Article
Chemistry, Medicinal
Zhipeng Zhang, Jie Guo, Maojun Cheng, Weixin Zhou, Yang Wan, Rikang Wang, Yuanying Fang, Yi Jin, Jing Liu, Sai-Sai Xie
Summary: A series of multifunctional hybrid compounds were designed and synthesized in this study, with compound 4j showing potent dual ChEs inhibition activity, good bioactivity, and promising potential for the treatment of Alzheimer's disease.
EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
(2021)
Article
Biochemistry & Molecular Biology
Elisa Uliassi, Christian Bergamini, Nicola Rizzardi, Marina Naldi, Angel Cores, Manuela Bartolini, J. Carlos Menendez, Maria Laura Bolognesi
Summary: Multi-target drug discovery is an active field in the search for new drugs against Alzheimer's disease. In this study, a novel set of multi-target-directed ligands (MTDLs) was designed and synthesized, with the most interesting hybrid 3 showing excellent inhibition of cholinesterase enzymes and antioxidant effects. The study uncovered the potential of the quinolinetrione scaffold as a novel motif for anti-amyloid aggregation and antioxidant properties in the development of anti-AD drugs.
BIOORGANIC & MEDICINAL CHEMISTRY
(2023)
Article
Chemistry, Physical
Meng-qiu Song, Wei Min, Jing Wang, Xi-Xi Si, Xiu-Jun Wang, Yu-Wei Liu, Da-Hua Shi
Summary: Twelve carbazole-coumarin hybrids were synthesized and compound 3h showed good AChE inhibitory activity. The structure-activity relationship studies revealed that the linker length and the structure of coumarin moieties affected the inhibitory activities of the hybrids on BuChE.
JOURNAL OF MOLECULAR STRUCTURE
(2021)
Article
Chemistry, Physical
Yongmei Zhao, Jianwu Lv, Hongli Yu, Kang Huang, Zhihan Du, Wen Luo
Summary: A series of novel dictamnine derivatives were synthesized and evaluated for their dual inhibition activity against cholinesterase and beta-amyloid aggregation. These derivatives showed potent inhibitory activities against acetylcholinesterase (AChE) and butyrylcholinesterase (BChE) at micromolar to sub-micromolar levels. Compound 7k exhibited the strongest inhibitory activity against both AChE and BChE, outperforming its precursor dictamnine and the commercial inhibitor galanthamine. Kinetic analyses and molecular modeling suggested a mixed-type inhibition of AChE by compound 7k. Additionally, some derivatives showed potent inhibitory activity against AChE-induced beta-amyloid (Aβ) aggregation. Furthermore, compound 7k showed no toxicity to SH-SY5Y and HL-7702 cells at the tested concentration. Therefore, these dictamnine derivatives, especially 7k, hold promise as potential candidates for Alzheimer's disease treatment and warrant further investigation.
JOURNAL OF MOLECULAR STRUCTURE
(2023)
Article
Biochemistry & Molecular Biology
Katerina Konstantoulea, Patricia Guerreiro, Meine Ramakers, Nikolaos Louros, Liam D. Aubrey, Bert Houben, Emiel Michiels, Matthias De Vleeschouwer, Yulia Lampi, Luis F. Ribeiro, Joris Wit, Wei-Feng Xue, Joost Schymkowitz, Frederic Rousseau
Summary: The study found that proteins enriched in homologous sequences to Aβ aggregation-prone regions are present in Aβ plaques from AD patients, suggesting heterotypic amyloid interactions may occur. These proteins can modify Aβ assembly kinetics, fibril morphology, and deposition pattern in vitro. Additionally, it was discovered that transient expression of three of these proteins in an Aβ reporter cell line promotes Aβ amyloid aggregation, indicating a potential role of heterotypic APR interactions in amyloid-deposition diseases.
Article
Biochemistry & Molecular Biology
Panpan Zhang, Ze Wang, Chenye Mou, Jiamei Zou, Yanfei Xie, Zhiwen Liu, C. Benjamin Naman, Yuechun Mao, Jiaxin Wei, Xinghan Huang, Jiahui Dong, Mengxiang Yang, Ning Wang, Haixiao Jin, Fufeng Liu, Dongdong Lin, Hao Liu, Fei Zhou, Shan He, Bin Zhang, Wei Cui
Summary: This study developed novel drug candidates that can inhibit AChE and Aβ(1-42) aggregation, demonstrating potential neuroprotective and cognitive-enhancing effects in mice.
BIOORGANIC CHEMISTRY
(2021)
Review
Chemistry, Inorganic & Nuclear
Bo Jiang, Angel A. Marti
Summary: Metal complexes in photoluminescence spectroscopy have been utilized for the detection of amyloid aggregates, exhibiting specific responses in the presence of these aggregates such as intensity changes, emission wavelength shifts, variations in lifetime, and anisotropy changes.
EUROPEAN JOURNAL OF INORGANIC CHEMISTRY
(2021)
Article
Biochemistry & Molecular Biology
Eugenie Nepovimova, Lucie Svobodova, Rafael Dolezal, Vendula Hepnarova, Lucie Junova, Daniel Jun, Jan Korabecny, Tomas Kucera, Zuzana Gazova, Katarina Motykova, Jana Kubackova, Zuzana Bednarikova, Jana Janockova, Catarina Jesus, Luisa Cortes, Joao Pina, Danijela Rostohar, Carlos Serpa, Ondrej Soukup, Laura Aitken, Rebecca E. Hughes, Kamil Musilek, Lubica Muckova, Petr Jost, Marketa Chvojkova, Karel Vales, Martin Valis, Zofia Chrienova, Katarina Chalupova, Kamil Kuca
Summary: The series of tacrine-benzothiazole hybrids show promising anti-AChE properties and capability to block Aβ aggregation, with the most potent derivative being 10w that exhibits highly selective inhibition of AChE. Moreover, 10w also demonstrates strong inhibitory effects against ABAD activity.
BIOORGANIC CHEMISTRY
(2021)
Article
Chemistry, Medicinal
Misato Tajiri, Ryo Yamada, Mayumi Hotsumi, Koki Makabe, Hiroyuki Konno
Summary: This study describes the total synthesis of berberine and selected analogues, and evaluates their effectiveness as amyloid beta (Aβ) aggregation inhibitors. The key step in the synthesis is the assembly of the berberine framework using an intermolecular Heck reaction. Berberine analog 17, incorporating a tertiary amine moiety, demonstrated good anti-Aβ aggregation activity, water solubility, and minimal toxicity to nerve cells.
EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
(2021)
Article
Biochemistry & Molecular Biology
Rajdeep Kaur, Simranjeet Singh Narang, Pritpal Singh, Bhupesh Goyal
Summary: A recent study found that C1 is a potential therapeutic drug for Alzheimer's disease. Molecular dynamics simulations were used to investigate the inhibitory mechanism of C1 against A beta(42) aggregation and BACE1 activity. The study also identified CHEMBL2019027 (C2) as a promising dual inhibitor of A beta(42) aggregation and BACE1 activity through virtual screening and molecular dynamics simulations.
JOURNAL OF BIOMOLECULAR STRUCTURE & DYNAMICS
(2023)
Review
Chemistry, Inorganic & Nuclear
Jun Li, Wang Liao, Dongqing Huang, Meitong Ou, Tongkai Chen, Xinlu Wang, Ruiyue Zhao, Lingyan Zhang, Lin Mei, Jun Liu, Ping Luan
Summary: Alzheimer's disease is a common central neurodegenerative disorder characterized by behavioral disturbance and progressive cognitive impairment. Accumulation of soluble oligomers and amyloid plaques outside nerve cells are crucial in its development. Advanced strategies for detecting and modulating amyloid beta (A beta) in diagnosis and treatment include the use of large-scale apparatus and novel devices, as well as therapeutic agents and nanomaterials.
COORDINATION CHEMISTRY REVIEWS
(2023)
Article
Engineering, Biomedical
Bibin Anand, Qi Wu, Maryam Nakhaei-Nejad, Govindarajan Karthivashan, Lyudmyla Dorosh, Sara Amidian, Abhishek Dahal, Xiuju Li, Maria Stepanova, Holger Wille, Fabrizio Giuliani, Satyabrata Kar
Summary: Native PLGA nanoparticles show therapeutic potential in the treatment of Alzheimer's disease by suppressing aggregation of beta-amyloid peptides, triggering their disassembly, reducing phosphorylation of tau protein, enhancing neuronal viability, and attenuating memory deficits and A beta levels in animal models of AD.
BIOACTIVE MATERIALS
(2022)
Article
Chemistry, Analytical
Cen Ding, Changhong Li, Qing Meng, Chengyuan Qian, Changli Zhang, Liu Yang, Xiaohui Wang, Yanqing Wang
Summary: A label-free fluorescent probe (BTS) was reported for dynamic in situ visualization of A beta 40 aggregation. The probe binds to all forms of A beta 40 with high affinity and can monitor the entire A beta aggregation process with high selectivity and sensitivity.
SENSORS AND ACTUATORS B-CHEMICAL
(2021)
Article
Biochemistry & Molecular Biology
Panagiotis M. Spatharas, Georgia I. Nasi, Paraskevi L. Tsiolaki, Marilena K. Theodoropoulou, Nikos C. Papandreou, Andreas Hoenger, Ioannis P. Trougakos, Vassiliki A. Iconomidou
Summary: Clusterin is identified as a glycoprotein involved in amyloid formation and has aggregation-prone regions that can form amyloid-like fibrils while also inhibiting amyloid-beta fibril formation. These findings suggest a potential role of clusterin in the molecular mechanism of inhibiting amyloid formation and indicate a possible involvement of molecular chaperones with amyloidogenic properties in regulating amyloid formation.
BIOCHIMICA ET BIOPHYSICA ACTA-MOLECULAR BASIS OF DISEASE
(2022)
Article
Biotechnology & Applied Microbiology
Pallabi Sil Paul, Jae-Young Cho, Qi Wu, Govindarajan Karthivashan, Emily Grabovac, Holger Wille, Mariana Kulka, Satyabrata Kar
Summary: The study found that native PLGA can inhibit the aggregation of A beta peptides and disassemble existing aggregates, protecting neurons from toxicity associated with Alzheimer's disease pathology at temperatures outside the physiological range. These findings support the unique therapeutic potential of PLGA nanoparticles in the treatment of AD.
JOURNAL OF NANOBIOTECHNOLOGY
(2022)
Article
Chemistry, Organic
Peng-Ran Cao, Yi-Lei Zheng, Yong-Qin Zhao, Xiao-Bing Wang, Hao Zhang, Mei-Hui Zhang, Ting Yang, Yu-Cheng Gu, Ming-Hua Yang, Ling-Yi Kong
Summary: Two novel natural products, beetleane A (1) and epicoane A (2), were isolated from the metabolites of an endophytic Epicoccum nigrum. Compound 1 features a unique beetlelike structure constructed by the fusion of an unusual [5.5.5.6]trioxafenestrane with a cycloheptane ring, while compound 2 possesses a compact cagelike structure with a unique 6/5/5/5/6/6/5 heptacyclic ring system. Both compounds exhibited strong antiliver fibrosis activity in vitro.
Article
Chemistry, Medicinal
Lailiang Qu, Limei Ji, Cheng Wang, Heng Luo, Shang Li, Wan Peng, Fucheng Yin, Dehua Lu, Xingchen Liu, Lingyi Kong, Xiaobing Wang
Summary: The selenium-containing compound 13f, based on ebselen and verubecestat, showed potential anti-Alzheimer's disease and antioxidant stress effects by reducing beta-amyloid production and alleviating oxidative stress. Furthermore, 13f also demonstrated anti-inflammatory and cytoprotective effects, making it a promising candidate for AD treatment.
EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
(2021)
Article
Chemistry, Medicinal
Cheng Wang, Lailiang Qu, Shang Li, Fucheng Yin, Limei Ji, Wan Peng, Heng Luo, Dehua Lu, Xingchen Liu, Xinye Chen, Lingyi Kong, Xiaobing Wang
Summary: The dual action of PARP inhibitors and EZH2 inhibitors can enhance the treatment of TNBC, with the compound 5a showing potential in reducing sensitivity to inhibitors in BRCA cells.
JOURNAL OF MEDICINAL CHEMISTRY
(2021)
Review
Pharmacology & Pharmacy
Shang Li, Lailiang Qu, Xiaobing Wang, Lingyi Kong
Summary: This review provides a comprehensive overview of the potential role of RIPK1 in the progression of Alzheimer's disease (AD). It explores the underlying linkages between RIPK1 and AD, including neuronal death, Aβ and Tau, inflammasome activation, BBB rupture, AMPK/mTOR, mitochondrial dysfunction, and O-glcNAcylation. The review also covers the discovery of RIPK1 inhibitors, ongoing clinical trials, and future RIPK1-targeted therapeutics.
PHARMACOLOGY & THERAPEUTICS
(2022)
Article
Chemistry, Organic
Fucheng Yin, Wan Peng, Cheng Wang, Lailiang Qu, Xinye Chen, Lingyi Kong, Xiaobing Wang
Summary: A protocol for Rh(III)-catalyzed cascade reaction was established, which allows the efficient construction of phthalides and isocoumarins skeleton with broad applicability. The method can potentially be applied to the total synthesis of natural products.
ASIAN JOURNAL OF ORGANIC CHEMISTRY
(2022)
Article
Biochemistry & Molecular Biology
Dehua Lu, Lailiang Qu, Cheng Wang, Heng Luo, Shang Li, Fucheng Yin, Xingchen Liu, Xinye Chen, Zhongwen Luo, Ningjie Cui, Wan Peng, Limei Ji, Lingyi Kong, Xiaobing Wang
Summary: Combining HDAC inhibitors with DNA damage agents has shown promise in treating solid tumors. We designed a series of harmine-based inhibitors, with compound 27 showing potential in binding to DNA and causing DNA damage. Compound 27 induced cell apoptosis through the p53 signaling pathway and exhibited significant anti-proliferation effects against HCT-116 cells.
BIOORGANIC CHEMISTRY
(2022)
Article
Chemistry, Medicinal
Cheng Wang, Xinye Chen, Xingchen Liu, Dehua Lu, Shang Li, Lailiang Qu, Fucheng Yin, Heng Luo, Yonglei Zhang, Zhongwen Luo, Ningjie Cui, Lingyi Kong, Xiaobing Wang
Summary: EZH2 is often overexpressed in TNBC and other tumors, affecting tumor development and prognosis. The designed PROTACs molecule U3i precision targets EZH2 and shows good inhibitory effects on TNBC cells, inducing apoptosis without causing much damage to normal cells. U3i is a potential anticancer molecule for TNBC treatment.
EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
(2022)
Article
Chemistry, Organic
Fucheng Yin, Yifan Chen, Zhongwen Luo, Shang Li, Lingyi Kong, Xiaobing Wang
Summary: This study demonstrates the application of aryl halides in organic synthesis, specifically focusing on the usage of methyl 2-bromobenzoate and 2-nitrophenyl iodides as mild and effective bromination and iodination reagents. This efficient cascade catalysis method can be applied to the total synthesis of natural products Mafaicheenamine A and Claulamine A.
Article
Chemistry, Medicinal
Jiafu Leng, Yongjun Zhao, Ping Sheng, Yuanzheng Xia, Tingting Chen, Shifang Zhao, Shanshan Xie, Xiangyu Yan, Xiaobing Wang, Yong Yin, Lingyi Kong
Summary: The newly synthesized compound C3 exhibits potential anticancer activity by targeting tubulin to inhibit cancer cell proliferation and angiogenesis.
JOURNAL OF MEDICINAL CHEMISTRY
(2022)
Article
Biochemistry & Molecular Biology
Xinye Chen, Cheng Wang, Dehua Lu, Heng Luo, Shang Li, Fucheng Yin, Zhongwen Luo, Ningjie Cui, Lingyi Kong, Xiaobing Wang
Summary: Aberrant expression of EZH2 is frequently observed in cancers, but EZH2 inhibitors are not effective in treating solid tumors. Combination of EZH2 and BRD4 inhibitors may be a promising strategy. Therefore, a series of EZH2/BRD4 dual inhibitors were designed and synthesized. Compound 28 (KWCX-28) showed the most potential and inhibited cell proliferation, induced apoptosis, arrested cell cycle, and resisted H3K27ac upregulation. KWCX-28 is a potential dual EZH2/BRD4 inhibitor for treating solid tumors.
BIOORGANIC & MEDICINAL CHEMISTRY
(2023)
Article
Chemistry, Medicinal
Ningjie Cui, Shang Li, Yonglei Zhang, Fucheng Yin, Xinye Chen, Zhongwen Luo, Siyuan Wan, Xinxin Li, Lingyi Kong, Xiaobing Wang
Summary: This study synthesized and evaluated a series of structural analogues of Sibiriline and found that the optimal compound KWCN-41 can inhibit cell death, protect cell survival, and reduce inflammation levels. It is expected to be a potential drug for treating inflammatory diseases.
EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
(2023)
Article
Chemistry, Medicinal
Panhu Zhu, Tao Zhou, Hong Chen, Xingru Chen, Xiaobing Wang, Lingyi Kong, Minghua Yang
Summary: Triazoles have shown significant efficacy in treating fungal infections, but the increasing drug resistance limits their effectiveness. By designing well-crafted side chains, triazoles can have advantages such as higher potency and overcoming drug resistance. In this study, we synthesized fluconazole-core compounds and optimized their side chains to develop a potent antifungal agent, S-F24, which exhibited excellent broad-spectrum activity and maintained its effectiveness against multi-resistant Candida albicans.
JOURNAL OF MEDICINAL CHEMISTRY
(2023)
Review
Integrative & Complementary Medicine
Liu Xingchen, Wang Xiaobing
Summary: Parthenolide (PTL), derived from feverfew, has shown significant anticancer activity and has the potential to be a first-line drug. Structural modification strategies are recommended to enhance its anticancer activity. This review focuses on representative PTL derivatives and their mechanisms in cancer therapy.
CHINESE JOURNAL OF NATURAL MEDICINES
(2022)
Article
Chemistry, Medicinal
Dehua Lu, Cheng Wang, Lailiang Qu, Fucheng Yin, Shang Li, Heng Luo, Yonglei Zhang, Xingchen Liu, Xinye Chen, Zhongwen Luo, Ningjie Cui, Lingyi Kong, Xiaobing Wang
Summary: Aberrance of epigenetic modification is an important factor in hematological malignancies. There is promising potential in using HDAC and EZH2 dual inhibitors as a therapeutic strategy. Compound 20 exhibited excellent inhibitory activity against HDAC1 and EZH2, and also showed good antiproliferation activity against tumor cells, indicating its potential in treating hematological malignancies.
JOURNAL OF MEDICINAL CHEMISTRY
(2022)
Article
Chemistry, Multidisciplinary
Wan Peng, Qiaohong Liu, Fucheng Yin, Cunjian Shi, Limei Ji, Lailiang Qu, Cheng Wang, Heng Luo, Lingyi Kong, Xiaobing Wang
Summary: This method utilizes rhodium catalysis to achieve the olefination and deuteration of tetrahydrocarbazoles in water, showing a broad substrate scope and high efficiency. Practical applications are demonstrated through the synthesis of various evodiamine derivatives, making this environmentally friendly approach appealing for academic and industrial research.
Article
Chemistry, Medicinal
Shuang Mei, Su Jiang, Yuting Wang, Han Jing, Peng Yang, Miao-Miao Niu, Jindong Li, Kai Yuan, Yan Zhang
Summary: This study identifies a dual-targeting peptide, AP-1, that effectively inhibits variants of concern (VOCs) of SARS-CoV-2 without impairing host cell viability. The findings suggest that AP-1 could be a promising broad-spectrum agent for treating emerging VOCs of SARS-CoV-2.
EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
(2024)
Article
Chemistry, Medicinal
Hyeonjun Lee, Ju Yeon Lee, Hyunsoo Jang, Hye Young Cho, Minhee Kang, Sang Hyun Bae, Suin Kim, Eunji Kim, Jaebong Jang, Jin Young Kim, Young Ho Jeon
Summary: By using liquid chromatography-tandem mass spectrometry and nuclear magnetic resonance experiments, we identified new chemical moieties that bind to the target sites of the protein of interest, allowing for reversible binding and protein degradation. This method has the potential to expand the application of PROTAC technology.
EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
(2024)
Article
Chemistry, Medicinal
Yingying Li, Xiyou Du, Xinru Kong, Yuelin Fang, Zhijing He, Dongzhu Liu, Hang Wu, Jianbo Ji, Xiaoye Yang, Lei Ye, Guangxi Zhai
Summary: This study proposes a novel nanoplatform based on the autophagy cascade to overcome the obstacles in chemo-immunotherapy. The platform combines chemotherapy and starvation therapy to initiate pro-death autophagy and enhance antigen presentation, while also remodeling the immunosuppressive tumor microenvironment. Furthermore, the study discovers a new therapeutic direction for the respiration inhibitor 3-bromopyruvic acid (3BP) in cancer treatment. Overall, this study offers an opportunity to improve antitumor efficacy and boost immune responses.
EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
(2024)
Article
Chemistry, Medicinal
Bingsi Wang, Mingxu Ma, Yusen Dai, Pengfei Yu, Liang Ye, Wenyan Wang, Chunjie Sha, Huijie Yang, Yingjie Yang, Yunjing Zhu, Lin Dong, Shujuan Wei, Linlin Wang, Jingwei Tian, Hongbo Wang
Summary: Breast cancer is a common malignant tumor in women, and drug resistance remains a clinical challenge. In this study, a novel compound, G-5b, was developed with potent antagonistic and degradation activities comparable to the current drug fulvestrant. G-5b also showed improved stability and solubility. Mechanistically, G-5b engages the proteasome pathway to degrade ER, inhibiting the ER signaling pathway and inducing apoptosis and cell cycle arrest. In animal models, G-5b exhibited superior pharmacokinetics and pharmacodynamics properties. Overall, G-5b is a promising long-acting SERD worthy of further investigation and optimization.
EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
(2024)
Article
Chemistry, Medicinal
Karoline B. Waitman, Larissa C. de Almeida, Marina C. Primi, Jorge A. E. G. Carlos, Claudia Ruiz, Thales Kronenberger, Stefan Laufer, Marcia Ines Goettert, Antti Poso, Sandra V. Vassiliades, Vinicius A. M. de Souza, Monica F. Z. J. Toledo, Neuza M. A. Hassimotto, Michael D. Cameron, Thomas D. Bannister, Leticia Costa-Lotufo, Joa o A. Machado-Neto, Mauricio T. Tavares, Roberto Parise-Filho
Summary: A series of hybrid inhibitors combining pharmacophores of known kinase inhibitors and benzohydroxamate HDAC inhibitors were synthesized and evaluated for their anticancer activity and pharmacokinetic properties. Compounds 4d-f exhibited promising cytotoxicity against hematological cells and moderate activity against solid tumor models. Compound 4d showed potent inhibition of multiple kinase targets and had stable interactions with HDAC and members of the JAK family. These compounds showed selective cytotoxicity with minimal effects on non-tumorigenic cells and favorable pharmacokinetic profiles.
EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
(2024)
Article
Chemistry, Medicinal
Michal Sulik, Diana Fontinha, Dietmar Steverding, Szymon Sobczak, Michal Antoszczak, Miguel Prudencio, Adam Huczynski
Summary: This study describes the synthesis of the first-in-class ivermectin derivatives obtained through derivatization of the C13 position, along with the unexpected rearrangement of the macrolide ring. These derivatives show potential for antiparasitic activity and are important for the development of new antiparasitic agents.
EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
(2024)
Article
Chemistry, Medicinal
Jun Liu, Qiu-Xian Chen, Wen-Fu Wu, Dong Wang, Si -Yu Zhao, Jia-Hao Li, Yi-Qun Chang, Shao-Gao Zeng, Jia-Yi Hu, Yu-Jie Li, Jia-Xin Du, Shu-Meng Jiao, Hai-Chuan Xiao, Qiang Zhang, Jun Xu, Jian-Fu Zhao, Hai -Bo Zhou, Yong-Heng Wang, Jian Zou, Ping-Hua Sun
Summary: A new anti-infective drug strategy has been discovered to attenuate virulence and modulate inflammation caused by drug-resistant Pseudomonas aeruginosa infections. Compound 5f inhibits biofilm formation, macrophage migration, and inflammatory response induced by P. aeruginosa, showing potential as a novel candidate against drug-resistant infections.
EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
(2024)
Article
Chemistry, Medicinal
Liuzeng Chen, Ke Wang, Lingyun Wang, Wei Wang, Lifan Wang, Jia Li, Xiaohan Liu, Mengya Wang, Banfeng Ruan
Summary: In this study, a series of novel anti-inflammatory compounds were designed and synthesized based on the natural product pterostilbene skeleton. Among them, compound 8 showed the highest activity and exhibited its effects through inhibition of pro-inflammatory cytokines by blocking the NF-KB/MAPK signaling pathway. Compound 8 also demonstrated a good relieving effect on acute colitis in mice and showed good safety in acute toxicity experiments.
EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
(2024)
Article
Chemistry, Medicinal
Si-Min Liang, Gui-Bin Liang, Hui-Ling Wang, Hong Jiang, Xian-Li Ma, Jian-Hua Wei, Ri-Zhen Huang, Ye Zhang
Summary: A series of novel multi-target antitumor agents were designed, synthesized, and evaluated. Some compounds exhibited significant antitumor activity and one compound showed excellent efficacy, limited toxicity, and low resistance. Further mechanism studies revealed that the compound exerted antitumor effects through multiple pathways.
EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
(2024)
