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成果及论文

In Zhejiang University

2023

1. Xin Han#, Weiguo Xiang#, Lijie Zhao#, Mi Wang#, Bukeyan Miao, Chong Qin, Donna McEachern, Jianfeng Lu, Yu Wang, Hoda Metwally, Paul Kirchhoff, Lu Wang, Aleksas Matvekas, John Takyi-Williams, Bo Wen, Duxin Sun, Mark Ator, Robert Mckean, Shaomeng Wang*.  Discovery of ARD-2051 as a Potent and Orally Efficacious PROTAC Degrader of Androgen Receptor (AR) for the Treatment of Advanced Prostate Cancer. J. Med. Chem.2023, minor revision.

2. Xin Han*, Yi Sun*. PROTACs: A novel strategy for cancer drug discovery and development. MedComm 2023, minor revision. (*Co-Corresponding Author)

2022

1. Xiaojuan Jia, Xin Han*. Targeting Androgen Receptor Degradation with PROTACs from Bench to Bedside. Biomed Pharmacother 2022158, 114112.

2. Xin Han*, Yi Sun*. Strategies for the discovery of oral PROTAC degraders aimed at cancer therapy. Cell Reports Physical Science 20223, 101062. (*Co-Corresponding Author)

3. Xin Han*, Wenyi Wei, Yi Sun*PROTAC Degraders with Ligands Recruiting MDM2 E3 Ubiquitin Ligase: An Updated Perspective. Acta Materia Medica 20221 (2), 244-259. (*Co-Corresponding Author)

4. Xinjin Liu, Jinsen Liang, Yongshi Yu, Xin Han, Lei Yu, Feifei Chen, Zhichao xu, Qi Chen, Mengyu Jin, Chune Dong, Hai-Bing Zhou, Ke Lan, Shuwen Wu. Discovery of Aryl Benzoyl Hydrazide Derivatives as Novel Potent Broad-Spectrum Inhibitors of Influenza A Virus RNA Dependent RNA Polymerase (RdRp). J. Med. Chem., 202265, 3814-3832.

5. Weiguo Xiang, Xin Han, Lijie Zhao, and Shaomeng Wang. Recent advances in targeting the androgen receptor with PTOTACs. ACS Medicinal Chemistry Reviews202257, 295-317.


Before Zhejiang University

1.       Weiguo Xiang#, Lijie Zhao#Xin Han#, Chong Qin, Bukeyan Miao, Donna McEachern, Yu Wang, Hoda Metwally, Lu Wang, Aleksas Matvekas, Bo Wen, Duxin Sun, Shaomeng WangARD-2585 as an Exceptionally Potent and Orally Active PROTAC Degrader of Androgen Receptor (AR) for the Treatment of Advanced Prostate Cancer. J. Med. Chem., 202164, 13487-13509. (#Co-First Author, Most Read ArticlesFaculty Opinions (F1000Prime)推荐)

2.       Xin Han#, Lijie Zhao#, Weiguo Xiang#, Chong Qin, Bukeyan Miao, Donna McEachern, Yu Wang, Hoda Metwally, Lu Wang, Aleksas Matvekas, Bo Wen, Duxin Sun, Shaomeng WangStrategies toward Discovery of Potent and Orally Bioavailable PROTAC Degraders of Androgen Receptor (AR) for the Treatment of Advanced Prostate Cancer. J. Med. Chem., 202164, 12831-12854. (#Co-First Author)

3.       Jiantao Hu#, Biao Hu#, Fuming Xu#, Mi Wang#Xin Han#, Chao-Yie Yang, Jeanne Stuckey and Shaomeng Wang*. J. Med. Chem.2022, under review. (#Co-First Author)

4.       Xin Han#, Lijie Zhao#, Weiguo Xiang, Chong Qin, Bukeyan Miao, Tianfeng Xu, Mi Wang, Chao-Yie Yang, Krishnapriya Chinnaswamy, Jeanne Stuckey, Shaomeng Wang*. Discovery of Highly Potent and Efficient PROTAC Degraders of Androgen Receptor (AR) by Employing Weak Binding Affinity VHL E3 Ligase Ligands. J. Med. Chem.201962, 11218-11231. (#Co-First Author, Most Read ArticlesFaculty Opinions (F1000Prime)推荐)

5.       Xin Han#, Chao Wang#, Chong Qin#, Weiguo Xiang#, Ester Fernandez-Salas, Chao-Yie Yang, Mi Wang, Lijie Zhao, Tiangfeng Xu, Krishnapriya Chinnaswamy, James Delproposto, Jeanne Stuckey, Shaomeng Wang*Discovery of ARD-69 as a Highly Potent Proteolysis Targeting Chimera (PROTAC) Degrader of Androgen Receptor (AR) for the Treatment of Prostate CancerJ. Med. Chem.201962, 941-964. (#Co-First Author, Most Read Articles, ESI高被引论文)

6.       Xin Han, Ningyuan Sun, Haoming Wu, Deyin Guo, Po Tien, Chune Dong, Shuwen Wu*, Hai-Bing Zhou*. Identification and Structure-Activity Relationships of Diarylhydrazides as Novel Potent and Selective Human Enterovirus InhibitorsJ. Med. Chem.201659, 2139-2150.

7.       Lijie Zhao#Xin Han#, Jianfeng Lu, Donna McEachern and Shaomeng Wang*. Induced AR Degradation as a Therapeutic Strategy in AR-positive Breast Cancer. Neoplasia, 202022, 522-532. (#Co-First Author, Highlight论文)

8.       Steven Kregel#, Chao Wang#Xin Han#, Lanbo Xiao, Ester Fernandez-Salas, Pushpinder Bawa, Ingrid Apel, Brooke L. McCollum, Kari Wilder-Romans, Xuhong Cao, Corey Speers, Shaomeng Wang*, Arul M. Chinnaiyan*. Androgen Receptor Degraders Overcome Common Resistance Mechanisms Developed During Prostate Cancer Treatment. Neoplasia202022, 111-119. (#Co-First Author, ESI高被引论文)

9.    Tazeem#Xin Han#, Qingjun Zhou, Jingchen Wei, Po Tien, Guichun Yang, Shuwen Wu* Chune Dong*. A facile one-pot multi-component synthesis of novel adamantine substituted imidazo[1,2-a] pyridine derivatives: identification and structure– activity relationship study of their anti-HIV-1 activity. RSC Adv., 20166, 95177-95188 (#Co-First Author).

10.    Xin HanHai-Bing Zhou, Chune Dong*. Applications of Chiral Squaramides: From Asymmetric Organocatalysis to Biologically Active Compounds. Chem. Rec.201616, 897-906.

11.    Jiawei Pan#Xin Han #, Ningyang Sun, Haoming Wu, DandanLin, Po Tien, Hai-Bing Zhou*, Shuwen Wu*. Synthesis of N-benzyl-N-phenylthiophene-2-carboxamide Analogues as a Novel Class of Enterovirus 71 Inhibitors. RSC Adv, 20155, 55100-55108 (#Co-First Author).

12.    Xin Han, Haoming Wu, Chune DongChune Dong, Wei Xie, Shuwen Wu*, Hai-Bing Zhou*. Halolactones are Potent HIV-1 Non-Nucleoside Reverse Transcriptase InhibitorsRSC Adv, 20155, 10005-10013.

13.    Xin HanChune DongHai-Bing Zhou*C3-Symmetrical Cinchonine-Squaramide-Catalyzed Asymmetric Chlorolactonization of Styrene-Type Carboxylic Acids with DCDMH Efficient Method to Chiral Isochroman-1-ones. Adv. Synth. Catal., 2014356, 1275-1280.

14.    Xin Han, Haoming Wu, Wei Wang, Chune Dong, Po Tien, Shuwen Wu*, Hai-Bing Zhou*. Synthesis and SARs of Indole-based α-Amino Acids as Potent HIV-1 Non-Nucleoside Reversed Transcriptase Inhibitors. Org. Biomol. Chem.201412, 8308-8317.

15.    Xin Han, Wenjie Ouyang, Bin Liu, Wei Wang*, Po Tien, Shuwen Wu*, Hai-Bing Zhou*. Enantioselective Inhibition of Reverse Transcriptase (RT) of HIV-1 by Non-Racemic Indole-based Triuoropropanoates Developed by Asymmetric Catalysis Using Recyclable Organocatalysts. Org. Biomol. Chem., 201311, 8463-8475.

16.    Xin Han, Bin Liu, Hai-Bing Zhou, Chune Dong*. Enhanced Efciency of Recyclable C3-Symmetric Cinchonine-Ssquaramides in the Asymmetric Friedel–Crafts Reaction of Indoles with Alkyl Triuoropyruvate. Tetrahedron-Asymmetry, 201223, 1332-1337.

17.    Xin Han, Xiangfei Wu, Chang Min, Hai-Bing Zhou, Chune Dong*. An Expedient Approach to Highly Enantioenriched Cyclic Nitrones Mediated by Robust and Recoverable C3-Symmetric Cinchonine-Squaramide Catalysts. RSC Adv, 20122, 7501-7505.

18.    Xinjin Liu, Jinsen Liang, Yongshi Yu, Xin Han, Lei Yu, Feifei Chen, Zhichao xu, Qi Chen, Mengyu Jin, Chune Dong, Hai-Bing Zhou, Ke Lan, Shuwen Wu. Discovery of Aryl Benzoyl Hydrazide Derivatives as Novel Potent Broad-Spectrum Inhibitors of Influenza A Virus RNA Dependent RNA Polymerase (RdRp). J. Med. Chem., 2019, under review (revision).

19.    Yangbing Li, Jiuling Yang, Angelo Aguilar, Donna McEachern, Sally Przybranowski, Liu Liu, Chaoyie Yang, Mi Wang, Xin Han, Shaomeng Wang. Discovery of MD-224 as a First-in-Class, Highly Potent and Efficacious PROTAC MDM2 Degrader Capable of Achieving Complete and Durable Tumor Regression. J. Med. Chem., 201962, 448-466. (ESI高被引论文)

20.    Xinyu Liao, Yang Lei, Songfeng Chen, Jing Cheng, Dan Zhao, Zhifeng Zhang, Xin Han, Ya Zhang, Huabao Liao, Yang Zhuang, Juan Chen, Haibing Zhou, Qi Wan, Yingying Zou. The Neuroprotective Effect of Bisperoxovanadium (pyridin-2-squaramide) in Intracerebral Hemorrhage. Drug Des Dev Ther201913, 1957–1967.

21.    Tazeem, Abdul R. Bhat, Xin Han, Fareeda Athar*. Synthesis, structure-activity relationship and anti-microbial evaluation of methyl-substituted tetrazoloquinoline based pyrazolinethioamides. ChemistrySelect, 20161, 5917-5922.

22.    Zhi-Feng Zhang#, Juan Chen#Xin Han, Ya Zhang, Hua-Bao Liao, Rui-Xue Lei, Yang Zhuang, Ze-Fen Wang, Zhi-Qiang Li, Jin-Cao Chen, Wei-Jing Liao, Hai-Bing Zhou, Fang, Liu, Qi Wan. Bisperoxovandium (pyridin-2-squaramide) Targets Both PTEN and Erk1/2 to Confer Neuroprotection. Br. J. Pharmacol., 2017174, 641-656. (#Co-First Author).

23.    Enshan Zhou*, Xin Han, Yuanyuan Li, Chao Guo, Chune Dong*. Synthesis of Phenylselanylisochroman-1-ones through Highly Selective Selenolactonization of Styrene-Typed Carboxylic AcidsHETEROCYCLES201591, 1628-1636.

24.    Bin Liu, Xin Han, Ze Dong, Hao Lv, Hai-Bing Zhou, Chune Dong*. Highly Enantioselective Michael Addition of 1,3-Dicarbonyl Compounds to Nitroalkenes Catalyzed by Designer Chiral BINOL–Quinine–Squaramide: Efcient Access to Optically Active Nitro-Alkanes and Their Isoxazole DerivativesTetrahedron-Asymmetry, 201324, 1276-1280.

25.    Chang Min, Xin Han, Zongquan Liao, Xiangfei Wu, Hai-Bing Zhou, Chune Dong*C3-Symmetrical Cinchonine-Squaramide as New Highly Efficient, and Recyclable Organocatalyst for Enantioselective Michael Addition. Adv. Synth. Catal.2011353, 2715-2720.