102: Wang, C., Chen, B., Yang, H., Huang, C., Zhang, Y., Yan, J., Zhang, D., Huang, A., Wu, Y.*, Zhu, J., Zhuang C*, & Miao, Z*. Discovery of Novel Drug-Conjugate Molecule ZM484 with Dual p53-MDM2 and TOP1 Inhibition for the Treatment of Colorectal Cancer. J Med Chem., 2025 Sep 25;68(18):18988-19001. https://doi.org/10.1021/acs.jmedchem.5c01003
101: Wang R, Zhuang C*, Graph neural networks driven acceleration in drug discovery, Acta Pharmaceutica Sinica B, 2025, https://doi.org/10.1016/j.apsb.2025.10.011
100: Xu L, Zhuang C*. Mixed Lineage Kinase Domain-Like Protein (MLKL): From Mechanisms to Therapeutic Opportunities. Adv Sci (Weinh). 2025 Aug 11:e09277. doi: 10.1002/advs.202509277. Epub ahead of print. PMID: 40788062.
99: Jianyu Yan, Tianyu Wang, Ruizhi Yu, Lijuan Xu, Hongming Shao, Tengfei Li, Zhe Wang, Xudong Cha, Zhenyuan Miao, Chengguo Xing, Ke Xu*, Huanhai Liu*, Chunlin Zhuang*, Chemical knockdown of Keap1 and homoPROTAC-ing allergic rhinitis, Acta Pharmaceutica Sinica B, 2025, https://doi.org/10.1016/j.apsb.2025.05.025.
Cover Gallery - Acta Pharmaceutica Sinica B | ScienceDirect.com by Elsevier
98: Chen Y, Qin Q, Ding W, Yu R, Wang R, Ji H, Yan J, Ma H, Jiang CS*, Sun Y*, Zhuang C*. Design of spiro-heterocyclic substituted diaminonaphthalene Keap1-Nrf2 protein-protein interaction inhibitors as novel anti-depressant agents. Eur J Med Chem. 2025 Jun 8;296:117848. doi: 10.1016/j.ejmech.2025.117848. Epub ahead of print. PMID: 40513368.
97: Dai P, Xin Y, Qin X, Ma H*, Zhuang C*. Advances in MLKL-targeted inhibitors and PROTACs for necroptosis therapeutics. Bioorg Med Chem. 2025 May 19;128:118246. doi: 10.1016/j.bmc.2025.118246. Epub ahead of print. PMID: 40409166.
96: Zou Y, Chai Y, Du B, Xin Y, Zhao L, Liu R*, Zhang W*, Zhuang C*. Bardoxolone Derivatives as Novel Pseudo-Natural Necroptosis Inhibitors by Destabilizing HSP90 Client Proteins. J Med Chem. 2025 May 22;68(10):9906-9925. doi: 10.1021/acs.jmedchem.4c02336. Epub 2025 Apr 30. PMID: 40307003.
95: Sun Y, Wang J, Ding W, Qin Q, Wang R, Yu R, Yan J, Hou R, Liu G, Cai X, Qu Z, Zhang W, Yu J, Xing C, Zhuang C*. Design of anti-depressant phosphodiester amino acidic Keap1-Nrf2 protein-protein interaction inhibitors. Redox Biol. 2025 Mar 26;82:103620. doi: 10.1016/j.redox.2025.103620. Epub ahead of print. PMID: 40174476; PMCID: PMC11999321.
94: Qin X, Hou R, Qu Z, Yu J, Zhang W, Ma H*, Zhuang C*. Structure-based molecular hybridization design and synthesis of Keap1-Nrf2 inhibitors for anti-inflammatory treatment. Bioorg Chem. 2025 May;158:108350. doi: 10.1016/j.bioorg.2025.108350. Epub 2025 Mar 5. PMID: 40073597.
93: Wang S, Zhang Y, Yu R, Chai Y, Liu R, Yu J, Qu Z*, Zhang W*, Zhuang C*. Labeled and Label-Free Target Identifications of Natural Products. J Med Chem. 2024 Oct 24;67(20):17980-17996. doi: 10.1021/acs.jmedchem.4c01576. Epub 2024 Oct 3. PMID: 39360958.
92: Han D, Li A, Zhu L, Zhuang C*, Zhao Q*, Zou Y*. Peptide inhibitors targeting Rasand Ras-associated protein-protein interactions. Eur J Med Chem. 2024 Dec 5;279:116878. doi: 10.1016/j.ejmech.2024.116878. Epub 2024 Sep 19. PMID: 39326269.
91: Li G, Lu J, Wang C, Chang X, Qu Z, Zhang W, Zhuang C, Miao Z, Xu W. Discovery of Sophoridine α-Aryl Propionamide Derivative ZM600 as a Novel Antihepatic Fibrosis Agent. J Med Chem. 2024 Jul 11;67(13):11389-11400. doi: 10.1021/acs.jmedchem.4c01010. Epub 2024 Jun 28. PMID: 38938102.
90: Wang S#, Ge Q#, Cong H, Zhang W, Liu H, Qu Z*, Chen H*, Zhuang C*. Structure-Activity Relationship Study of (E)-3-(6-Fluoro-1H-indol-3-Yl)-2-methyl-1-(3,4,5-trimethoxyphenyl)prop-2-en-1-one (FC116) Against Metastatic Colorectal Cancers Resistant to Oxaliplatin. ACS Pharmacol Transl Sci. 2024 Apr 12;7(5):1386-1394. doi: 10.1021/acsptsci.4c00024. PMID: 38751617; PMCID: PMC11091977.
89: Zou J, Yan J, Lu Y, Yu Z, Zhang K, Han Q, Han D, Gai C, Chai X, Zhao Q*, Zhuang C*, Zou Y*. Cyclic Peptide Keap1-Nrf2 Protein-Protein Interaction Inhibitors: Design, Synthesis, and In Vivo Treatment of Acute Lung Injury. J Med Chem. 2024 Mar 28;67(6):4889-4903. doi: 10.1021/acs.jmedchem.4c00065. Epub ahead of print. PMID:38485922.
88: Tang Y, Zhuang C*. Design, synthesis and anti-necroptosis activity of fused heterocyclic MLKL inhibitors. Bioorg Med Chem. 2024 Mar 15;102:117659. doi: 10.1016/j.bmc.2024.117659. Epub 2024 Mar 1. PMID: 38442525.
87: Xin Y, Dai P, Shao H, Zhuang C*, Li J*. Discovery of novel biaryl benzoxazepinones as dual-mode receptor-interacting protein kinase-1 (RIPK1) inhibitors. Bioorg Med Chem. 2024 Feb 15;100:117611. doi: 10.1016/j.bmc.2024.117611. Epub 2024 Feb 1. PMID: 38309200.
86：Tian J, Zhao W, Wu Y, Shi Y, Yu J, Zhang W, Xing C, Zhuang C*, Qu Z*. Diallyl Disulfide Blocks Cigarette Carcinogen 4-(Methylnitrosamino)-1-(3-pyridyl)-1-butanone-Induced Lung Tumorigenesis via Activation of the Nrf2 Antioxidant System and Suppression of NF-κB Inflammatory Response. J Agric Food Chem. 2023 Nov 22;71(46):17763-17774. doi: 10.1021/acs.jafc.3c02007.
85：Fang JJ, Yao HZ, Zhuang C*, Chen FE*. Insight from Linker Investigations: Discovery of a Novel Phenylbenzothiazole Necroptosis Inhibitor Targeting Receptor-Interacting Protein Kinase 1 (RIPK1) from a Phenoxybenzothiazole Compound with Dual RIPK1/3 Targeting Activity. J Med Chem. 2023 Nov 2. doi: 10.1021/acs.jmedchem.3c01351.
84：Zhang J, Cai YS, Ji HL, Ma M, Zhang JH, Cheng ZQ, Wang KM, Jiang CS*, Zhuang C*, Hu Y*, Meng N*. Discovery of marine phidianidine-based Nrf2 activators and their potential against oxLDL- and HG-induced injury in HUVECs. Bioorg Med Chem Lett. 2023 Oct 15;95:129468. doi: 10.1016/j.bmcl.2023.129468.
83：Zhang JB, Jia X, Cao Q, Chen YT, Tong J, Lu GD, Li DJ, Han T*, Zhuang CL*, Wang P*. Ferroptosis-Regulated Cell Death as a Therapeutic Strategy for Neurodegenerative Diseases: Current Status and Future Prospects. ACS Chem Neurosci. 2023 Sep 6;14(17):2995-3012. doi: 10.1021/acschemneuro.3c00406.
82： Sun Y, Xu L, Zheng D, Wang J, Liu G, Mo Z, Liu C, Zhang W, Yu J, Xing C, He L*, Zhuang C*. A potent phosphodiester Keap1-Nrf2 protein-protein interaction inhibitor as the efficient treatment of Alzheimer's disease. Redox Biology, 2023: 102793.
81:Liu X, Jin J, Wu Y, Du B, Zhang L, Lu D, Liu Y, Chen X, Lin J, Chen H, Zhang W*, Zhuang C*, Luan X*. Fluoroindole chalcone analogues targeting the colchicine binding site of tubulin for colorectal oncotherapy. Eur. J. Med. Chem. 2023 Sep 5:115540. doi:10.1016/j.ejmech.2023.115540
80: Shao H, Xu L, Li G, Wang S, Han T*, Zhuang C*. Analysis on benzothiazole necroptosis inhibitors with chiral substitutions in the solvent-accessible region of RIP kinase domain. Bioorg Chem. 2023 Jun 1;137:106647.
79: Yan J, Li Y, Ding L, Hou R, Xing C, Jiang C*, Miao Z*, Zhuang C*. Fragment-Based Discovery of Azocyclic Alkyl Naphthalenesulfonamides as Keap1-Nrf2 Inhibitors for Acute Lung Injury Treatment. J Med Chem. 2023 May 31;66(12):8267-8280.
78: Ling ZY, Lv QZ, Li J, Lu RY, Chen LL, Xu WH, Wang Y*, Zhuang CL*. Protective Effect of a Novel RIPK1 Inhibitor, Compound 4-155, in Systemic Inflammatory Response Syndrome and Sepsis. Inflammation. 2023 May 25. doi: 10.1007/s10753-023-01842-1.
77: Xu L, Zhuang C*. Profiling of small-molecule necroptosis inhibitors based on the subpockets of kinase-ligand interactions. Med Res Rev. 2023 Nov;43(6):1974-2024. doi: 10.1002/med.21968.
published as Front Cover Image, Volume 43, Issue 6
Lijuan Xu, Chunlin Zhuang
First published: 03 October 2023 https://doi.org/10.1002/med.21911
76: Du B, Liu X, Luan X, Zhang W*, Zhuang C*. Structure optimization of an F-indole-chalcone (FC116) on 4-methoxyphenyl group and therapeutic potential against colorectal cancers with low cytotoxicity. Bioorg. Chem. 2023 Jun;135:106531.
75: Xu L, Zhang W, Zhuang C*. Receptor-interacting protein kinase 1 (RIPK1) inhibitor: a review of the patent literature (2018-present). Expert Opin. Ther. Pat. 2023 Feb;33(2):101-124.
74: Zhang X, Han Q, Hou R, Xu L, Zhang W, Xing C, Xue L*, Zhuang C*. Targeting Receptor-Interacting Protein Kinase 1 by Novel Benzothiazole Derivatives: Treatment of Acute Lung Injury through the Necroptosis Pathway. J. Med. Chem. 2023 Apr 13;66(7):5261-5278. (Cover story)
73: Ding Y, Hou R, Yu J, Xing C, Zhuang C*, Qu Z*. Dietary Phytochemicals as Potential Chemopreventive Agents against Tobacco-Induced Lung Carcinogenesis. Nutrients. 2023 Jan 17;15(3):491.
72: Quan D, Hou R, Shao H, Zhang X, Yu J, Zhang W, Yuan H*, Zhuang C*. Structure-Based Design of Novel Alkynyl Thio-Benzoxazepinone Receptor-Interacting Protein Kinase-1 Inhibitors: Extending the Chemical Space from the Allosteric to ATP Binding Pockets. J. Med. Chem. 2023 Feb 23;66(4):3073-3087.
71: Xu Y, Liang C, Zhang W, Yu J, Xing C, Liu H*, Zhuang C*. Profiling of the chemical space on the phenyl group of substituted benzothiazole RIPK3 inhibitors. Bioorg. Chem. 2023 Feb;131:106339.
70: Shao H, Wu W, Wang P*, Han T*, Zhuang C*. Role of Necroptosis in Central Nervous System Diseases. ACS Chem Neurosci. 2022 Dec 7;13(23):3213-3229.
69: Sun Y, Xu L, Shao H, Quan D, Mo Z, Wang J, Zhang W, Yu J, Zhuang C*, Xu K*. Discovery of a Trifluoromethoxy Cyclopentanone Benzothiazole Receptor- Interacting Protein Kinase 1 Inhibitor as the Treatment for Alzheimer's Disease. J. Med. Chem. 2022 Nov 10;65(21):14957-14969. (Cover story)
68: Li J, Cai Z, Li XW*, Zhuang C*. Natural Product-Inspired Targeted Protein Degraders: Advances and Perspectives. J. Med. Chem. 2022 Oct 27;65(20):13533-13560.
67: Yan J, Li T, Miao Z, Wang P, Sheng C*, Zhuang C*. Homobivalent, Trivalent, and Covalent PROTACs: Emerging Strategies for Protein Degradation. J. Med. Chem. 2022 Jul 14;65(13):8798-8827.
66: Liu G, Hou R, Xu L, Zhang X, Yan J, Xing C, Xu K*, Zhuang C*. Crystallography-Guided Optimizations of the Keap1-Nrf2 Inhibitors on the Solvent Exposed Region: From Symmetric to Asymmetric Naphthalenesulfonamides. J. Med. Chem. 2022 Jun 23;65(12):8289-8302. (Cover story)
65: Song Z#, Tang G#, Zhuang C#, Wang Y, Wang M, Lv D, Lu G, Meng J, Xia M, Zhu Z, Chai Y, Yang J, Liu Y. Metabolomic profiling of cerebrospinal fluid reveals an early diagnostic model for central nervous system involvement in acute lymphoblastic leukaemia. Br. J. Haematol. 2022 Sep;198(6):994-1010.
64: Zhao W, Liu Y, Xu L, He Y, Cai Z, Yu J, Zhang W, Xing C, Zhuang C*, Qu Z*. Targeting Necroptosis as a Promising Therapy for Alzheimer's Disease. ACS Chem. Neurosci. 2022 Jun 15;13(12):1697-1713. (Cover story)
63: Hao Y, Shao H, Qu Z, Li J, Shi Y, Zhang W, Yu J, Fu P*, Zhuang C*. Investigation on the chemical space of the substituted triazole thio-benzoxazepinone RIPK1 inhibitors. Eur. J. Med. Chem. 2022 Jun 5;236:114345.
62: Zhang CX, Tu Y, Sun XC, Chen DG, Zhang WN, Zhuang CL*, Wang ZB*, Su L*. Peramivir, an Anti-Influenza Virus Drug, Exhibits Potential Anti-Cytokine Storm Effects. Front. Immunol. 2022 Feb 28;13:856327.
61: Ding L, Pannecouque C, De Clercq E, Zhuang C*, Chen FE*. Discovery of Novel Pyridine-Dimethyl-Phenyl-DAPY Hybrids by Molecular Fusing of Methyl-Pyrimidine-DAPYs and Difluoro-Pyridinyl-DAPYs: Improving the Druggability toward High Inhibitory Activity, Solubility, Safety, and PK. J. Med. Chem. 2022 Feb 10;65(3):2122-2138.
60: Zhu J, Xin M, Xu C, He Y, Zhang W, Wang Z*, Zhuang C*. Ligand-based substituent-anchoring design of selective receptor-interacting protein kinase 1 necroptosis inhibitors for ulcerative colitis therapy. Acta Pharm. Sin. B. 2021 Oct;11(10):3193-3205.
59. Xu L, Tu Y, Li J, Zhang W, Wang Z, Zhuang C*, Xue L*. Structure-based optimizations of a necroptosis inhibitor (SZM594) as novel protective agents of acute lung injury. Chin. Chem. Lett. 2022, May;33(5):2545-2549.
58: Li J, Zhuang C*. Natural Indole Alkaloids from Marine Fungi: Chemical Diversity and Biological Activities. Pharmceutical Fronts, 2021;3(04):e139-e163.
57. Jin X, Piao HR, Pannecouque C, De Clercq E, Zhuang C*, Chen FE*. Design of the naphthyl-diarylpyrimidines as potent non-nucleoside reverse transcriptase inhibitors (NNRTIs) via structure-based extension into the entrance channel. Eur. J. Med. Chem. 2021 Dec 15;226:113868.
56. Zhang L, Qu Z, Song A, Yang J, Yu J, Zhang W*, Zhuang C*. Garlic oil blocks tobacco carcinogen 4-(methylnitrosamino)-1-(3-pyridyl)-1-butanone (NNK)-induced lung tumorigenesis by inducing phase II drug-metabolizing enzymes. Food Chem. Toxicol. 2021 Nov;157:112581.
55. Ding L, Pannecouque C, De Clercq E, Zhuang C*, Chen FE*. Improving Druggability of Novel Diarylpyrimidine NNRTIs by a Fragment-Based Replacement Strategy: From Biphenyl-DAPYs to Heteroaromatic-Biphenyl-DAPYs. J. Med. Chem. 2021 Jul 22;64(14):10297-10311.
54. Zhang L, Xu L, Chen H, Zhang W, Xing C, Qu Z*, Yu J*, Zhuang C*. Structure-based molecular hybridization design of Keap1-Nrf2 inhibitors as novel protective agents of acute lung injury. Eur. J. Med. Chem. 2021 Oct 15;222:113599.
53. Zhu J, Qu Z, Huang J, Xu L, Zhang H, Yu J, Zhang W*, Zhuang C*. Enantiomeric profiling of a chiral benzothiazole necroptosis inhibitor. Bioorg. Med. Chem. Lett. 2021 May 6;43:128084.
52. Qu Z, Zhang L, Hou R, Ma X, Yu J, Zhang W*, Zhuang C*. Exposure to a mixture of cigarette smoke carcinogens disturbs gut microbiota and influences metabolic homeostasis in A/J mice. Chem. Biol. Interact. 2021 May 1;344:109496.
51. Xia C, Yao Z, Xu L, Zhang W, Chen H*, Zhuang C*. Structure-based bioisosterism design of thio-benzoxazepinones as novel necroptosis inhibitors. Eur. J. Med. Chem. 2021 Apr 27;220:113484.
50. Sang Y, Pannecouque C, De Clercq E, Zhuang C*, Chen F*. Chemical space exploration of novel naphthyl-carboxamide-diarylpyrimidine derivatives with potent anti-HIV-1 activity. Bioorg Chem. 2021 Apr 20;111:104905.
49: Ding L, Pannecouque C, De Clercq E, Zhuang C*, Chen F*. Hydrophobic pocket occupation design of difluoro-biphenyl-diarylpyrimidines as non-nucleoside HIV-1 reverse transcriptase inhibitors: from N-alkylation to methyl hopping on the pyrimidine ring, J. Med. Chem., 2021, 64(8):5067-5081
48: Ding L, Zhuang C*, Chen F*. Druggability modification strategies of the diarylpyrimidine-type non-nucleoside reverse transcriptase inhibitors. Med. Res. Rev. 2021, 41, 1255-1290.
47: Shi Y, Wu Y. R., Yu J.Q., Zhang W.N., Zhuang C.L.* DNA-encoded libraries (DELs): a review of on-DNA chemistries and their output. RSC Adv. 2021. Jan 19; 11: 2359-2376.
46: Wang Y, Ma H, Huang J, Yao Z, Yu J, Zhang W, Zhang L*, Wang Z*, Zhuang C*. Discovery of bardoxolone derivatives as novel orally active necroptosis inhibitors. Eur. J. Med. Chem. 2020 Nov 21:113030.
45: Sang Y, Ding L, Zhuang C*, Chen F*. Design strategies for long-acting anti-HIV pharmaceuticals. Curr. Opin. Pharmacol. 2020 Oct; 54: 158-165.
44: Sun Y, Huang J, Chen Y, Shang H, Zhang W, Yu J, He L*, Xing C*, Zhuang C*. Direct inhibition of Keap1-Nrf2 Protein-Protein interaction as a potential therapeutic strategy for Alzheimer's disease. Bioorg. Chem. 2020 Oct; 103:104172.
43: Su L, Tu Y, Kong DP, Chen DG, Zhang CX, Zhang WN, Zhuang CL*, Wang ZB*. Drug repurposing of anti-infective clinical drugs: Discovery of two potential anti-cytokine storm agents. Biomed. Pharmacother. 2020 Nov; 131: 110643.
42: Ma H, Wu Y, Zhang W, Zhang H, Miao Z*, Zhuang C*. Radiosensitization of human pancreatic cancer by piperlongumine analogues. Chin. Chem. Lett. 2020, doi: 10.1016/j.cclet.2020.08.049
41: Qu Z, Sun J, Zhang W, Yu J*, Zhuang C*. Transcription factor NRF2 as a promising therapeutic target for Alzheimer's disease. Free Radic. Biol. Med. 2020 Nov 1; 159: 87-102.
40: Chen X, Ding L, Tao Y, Pannecouque C, De Clercq E, Zhuang C*, Chen FE*. Bioisosterism-based design and enantiomeric profiling of chiral hydroxyl-substituted biphenyl-diarylpyrimidine nonnucleoside HIV-1 reverse transcriptase inhibitors. Eur. J. Med. Chem. 2020 Sep 15; 202: 112549.
39: Zhuang C, Pannecouque C, De Clercq E, Chen F*. Development of non-nucleoside reverse transcriptase inhibitors (NNRTIs): our past twenty years. Acta Pharm. Sin. B. 2020 Jun; 10(6): 961-978.
38: Yang Y, Pannecouque C, Clercq E, Zhuang C*, Chen FE*. Privileged scaffold inspired design of novel oxime-biphenyl-DAPYs in treatment of HIV-1. Bioorg. Chem. 2020 Jun; 99: 103825.
37: Han S, Lei Y, Pannecouque C, De Clercq E, Zhuang C*, Chen FE*. Fragment-based discovery of sulfur-containing diarylbenzopyrimidines as novel nonnucleoside reverse transcriptase inhibitors. Chin. Chem. Lett. 2020, Mar; 31(3): 764-768.
36: Wang Y, Huang G, Shi Y, Tian WS, Zhuang C*, Chen FE*. Asymmetric synthesis of (-)-solanidine and (-)-tomatidenol. Org. Biomol. Chem. 2020 Apr 29; 18(16):3169-3176.
35: Li TT, Pannecouque C, De Clercq E, Zhuang CL*, Chen FE*. Scaffold Hopping in Discovery of HIV-1 Non-Nucleoside Reverse Transcriptase Inhibitors: From CH(CN)-DABOs to CH(CN)-DAPYs. Molecules. 2020 Mar 30; 25(7): 1581.
34: Lei Y, Han S, Yang Y, Pannecouque C, De Clercq E, Zhuang C*, Chen FE*. Design of Biphenyl-Substituted Diarylpyrimidines with a Cyanomethyl Linker as HIV-1 NNRTIs via a Molecular Hybridization Strategy. Molecules. 2020 Feb 26; 25(5): 1050.
33: Sang Y, Pannecouque C, De Clercq E, Zhuang C*, Chen F*. Pharmacophore-fusing design of pyrimidine sulfonylacetanilides as potent non-nucleoside inhibitors of HIV-1 reverse transcriptase. Bioorg. Chem. 2020 Mar; 96: 103595.
32: Han S, Sang Y, Wu Y, Tao Y, Pannecouque C, De Clercq E, Zhuang C*, Chen FE*. Fragment hopping-based discovery of novel sulfinylacetamide-diarylpyrimidines (DAPYs) as HIV-1 nonnucleoside reverse transcriptase inhibitors. Eur. J. Med. Chem. 2020 Jan 1; 185:111874.
31: Sang Y, Han S, Pannecouque C, De Clercq E, Zhuang C*, Chen F*. Ligand-Based Design of Nondimethylphenyl-Diarylpyrimidines with Improved Metabolic Stability, Safety, and Oral Pharmacokinetic Profiles. J. Med. Chem. 2019 Dec 26; 62(24): 11430-11436. (Cover story)
30: Zhuang C*, Chen F*. Small-Molecule Inhibitors of Necroptosis: Current Status and Perspectives. J. Med. Chem. 2020 Feb 27;63(4):1490-1510.
29: Han S, Sang Y, Wu Y, Tao Y, Pannecouque C, De Clercq E, Zhuang C*, Chen FE*. Molecular Hybridization-Inspired Optimization of Diarylbenzopyrimidines as HIV-1 Nonnucleoside Reverse Transcriptase Inhibitors with Improved Activity against K103N and E138K Mutants and Pharmacokinetic Profiles. ACS Infect. Dis. 2020 May 8; 6(5): 787-801. (Cover story)
28: Sang Y, Han S, Pannecouque C, De Clercq E, Zhuang C*, Chen F*. Conformational restriction design of thiophene-biphenyl-DAPY HIV-1 non-nucleoside reverse transcriptase inhibitors. Eur. J. Med. Chem. 2019 Aug 8;182:111603.
27: Zhang H, Xu L, Qin X, Chen X, Cong H, Hu L, Chen L, Miao Z, Zhang W*, Cai Z*, Zhuang C*. N-(7-Cyano-6-(4-fluoro-3-(2-(3-(trifluoromethyl)phenyl)acetamido)phenoxy) benzo[d]thiazol-2-yl)cyclopropanecarboxamide (TAK-632) Analogues as Novel Necroptosis Inhibitors by Targeting Receptor-Interacting Protein Kinase 3 (RIPK3): Synthesis, Structure-Activity Relationships and In Vivo Efficacy. J. Med. Chem. 2019, 62(14): 6665-6681. (Cover story)
26: Chen X#, Zhuang C#*, Ren Y, Zhang H, Qin X, Hu L, Fu J, Miao Z, Chai Y, Liu ZG, Zhang H, Cai Z*, Wang HY*. Identification of the Raf kinase inhibitor TAK-632 and its analogues as potent inhibitors of necroptosis by targeting RIPK1 and RIPK3. Br. J. Pharmacol. 2019 Jun; 176(12): 2095-2108.
25: Wang H, Wei W, Lan X, Liu N, Li Y, Ma H, Sun T, Peng X*, Zhuang C*, Yu J*. Neuroprotective Effect of Swertiamain on Cerebral Ischemia/Reperfusion Injury by Inducing the Nrf2 Protective Pathway. ACS Chem. Neurosci. 2019 May 15;10(5):2276-2286.
24: Cong H, Xu L, Wu Y, Qu Z, Bian T, Zhang W, Xing C*, Zhuang C*. Inhibitor of Apoptosis Protein (IAP) Antagonists in Anticancer Agent Discovery: Current Status and Perspectives. J. Med. Chem. 2019 Jun 27;62(12):5750-5772.
23: Zhuang C*, Guan X, Ma H, Cong H, Zhang W, Miao Z*. Small molecule-drug conjugates: A novel strategy for cancer-targeted treatment. Eur. J. Med. Chem. 2018 Dec 16; 163: 883-895.
22: Cong H, Zhao X, Castle BT, Pomeroy EJ, Zhou B, Lee J, Wang Y, Bian T, Miao Z, Zhang W, Sham YY, Odde DJ, Eckfeldt CE, Xing C*, Zhuang C*. An Indole-Chalcone Inhibits Multidrug-Resistant Cancer Cell Growth by Targeting Microtubules. Mol. Pharm. 2018 Sep 4; 15(9): 3892-3900.
21: Jiang CS, Zhuang CL (co-first author), Zhu K, Zhang J, Muehlmann LA, Figueiró Longo JP, Azevedo RB, Zhang W, Meng N, Zhang H. Identification of a novel small-molecule Keap1-Nrf2
PPI inhibitor with cytoprotective effects on LPS-induced cardiomyopathy. J. Enzyme Inhib. Med. Chem. 2018 Dec; 33(1): 833-841.
20: Chen L, Zhuang C (co-first author), Lu J, Jiang Y, Sheng C*. Discovery of Novel KRAS-PDEδ Inhibitors by Fragment-Based Drug Design. J. Med. Chem. 2018 Mar 22; 61(6): 2604-2610.
19: Meng N, Tang H, Zhang H, Jiang C, Su L, Min X, Zhang W, Zhang H*, Miao Z*, Zhang W*, Zhuang C*. Fragment-growing guided design of Keap1-Nrf2 protein-protein interaction inhibitors for targeting myocarditis. Free Radic. Biol. Med. 2018 Mar; 117: 228-237.
18: Jiang Y, Zhuang C (co-first author), Chen L, Lu J, Dong G, Miao Z, Zhang W, Li J, Sheng C*. Structural Biology-Inspired Discovery of Novel KRAS-PDEδ Inhibitors. J. Med. Chem. 2017 Nov 22; 60(22): 9400-9406.
17: Zhang BW, Li X, Sun WL, Xing Y, Xiu ZL, Zhuang CL*, Dong YS*. Dietary Flavonoids and Acarbose Synergistically Inhibit α-Glucosidase and Lower Postprandial Blood Glucose. J. Agric. Food Chem. 2017 Sep 27;65(38):8319-8330.
16: Sun W, Zhuang C*, Li X, Zhang B, Lu X, Zheng Z, Dong Y*. Varic acid analogues from fungus as PTP1B inhibitors: Biological evaluation and structure-activity relationships. Bioorg. Med. Chem. Lett. 2017 Aug 1;27(15):3382-3385.
15: Zhuang C, Zhang W, Sheng C, Zhang W, Xing C*, Miao Z*. Chalcone: A Privileged Structure in Medicinal Chemistry. Chem. Rev. 2017 Jun 28;117(12):7762-7810. (Highly Cited paper)
14: Zhang Y, Ma H, Wu Y, Wu Z, Yao Z, Zhang W, Zhuang C*, Miao Z*. Novel non-trimethoxylphenyl piperlongumine derivatives selectively kill cancer cells. Bioorg. Med. Chem. Lett. 2017 Jun 1;27(11):2308-2312.
13: Ma H, Zhuang C (co-first author), Xu X, Li J, Wang J, Min X, Zhang W, Zhang H*, Miao Z*. Discovery of benzothiazole derivatives as novel non-sulfamide NEDD8 activating enzyme inhibitors by target-based virtual screening. Eur. J. Med. Chem. 2017 Jun 16; 133: 174-183.
12: Zhuang C, Wu Z, Xing C*, Miao Z*. Small molecules inhibiting Keap1-Nrf2 protein-protein interactions: a novel approach to activate Nrf2 function. Medchemcomm. 2016 Nov 17; 8(2): 286-294.
11: Zhou B, Yu X, Zhuang C*, Villalta P, Lin Y, Lu J, Xing C*. Unambiguous Identification of β-Tubulin as the Direct Cellular Target Responsible for the Cytotoxicity of Chalcone by Photoaffinity Labeling. ChemMedChem. 2016 Jul 5;11(13):1436-1445.
10: Zhou, W. H.; Xu, X. G.; Li, J.; Min, X.; Yao, J. Z.; Dong, G. Q.; Zhuang, C. L.*; Miao, Z. Y.*; Zhang, WN*. Design, synthesis and structure-activity relationship of 4,5-dihydropyrrolo[3,4-c]pyrazol-6(1H)-ones as potent p53-MDM2 inhibitors. Chin. Chem. Lett. 2017, 28, 422–425.
Ph. D period
9: Zhuang C, Sheng C, Shin WS, Wu Y, Li J, Yao J, Dong G, Zhang W, Sham YY*, Miao Z*, Zhang W*. A novel drug discovery strategy: mechanistic investigation of an enantiomeric antitumor agent targeting dual p53 and NF-κB pathways. Oncotarget. 2014 Nov 15; 5(21): 10830-10839.
8: Yu Z, Zhuang C (co-first author), Wu Y, Guo Z, Li J, Dong G, Yao J, Sheng C, Miao Z, Zhang W. Design, synthesis and biological evaluation of sulfamide and triazole benzodiazepines as novel p53-MDM2 inhibitors. Int. J. Mol. Sci. 2014 Sep 5;15(9):15741-15753.
7: Zhuang C, Miao Z, Sheng C, Zhang W. Updated research and applications of small molecule inhibitors of Keap1-Nrf2 protein-protein interaction: a review. Curr. Med. Chem. 2014; 21(16):1861-1870.
6: Zhuang C, Miao Z, Wu Y, Guo Z, Li J, Yao J, Xing C, Sheng C, Zhang W. Double-edged swords as cancer therapeutics: novel, orally active, small molecules simultaneously inhibit p53-MDM2 interaction and the NF-κB pathway. J. Med. Chem. 2014 Feb 13;57(3):567-577.
5: Zhuang C, Narayanapillai S, Zhang W, Sham YY, Xing C. Rapid identification of Keap1-Nrf2 small-molecule inhibitors through structure-based virtual screening and hit-based substructure search. J. Med. Chem. 2014 Feb 13;57(3): 1121-1126.
4: Zhu L, Zhuang C (co-first author), Lei N, Guo Z, Sheng C, Dong G, Wang S, Zhang Y, Yao J, Miao Z, Zhang W. Synthesis and preliminary bioevaluation of novel E-ring modified acetal analog of camptothecin as cytotoxic agents. Eur. J. Med. Chem. 2012 Oct; 56: 1-9.
3: Zhuang C, Miao Z, Zhu L, Dong G, Guo Z, Wang S, Zhang Y, Wu Y, Yao J, Sheng C, Zhang W. Discovery, synthesis, and biological evaluation of orally active pyrrolidone derivatives as novel inhibitors of p53-MDM2 protein-protein interaction. J. Med. Chem. 2012 Nov 26; 55(22): 9630-9642.
2: Guo Z, Zhuang C (co-first author), Zhu L, Zhang Y, Yao J, Dong G, Wang S, Liu Y, Chen H, Sheng C, Miao Z, Zhang W. Structure-activity relationship and antitumor activity of thio-benzodiazepines as p53-MDM2 protein-protein interaction inhibitors. Eur. J. Med. Chem. 2012 Oct; 56: 10-16.
1: Zhuang C, Miao Z, Zhu L, Zhang Y, Guo Z, Yao J, Dong G, Wang S, Liu Y, Chen H, Sheng C, Zhang W. Synthesis and biological evaluation of thio-benzodiazepines as novel small molecule inhibitors of the p53-MDM2 protein-protein interaction. Eur. J. Med. Chem. 2011 Nov; 46(11):5654-5661.
