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Discovery of Novel Bicyclic Phenylselenyl-Containing Hybrids: An Orally Bioavailable, Potential and Multi-acting Class of Estrogen Receptor Modulators against Endocrine-Resistant Breast Cancer. Xiangping Deng, Baohua Xie, Qiuzi Li, Yuan Xiao, Zhiye Hu, Xiaofei Deng, Pingping Fang,* Chune Dong,* Hai-Bing Zhou,* and Jian Huang,* J. Med. Chem., 2022, 65 (11), 7993–8010. (IF: 8.039)
Discovery of Aryl Benzoyl Hydrazide Derivatives as Novel Potent Broad-Spectrum Inhibitors of Influenza A Virus RNA Dependent RNA Polymerase (RdRp). Xinjin Liu,† Jinsen Liang,† Yongshi Yu,b,† Xin Han, Lei Yu, Feifei Chen, Zhichao Xu, Qi Chen, Mengyu Jin, Chune Dong, Hai-Bing Zhou*, Ke Lan*, and Shuwen Wu*. J. Med. Chem., 2022, 65 (5), 3814–3832. (IF: 8.039)
ERβ-Targeted Near-Infrared Inherently Fluorescent Probe: A Potent Tool for ERβ Research. Qiuyu Meng#, Baohua Xie#, Huiguang Yu, Kang Shen, Xiangping Deng, Hai-Bing Zhou,* Chune Dong*. ACS Sensors 2022, 7 (1), 109–115. (IF: 9.618)
Estrogen receptor β-targeted hypoxia-responsive near-infrared fluorescence probes for prostate cancer study. Baohua Xie†, Qiuyu Meng†, Huiguang Yu, Kang Shen, Yan Cheng, Chune Dong*, Hai-Bing Zhou*. Eur. J. Med. Chem., 2022, 238, 114506. (IF: 7.088)
Discovery of Oseltamivir-Based Novel PROTACs as Degraders Targeting Neuraminidase to Combat H1N1 Influenza Virus. Zhichao Xu, Xinjin Liu, Xiaoyu Ma, Wenting Zou, Qi Chen, Feifei Chen, Xiaofei Deng, Jinsen Liang, Chune Dong, Ke Lan*, Shuwen Wu* and Hai-Bing Zhou*. Cell Insight 2022, 1 (3), 100030.
Discovery of Aminothiazole Derivatives as Novel Human Enterovirus A71 Capsid Protein Inhibitors. Zhichao Xu,# Qi Tangb,# Ting Xu, Yang Cai, Ping Lei, Yinuo Chen, Wenting Zou, Chune Dong, Ke Lan,* Shuwen Wu* and Hai-Bing Zhou*. Bioorganic Chemistry 2022, 122, 105683. (IF: 5.307)
Rational Design of ERα Targeting Hypoxia Turn-on Fluorescent Probes with Antiproliferative Activity for Breast Cancer. Qiuyu Meng, Baohua Xie, Xiaoyu Ma, Zhiye Hu, Fuling Zhou, Hai-Bing Zhou*, Chune Dong*. Chem. Comm. 2020, 56 (72), 10493-10496. (IF: 5.996)
Identification of Dibucaine Derivatives as Novel Potent Enterovirus 2C Helicase Inhibitors: In Vitro, In Vivo, and Combination Therapy Study. Qi Tang, Zhichao Xu, Mengyu Jin, Ting Shu, Yinuo Chen, Leilei Feng, Qiuhan Zhang, Ke Lan*, Shuwen Wu* and Hai-Bing Zhou*. Eur. J. Med. Chem. 2020, 202, 112310. (IF: 5.572)
Design, synthesis and biological evaluation of novel dual-acting modulators targeting both estrogen receptor a (ERa) and lysinespecific demethylase 1 (LSD1) for treatment of breast cancer. Ming He, Wentao Ning, Zhiye Hu, Jian Huang, Chune Dong*, Hai-Bing Zhou*. Eur. J. Med. Chem. 2020, 195, 112281. (IF: 5.572)
Construction of Benzofuranone Library via Metal-Free, One-Pot Intermolecular Condensation and Their Application as Efficient Estrogen Receptor β Modulators. Xueke Peng, Zhiye Hu, Jing Zhang, Wentao Ning, Silong Zhang, Chune Dong, Xiaodong Shi,* and Hai-Bing Zhou*. Chem. Comm. 2019, 55 (97), 14570–14573. (IF: 5.996)
Novel class of 7-Oxabicyclo[2.2.1]heptene sulfonamides with long alkyl chains displaying improved estrogen receptor a degradation activity. Zhiye Hu, Yuanyuan Li, Baohua Xie, Wentao Ning, Yuan Xiao, Yuan Huang, Chenxi Zhao, Jian Huang*, Chune Dong*, Hai-Bing Zhou*. Eur. J. Med. Chem. 2019, 182, 111605. (IF: 5.572).
Exploring the PROTAC Degron Candidates: OBHSA with Different Side Chains as Novel Selective Estrogen Receptor Degraders (SERDs). Yuanyuan Li, Silong Zhang, Jing Zhang, Zhiye Hu, Yuan Xiao, Jian Huang, Chune Dong,* Shengtang Huang,* and Hai-Bing Zhou*. Eur. J. Med. Chem. 2019, 172, 48-61. (IF: 5.572).
Novel Hybrid Conjugates with Dual Suppression of Estrogenic and Inflammatory Activities Display Significantly Improved Potency against Breast Cancer. Wentao Ning, Zhiye Hu, Chu Tang, Lu Yang, Silong Zhang, Chune Dong, Jian Huang and Hai-Bing Zhou*. J. Med. Chem. 2018, 61 (18), 8155-8173. (IF: 6.253) (Highlighted by Supplementary Cover)
Synthesis and structure-activity relationship study of arylsulfonamides as novel potent H5N1 inhibitors. Yongshi Yu, Qi Tang, Zhichao Xu, Siliang Li, Mengyu Jin, Zixuan Zhao, Chune Dong, Shuwen Wu, Hai-BingZhou*. Eur. J. Med. Chem. 2018, 159, 206-216. (IF: 4.816).
A high-affinity subtype-selective fluorescent probe for estrogen receptor β imaging in living cells. Zhiye Hu, Lu Yang, Wentao Ning, Chu Tang, Qiuyu Meng, Jie Zheng, Chune Dong, and Hai-Bing Zhou*. Chem. Comm. 2018, 54 (31), 3887-3890. (IF: 6.290) (Highlighted by Hot off the Press from Natural Product Reports on 07 Jun 2018)
Estrogen receptor sensing in living cells by a high affinity turn-on fluorescent probe. Lu Yang, Qiuyu Meng, Zhiye Hu, Wentao Ning, Jie Zheng, Chune Dong, Hai-Bing Zhou*. Sensors and Actuators B: Chemical 2018, 272, 589–597. (IF: 5.667).
A novel HDAC6 inhibitor exerts an anti-cancer effect by triggering cell cycle arrest and apoptosis in gastric cancer. Jing Dong, Nan Zheng, Xue Wang, Chu Tang, Ping Yan*, Hai-Bing Zhou*, Jian Huang*. Eur. J. Pharmacol. 2018, 828, 67-79. (IF: 3.040)
Full Antagonism of the Estrogen Receptor without a Prototypical Ligand Side Chain. Sathish Srinivasan, Jerome C. Nwachukwu, Nelson E. Bruno, Venkatasubramanian Dharmarajan, Devrishi Goswami, Irida Kastrati, Scott Novick, Jason Nowak, Valerie Cavett, Hai-Bing Zhou, Nittaya Boonmuen, Yuechao Zhao, Jian Min, Jonna Frasor, Benita S. Katzenellenbogen, Patrick R. Griffin, John A. Katzenellenbogen, Kendall W. Nettles*. Nature Chemical Biology 2017, 13 (1), 111-118. (IF: 13.843)
Recent Advances in Gossypol Derivatives and Analogues: A Chemistry and Biology View. Y. Lu, J. Li, W. Wang,* H.-B. Zhou*. Future Medicinal Chemistry 2017, 9 (11), 1243-1275. (IF: 3.969)
Selenophenes: Introducing a New Element into the Core of Non-Steroidal Estrogen Receptor Ligands. Silong Zhang, Zhiyong Wang, Zhiye Hu, Changhao Li, Chu Tang, Kathryn E. Carlson, Junjie Luo, Chune Dong, John A. Katzenellenbogen, Jian Huang*, Hai-Bing Zhou*. ChemMedChem 2017, 12 (3), 235–249. (IF: 3.009)
Identification and Structure–Activity Relationships of Diarylhydrazides as Novel Potent and Selective Human Enterovirus Inhibitors. Xin Han, Ningyuan Sun, Haoming Wu, Deyin Guo, Po Tien, Chune Dong, Shuwen Wu*, and Hai-Bing Zhou*. J. Med. Chem. 2016, 59 (5), 2139-2150. (IF: 5.589) (Highlighted by BioCentury Innovations (Formerly SciBX, Science-Business eXchange) on March 3, 2016)
Predictive Features of Ligand-Specific Signaling through the Estrogen Receptor. Jerome C. Nwachukwu, Sathish Srinivasan, Yangfan Zheng, Song Wang, Jian Min, Chune Dong, Zongquan Liao, Jason Nowak, Nicholas J. Wright, René Houtman, Kathryn E. Carlson, Jatinder S. Josan, Olivier Elemento, John A. Katzenellenbogen*, Hai-Bing Zhou*, Kendall W. Nettles*. Molecular Systems Biology 2016, 12, 864. (IF: 10.581)
Gossypol with Hydrophobic Linear Esters Exhibits Enhanced Anti-Tumor Activity as an Inhibitor of Antiapoptotic Proteins. Yuzhi Lu, Shuangchan Wu, Yuan Yue, Si He, Jun Li, Jun Tang, Wei Wang,* and Hai-Bing Zhou*. ACS Med. Chem. Lett. 2016, 7 (12), 1185–1190. (IF: 3.746)
Novel Bioactive Hybrid Compounds Dual Targeting Estrogen Receptor and Histone Deacetylase for Treatment of Breast Cancer. Chu Tang, Changhao Li, Silong Zhang, Zhiye Hu, Jun Wu, Chune Dong*, Jian Huang*, and Hai-Bing Zhou*. J. Med. Chem. 2015, 58 (11), 4550-4572. (IF: 5.589)
Tunable Bifunctional Phosphine Squaramide Promoted Morita-Baylis-Hillman Reaction of N-alkyl Isatins with Acrylates. Ze Dong, Chao Yan, Yongzhi Gao, Chune Dong, Guofu Qiu*, Hai-Bing Zhou*. Adv. Synth. Catal. 2015, 357 (9), 2132–2142. (IF: 6.453).
Triaryl-substituted Schiff Bases are High-Affinity Subtype-Selective Ligands for the Estrogen Receptor. Zong-Quan Liao, Chune Dong, Kathryn E. Carlson, Sathish Srinivasan, Jerome C. Nwachukwu, Robert W. Chesnut, Abhishek Sharma, Kendall W. Nettles, John A. Katzenellenbogen,* and Hai-Bing Zhou*. J. Med. Chem. 2014, 57 (8), 3532-3545. (IF: 5.447)
C3-Symmetric Cinchonine-Squaramide-Catalyzed Asymmetric Chlorolactonization of Styrene-Type Carboxylic Acids with 1,3-Dichloro-5,5-dimethylhydantoin: An Efficient Method to Chiral Isochroman-1-ones. Xin Han, Chune Dong, and Hai-Bing Zhou*. Adv. Synth. Catal. 2014, 356 (6), 1275–1280. (IF: 5.663).
Synthesis and SARs of Indole-based α-Amino Acids as Potent HIV-1 Non-Nucleoside Reversed Transcriptase Inhibitors. Xin Han, Haoming Wu, Wei Wang, Chune Dong, Po Tien, Shuwen Wu*, Hai-Bing Zhou*. Org. Biomol. Chem. 2014, 12 (41), 8308 - 8317. (IF: 3.562)
Thiophene-Core Estrogen Receptor Ligands Having Superagonist Activity. Jian Min, Pengcheng Wang, Sathish Srinivasan, Jerome C. Nwachukwu, Pu Guo, Minjian Huang, Kathryn E. Carlson, John A. Katzenellenbogen*, Kendall W. Nettles, Hai-Bing Zhou*. J. Med. Chem. 2013, 56 (8), 3346–3366. (IF: 5.480)
Enantioselective inhibition of reverse transcriptase (RT) of HIV-1 by non-racemic indole-based trifluoropropanoates developed by asymmetric catalysis using recyclable organocatalysts. Xin Han, Wenjie Ouyang, Bin Liu, Wei Wang*, Po Tien, Shuwen Wu*, Hai-Bing Zhou*. Org. Biomol. Chem. 2013, 11 (48), 8463-8475. (IF: 3.487)
Identification and Structure-Activity Relationships of a Novel Series of Estrogen Receptor Ligands Based on 7-Thiabicyclo[2.2.1]hept-2-ene-7-oxide. Pengcheng Wang, Jian Min, Jerome C. Nwachukwu, Valerie Cavett, Kathryn E. Carlson, Pu Guo, Manghong Zhu, Yangfan Zheng, Chune Dong, John A. Katzenellenbogen*, Kendall W. Nettles, Hai-Bing Zhou*. J. Med. Chem. 2012, 55 (5), 2324-2341. (IF: 5.614)
Development of Selective Estrogen Receptor Modulator (SERM)-Like Activity Through an Indirect Mechanism of Estrogen Receptor Antagonism: Defining the Binding Mode of 7-Oxabicyclo[2.2.1]hept-5-ene Scaffold Core Ligands. Yangfan Zheng, Manghong Zhu, Sathish Srinivasan, Jerome C. Nwachukwu, Valerie Cavett, Jian Min, Kathryn E. Carlson, Pengcheng Wang, Chune Dong, John A. Katzenellenbogen*, Kendall W. Nettles, Hai-Bing Zhou*. ChemMedChem 2012, 7 (6), 1094-1100. (IF: 2.835)
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