.127300.
- P. Wang, U. Luchowska-Stańska, H. Chen, Z. Liu, J. Wiejak, P. Whelan, D. Morgan, E. Lochhead, G. Barker, H. Rehmann, S. J. Yarwood, J. Zhou. Synthesis and Biochemical Evaluation of Non-Cyclic Nucleotide Exchange Protein Directly Activated by cAMP1 (EPAC1) Regulators. J. Med. Chem. 2020, 63 (10), 5159-5184. PMID: 32340447.
- J. Xu, J. Berastegui-Cabrera, H. Chen, J. Pachón-Díaz, J. Zhou* (Co-Corresponding author), Javier Sánchez-Céspedes. Structure-Activity Relationship Studies on Diversified Salicylamide Derivatives as Potent Inhibitors of Human Adenovirus Infection. J. Med. Chem. 2020, 63 (6), 3142-3160. PMID: 32045239. [Journal Cover Article]
- J. Xu, P.-Y. Shi, H. Li, J. Zhou. Broad Spectrum Antiviral Agent Niclosamide and Its Therapeutic Potential. ACS Infectious Diseases, 2020, 6 (5), 909-915. PMID: 32125140. PMCID: PMC7098069.
- H. Shao, H. Mohamed, S. Boulton, J. Huang, P. Wang, H. Chen, J. Zhou, U. Luchowska-Stańska, N. Jentsch, A. Armstrong, J. Magolan, S. Yarwood; G. Melacini. Mechanism of Action of an EPAC1-Selective Competitive Partial Agonist. J. Med. Chem. 2020, 63 (9), 4762-4775. PMID: 32297742.
- A. R. Brasier*, J. Zhou*. Validation of the epigenetic reader bromodomain-containing protein 4 (BRD4) as a therapeutic target for treatment of airway remodeling. Drug Discov. Today, 2020, 25 (1), 126-132. PMID: 31733396. PMCID: PMC6980722.
- J. Xu, X. Xie, H. Chen, J. Zou, Y. Xue, N. Ye, P.Y. Shi, J. Zhou. Design, synthesis and biological evaluation of spiropyrazolopyridone derivatives as potent dengue virus inhibitors. Bioorg. Med. Chem. Lett., 2020, 30 (11), 127162. PMID: 32247736.
- C. T. Wild, J. M. Miszkiel, E. A. Wold, C. A. Soto, C. Ding, R. M. Hartley, M. A. White, N. C. Anastasio, K. A. Cunningham, and J. Zhou. Design, Synthesis and Characterization of 4-Undecylpiperidine-2-Carboxamides as Positive Allosteric Modulators of the Serotonin (5-HT) 5-HT2C Receptor. J. Med. Chem. 2019, 62 (1), 288-305. PMID: 29620897. [Paper of a Special Issue on Allosteric Modulators of Drug Targets]
- E. A. Wold, C. Wild, K. A. Cunningham, J. Zhou. Targeting the 5-HT2C Receptor in Biological Context and the Current State of 5-HT2C Receptor Ligand Development. Curr. Top. Med. Chem., 2019, 19 (16), 1381-1398. PMID: 31288724.
- N. Ye, Q. Xu, W. Li, P. Wang, J. Zhou. Recent Advances in Developing K-Ras Plasma Membrane Localization Inhibitors. Curr. Top. Med. Chem. 2019, 19 (23), 2114-2127. PMID: 31475899.
- J. Xu, X. Xie, N. Ye, J. Zou, H. Chen, M. A. White, P. Y. Shi, J. Zhou. Design, Synthesis, and Biological Evaluation of Substituted 4,6-Dihydrospiro[[1,2,3]triazolo[4,5-b]pyridine-7,3'-indoline]-2',5(3H)-dione Analogues as Potent NS4B Inhibitors for the Treatment of Dengue Virus Infection. J. Med. Chem., 2019, 62 (17):7941-7960. PMID: 31403780.
- P. Wang, D. E. Felsing, H. Chen, S. R. Raval, J. A. Allen, J. Zhou. Synthesis and Pharmacological Evaluation of Non-catechol G Protein Biased and Unbiased Dopamine D1 Receptor Agonists. ACS Med. Chem. Lett., 2019, 10 (5), 792-799. PMCID: PMC6511950. [Cover paper of the journal; F1000Prime Recommended Article].
- Q. Niu, Z. Liu, F. Liu, E. Alamer, X. Fan, H. Chen, J. Endsley, B. B. Gelman, B. Tian, J. H. Kim, N. L. Michael, M. L. Robb, J. Ananworanich, J. Zhou* (Co-Corresponding author), H. Hu*. Structure-guided drug design identifies a BRD4-selective small molecule that suppresses HIV. J. Clin. Investig. (JCI), 2019, 129 (8), 3361-3373. PMID: 31329163.
- B. Tian, K. Hosoki, Z. Liu, J. Yang, Y. Zhao, H. Sun, J. Zhou, E. Rytting, L. Kaphalia, W. J Calhoun, S. Sur, A. R Brasier. Mucosal Bromodomain-Containing Protein 4 (BRD4) Regulates Aeroallergen-induced Airway Remodeling and Sensitization. J. Allergy Clin. Immunol., 2019, 143 (4), 1380-1394.e9. PMID: 30321559.
- G. Liu, T. Yin, H. Kim, C. Ding, Z. Yu, H. Wang, H. Chen, R. Yan, E. A. Wold, H. Zou, X. Liu, Y. Ding, Q. Shen, J. Zhou. Structure-Activity Relationship Studies on Bax Activator SMBA1 for the Treatment of ER-Positive and Triple-Negative Breast Cancer. Eur. J. Med. Chem., 2019, 178, 589-605. PMID: 31220676.
- J. Xu, M. E., Pachón-Ibáñez, T. Cebrero-Cangueiro, H. Chen, J. Sánchez-Céspedes, J. Zhou. Discovery of niclosamide and its O-alkylamino-tethered derivatives as potent antibacterial agents against carbapenemase-producing and/or colistin resistant Enterobacteriaceae isolates. Bioorg. Med. Chem. Lett., 2019, 29 (11), 1399-1402. PMID: 30954430.
- B. Tian, Z. Liu, J. Litvinov, R. Maroto, M. Jamaluddin, E. Rytting, I. Patrikeev, L. Ochoa, G. Vargas, M. Motamedi, B. T. Ameredes, J. Zhou, A. R Brasier. Efficacy of Novel Highly Specific Bromodomain-Containing Protein 4 (BRD4) Inhibitors in Innate Inflammation-Driven Airway Remodeling. Am. J. Respir. Cell Mol. Biol. 2019, 60 (1), 68-83. PMID: 30153047.
- J. Zhou*(Co-Corresponding author), K. A. Cunningham*. Positive Allosteric Modulation of the 5-HT2C Receptor: Implications for Neuropsychopharmacology and Neurotherapeutics. Neuropsychopharmacology, 2019, 44 (1), 230-231. PMID: 30202047. PMCID: PMC6235849
- N. Ye, B. Li, Q. Mao, E. A. Wold, S. Tian, J. A. Allen, J. Zhou. Orphan Receptor GPR88 as an Emerging Neurotherapeutic Target. ACS Chem. Neurosci., 2019, 10 (1), 190-200. PMID: 30540906.
- Z. Liu, P.Wadsworth, A. K. Singh, H. Chen, P. Wang, O. Folorunso, P. Scaduto, S. R. Ali, F. Laezza, J. Zhou. Identification of Peptidomimetics as Novel Chemical Probes Modulating Fibroblast Growth Factor 14 (FGF14) and Voltage-Gated Sodium Channel 1.6 (Nav1.6) Protein-Protein Interactions. Bioorg. Med. Chem. Lett. 2019, 29 (3), 413-419. PMID: 30587448.
- E. A. Wold, J. Chen, K. A. Cunningham, J. Zhou. Allosteric Modulation of Class A GPCRs: Targets, Agents, and Emerging Concepts. J. Med. Chem., 2019, 62 (1), 88-127. PMID: 30106578. [Paper of a Special Issue on Allosteric Modulators of Drug Targets]
- E. A. Wold, J. Zhou. GPCR Allosteric Modulators: Mechanistic Advantages and Therapeutic Applications. Curr. Top. Med. Chem., 2018, 18 (23), 2002-2006. PMID: 30621563.
- P. Wang, J. Zhou. Proteolysis Targeting Chimera (PROTAC): A Paradigm-Shifting Approach in Small Molecule Drug Discovery. Curr. Top. Med. Chem. 2018, 18 (16):1354-1356. PMID: 30306871.
- B. Tian, Z. Liu, J. Yang, H. Sun, Y. Zhao, M. Wakamiya, H. Chen, E. Rytting, J. Zhou*(Co-Senior author), A. R Brasier. Selective Antagonists of the Epithelial NFκB-Bromodomain-Containing Protein 4 (BRD4) Pathway in Viral-Induced Airway Inflammation. Cell Rep., 2018, 23, 1138-1151. PMID: 29694891.
- X. Hu, X. Tian, H. Chen, J. Zhou, Z. J. Wang. AMPA Positive Allosteric Modulators Attenuate Opioid Tolerance and Dependence. Neuropharmacology, 2018, 137, 50-58. PMID: 29751227.
- Y. Ding, D. Li, C. Ding, Z. Liu, E. A. Wold, P. Wang, N. Ye, H. Chen, M. A. White, Q. Shen, J. Zhou. Regio- and Stereospecific Synthesis of Oridonin D-ring Aziridinated Analogues for the Treatment of Triple-Negative Breast Cancer via Mediated Irreversible Covalent Warheads. J. Med. Chem., 2018, 61 (7), 2737-2752. PMID: 29528645.
- Z. Liu, B. Tian, H.Y. Chen, P. Wang, A. R. Brasier, J. Zhou. Discovery of Potent and Selective BRD4 Inhibitors Capable of Blocking TLR3-Induced Acute Airway Inflammation. Eur. J. Med. Chem., 2018, 151, 450-461. PMID: 29649741.
- D. Li, H. Wang, Y. Ding, Z. Zhang, Z. Zheng, J. Dong, H. Kim, X. Meng, Q. Zhou, J. Zhou*(Co-Corresponding author), L. Fang*, Q. Shen*. Targeting the NRF-2/RHOA/ROCK signaling pathway with a novel aziridonin, YD0514, to suppress breast cancer progression and lung metastasis. Cancer Lett. 2018, 424, 97-108. PMID: 29580806.
- J. Levesley, L. Steele, A. Brüning-Richardson, A. Davison, J. Zhou, C. Ding, S. Lawler, S. C. Short. Selective BCL-XL inhibition promotes apoptosis in combination with MLN8237 in medulloblastoma and pediatric glioblastoma cells. Neuro Oncol. 2018, 20 (2), 203-214. PMID: 29016820.
- S. R. Ali, Z. Liu, M. N. Nenov, O. Folorunso, A. Singh, F. Scala, H.Y. Chen, T. F. James, M. Alshammari, N. I. Panova-Elektronova, M. A. White, J. Zhou*(Co-Corresponding author), F. Laezza. Functional modulation of voltage-gated sodium channels by a FGF14-based peptidomimetic. ACS Chem. Neurosci., 2018, 9 (5), 976-987. PMID: 29359916.
- J. Xu, E. A. Wold, Y. Ding, Q. Shen, J. Zhou. Therapeutic Potential of Oridonin and Its Analogs: From Anticancer and Antiinflammation to Neuroprotection. Molecules, 2018, 23 (2), 474. PMID: 29470395.
- Z. Liu, Y. Zhu, H. Y. Chen, P. Y. Wang, F. C. Mei, N. Ye, X. Cheng, J. Zhou. Structure-activity relationships of 2-substituted phenyl-N-phenyl-2-oxoacetohydrazonoyl cyanides as novel antagonists of exchange proteins directly activated by cAMP (EPACs). Bioorg. Med. Chem. Lett. 2017, 27 (23), 5163-5166. PMID: 29100797. PMCID: PMC5693616.
- Y. Wang, S. Wang, Y. Wu, Y. Ren, Z. Li, X. Yao, C. Zhang, N. Ye, C. Jing, J. Dong, S. Sun, M. Zhao, W. Guo, X. Qu, Y. Qiao, H. Y. Chen, L. Kong, R. Jin, X. Wang, L. Zhang, J. Zhou*(Co-Corresponding author), Q. Shen*, X. Zhou*. Suppression of the Growth and Invasion of Human Head and Neck Squamous Cell Carcinomas via Regulating STAT3 Signaling and miR-21/β-catenin Axis with HJC0152. Mol. Cancer Ther., 2017, 16 (4), 578-590. PMID: 28138036. PMCID: PMC5380531.
- R. Li, C. Ding, J. Zhang, M. Xie, D. Park, Y. Ding, G. Chen, T. K. Owonikoko, G. Zhang, M. Gilbert-Ross, S. Sun, Z. G. Chen, G. L. Sica, S. S. Ramalingam, A. T. Magis, D. M. Shin, J. Zhou*(Co-Corresponding author), X. Deng. Modulation of Bax and mTOR in cancer therapeutics. Cancer Res., 2017, 77 (11), 3001-3012. PMCID: PMC5503158.
- Z. Li, M. Brecher, J. Zhang, S. Sakamuru, B. Liu, R. Huang, C. Koetzner, S. Jones, F. Gao, N. Banavali, L. Kramer, C. Allen, N. Boles, Y. Deng, C. Qin, H.Y. Chen, J. Zhou, Q. Lin, N. Zhang, M. Tian, H. Li. Existing drugs as broad spectrum and potent inhibitors for Zika virus by targeting NS2B-NS3 interaction. Cell Res., 2017, 27(8), 1046-1064. PMCID: PMC5539352.
- Z. Chen, Q. Wu, Y. Ding, W. Zhou, R. Liu, H. Chen, J. Zhou*(Co-Corresponding author), J. Feng*, C. Chen*. YD277 Suppresses Triple-Negative Breast Cancer Partially Through Activating the Endoplasmic Reticulum Stress Pathway. Theranostics, 2017; 7 (8), 2339-2349. PMCID: PMC5505065.
- Z. Liu, P. Wang, H. Chen, E. A. Wold, B. Tian, A. R. Brasier, J. Zhou. Drug Discovery Targeting Bromodomain-Containing Protein 4 (BRD4). J. Med. Chem., 2017, 60 (11), 4533-4558. PMID: 28195723. PMCID: PMC5464988.
- J.C. Zhou, E.J. Yun, W. Chen, Y. Ding, K. Wu, B. Wang, C. Ding, E. Hernandez, J. Santoyo, R. Pong, H. Y. Chen, D. He, J. Zhou*(Co-Corresponding author), J.T. Hsieh. Targeting 3-phosphoinositide-dependent protein kinase 1 associated with drug resistant mechanism in renal cell carcinoma with new Oridonin analogues. Cell Death and Disease, 2017, 8, e2701; doi:10.1038/cddis.2017.121. PMCID: PMC5386527.
- N. Ye, Y. Zhu, Z. Liu, F. C. Mei, H. Chen, P. Wang, X. Cheng, J. Zhou. Identification of novel 2-(benzo[d]isoxazol-3-yl)-2-oxo-N-phenylacetohydrazonoyl cyanide analogues as potent EPAC antagonists. Eur. J. Med. Chem., 2017, 134, 62-71. PMCID: PMC5492227.
- P. Wang, Z. Liu, H. Chen, N. Ye, X. Cheng, J. Zhou. Exchange proteins directly activated by cAMP (EPACs): Emerging therapeutic targets. Bioorg. Med. Chem. Lett., 2017, 27 (8), 1633-1639. PMCID: PMC5397994. [Cover paper of the journal].
- C. Wild, Y. Zhu, N. Ye, F. Mei, M. A. Ynalvez, H. Chen, X. Cheng, J. Zhou. Functionalized N,N-Biarylamines as Potent and Selective EPAC2 Inhibitors. ACS Med. Chem. Lett., 2016, 7 (5), 460-4. PMID: 27190593. PMCID: PMC4867506.
- O. N. Lopez, F. J. Bohanon, X. Wang, T. Corsello, N. Ye, Y. Rojas-Khalil, H.J. Chen, H.Y. Chen, J. Zhou*(Co-Corresponding author), R. S. Radhakrishnan. STAT3 Inhibition Suppresses Hepatic Stellate Cells Fibrogenesis: HJC0123, a Potential Therapeutic Agent for Liver Fibrosis. RSC Adv., 2016, 6, 100652-100663.
- W. Chen, J.C. Zhou, K. Wu, J. Huang, Y. Ding, E.J. Yun, B. Wang, C. Ding, E. Hernandez, J. Santoyo, H.Y. Chen, H. Lin, D. He, J. Zhou*(Co-Corresponding author), J.T. Hsieh. Targeting new regulatory mechanism of XBP1-mediated β-catenin expression associated with bladder cancer with newly synthetic Oridonin analogues. Oncotarget, 2016, 7 (35), 56842-56854. PMID: 27472396.
- Y. Ding, C. Ding, N. Ye, Z. Liu, E. A. Wold, H. Chen, C. Wild, Q. Shen, J. Zhou. Discovery and Development of Natural Product Oridonin-Inspired Anticancer Agents. Eur. J. Med. Chem., 2016, 122, 102-117. PMID: 27344488. PMCID: PMC5003635.
- J. S. Rudra, Y. Ding, H. Neelakantan, C. Ding, R. Appavu, S. J. Stutz, J. D. Snook, H.Y. Chen, K. A. Cunningham, J. Zhou. Suppression of Cocaine-evoked Hyperactivity by Self-adjuvanting and Multivalent Peptide Nanofiber Vaccines. ACS Chem. Neurosci., 2016, 7 (5), 546−552. PMID: 26926328. PMCID: PMC4871789.
- N. Ye, H. Y. Chen, E. A. Wold, P.Y. Shi, J. Zhou. Therapeutic Potential of Spirooxindoles as Antiviral Agents. ACS Infectious Diseases, 2016, 2 (6), 382-392.
- C. Chao, J. R. Zatarain, Y. Ding, C. Coletta, A. A. Mrazek, N., Druzhyna, P. Johnson, H.Y. Chen, J. L. Hellmich, A. Asimakopoulou, K. Yanagi, G. Olah, P. Szoleczky, G. Törö, F. J. Bohanon, M. Cheema, R. Lewis, D. Eckelbarger, A. Ahmad, K. Módis, A. Untereiner, B. Szczesny, A. Papapetropoulos, J. Zhou*(Co-Corresponding author), M. R. Hellmich, C. Szabo. Cystathionine-beta-synthase inhibition for colon cancer: Enhancement of the efficacy of aminooxyacetic acid via the prodrug approach. Mol. Med. 2016, 22, 361-379. PMID: 27257787.
- H.J. Chen, J. Wu, Y. Gao, H.Y. Chen, J. Zhou. Scaffold Repurposing of Old Drugs Towards New Cancer Drug Discovery. Curr. Top. Med. Chem., 2016, 16 (19), 2107-2114. PMID: 26881709.
- Z. Liu, Y. Ding, N. Ye, C. Wild, H.Y. Chen, J. Zhou. Direct Activation of Bax Protein for Cancer Therapy. Med. Res. Rev. 2016, 36 (2), 313-341. PMID: 26395559
- Z. Liu, C. Wild, Y. Ding, N. Ye, H.Y. Chen, E. A. Wold, J. Zhou. BH4 domain of Bcl-2 as a novel target for cancer therapy. Drug Discov. Today, 2016, 21 (6), 989-996. PMCID: PMC4882289
- N. Ye, Y. Zhu, H.J. Chen, Z. Liu, F. C. Mei, C. Wild, H.Y. Chen, X. Cheng, and J. Zhou. Structure-Activity Relationship Studies of Substituted 2-(Isoxazol-3-yl)-2-Oxo-N'-Phenyl-Acetohydrazonoyl Cyanide Analogues: Identification of Potent Exchange Proteins Directly Activated by cAMP (EPAC) Antagonists. J. Med. Chem., 2015, 58 (15), 6033-6047.
- B. Han, D. Park, R. Li, M. Xie, T. Owonikoko, G. Sica, C. Ding, J. Zhou, A. Magis, S. Ramalingam, F. Khuri, W. Curran, X. Deng. Bcl2 BH4 Antagonist for Lung Cancer Therapeutics. Cancer Cell, 2015, 27 (6), 852-863.
- C. Ding, L. Wang, H. Chen, C. Wild, N. Ye, Y. Ding, T. Wang, M. A. White, Q. Shen, J. Zhou. ent-Kaurane-Based Regio- and Stereoselective Inverse Electron Demand Hetero-Diels-Alder Reactions: Synthesis of Dihydropyran-Fused Diterpenoids. Org. Biomol. Chem. 2014, 12 (42), 8442-8452.
- M. Xin, R. Li, D. Park, M. Xie, T. K. Owonikoko, G. L. Sica, P. E. Corsino, J. Zhou, C. Ding, M. A. White, A. T. Magis, S. S. Ramalingam, W. J. Curran, F. R. Khuri, X. Deng, Small Molecule Bax Agonists for Cancer Therapy. Nature Communications, 2014, 5, 4935. DOI: 10.1038/ncomms5935.
- C. Ding, Y. Zhang, H. Chen, Z. Yang, C. Wild, C. D. Ester, A. Xiong, M. A. White, Q. Shen, J. Zhou. Oridonin Ring A-Based Diverse Constructions of Enone Functionality: Identification of Dienone Analogues Effective for Highly Aggressive Breast Cancer by Inducing Apoptosis. J. Med. Chem. 2013, 56 (21), 8814-8825.
- H. Chen, T. Tsalkova, O. G. Chepurny, F. C. Mei, G. G. Holz, X. Cheng, J. Zhou, Identification and Characterization of Small Molecules as Potent and Specific Epac2 Antagonists, J. Med. Chem., 2013, 56 (3), 952-962.
- C. Ding, Y. Zhang, H. Chen, C. Wild, T. Wang, M. White, Q. Shen, J. Zhou. Overcoming Synthetic Challenges of Oridonin A-Ring Structural Diversification: Regio- and Stereoselective Installation of Azides and 1,2,3-Triazoles at the C-1, C-2, or C-3 Position. Org. Lett., 2013, 15 (14), 3718-3721.
- C. Ding, Y. Zhang, H. Chen, L. Chu, Z. Yang, C. Wild, H. Liu, Q. Shen, J. Zhou. Novel Nitrogen-Enriched Oridonin Analogs with Thiazole-Fused A-Ring: Protecting Group-Free Synthesis, Enhanced Anticancer Profile, and Improved Aqueous Solubility. J. Med. Chem. 2013, 56 (12), 5048-5058.
- C. Ding, N. M. Bremer, T. D. Smith, P. K. Seitz, N. C. Anastasio, K. A. Cunningham, J. Zhou.
Exploration of Synthetic Approaches and Pharmacological Evaluation of
PNU-69176E and Its Stereoisomer as 5-HT2C Receptor Allosteric
Modulators. ACS Chem. Neurosci., 2012, 3 (7), 538-545.