Article
Chemistry, Medicinal
Xuefeng Liu, Hongmei Cui, Mi Li, Zuohu Chai, Haibo Wang, Xiaojie Jin, Fang Dai, Yongqi Liu, Bo Zhou
Summary: Compared to normal cells, cancer cells have intrinsic oxidative stress, making them more susceptible to the production of reactive oxygen species (ROS) by pro-oxidative anticancer agents (PAAs). However, PAAs also generate ROS in normal cells, limiting their clinical application due to narrow therapeutic window and toxic side effects. In this study, a selective ROS-generating agent, 2c, was designed using three series of dietary curcumin analogs. It showed potent selectivity in killing non-small cell lung cancer cells and inhibited tumor growth in mice. This work highlights a practical strategy of targeting thioredoxin reductase (TrxR) overexpressed in cancer cells to develop PAAs capable of generating ROS selectively.
EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
(2023)
Article
Biochemistry & Molecular Biology
Junmin Zhang, Yaxiong Chen, Jianguo Fang
Summary: The inhibition of thioredoxin reductase (TrxR) is vital for the development of antineoplastic drugs and radiosensitizers. In this study, it is found that micheliolide (MCL), derived from Michelia, not only induces oxidative stress-mediated apoptosis in HeLa cells but also sensitizes ionizing radiation (IR) treatment by targeting TrxR. Mechanistic studies reveal that MCL covalently binds to TrxR at position 498 to inhibit its biological function. Knockdown of TrxR enhances the cytotoxicity and radiation response induced by MCL, supporting the potential of MCL as a prospective radiosensitizer and cancer chemotherapeutic agent.
FREE RADICAL BIOLOGY AND MEDICINE
(2022)
Article
Biochemistry & Molecular Biology
Junmin Zhang, Qianhe Xu, Di Ma
Summary: This study found that beta-Lapachone can selectively kill human promyelocytic leukemia HL-60 cells by inhibiting TrxR and increasing oxidative stress. Overexpression of TrxR reduced the effectiveness of beta-Lapachone, while knockdown of the enzyme increased its cytotoxicity. This discovery contributes to the understanding of the mechanism of action of beta-Lapachone and supports its potential as an anticancer drug candidate.
FREE RADICAL BIOLOGY AND MEDICINE
(2022)
Article
Biochemistry & Molecular Biology
Miao Zhong, Lingzhen Chen, Yue Tao, Jintao Zhao, Bingbing Chang, Fang Zhang, Jingwen Tu, Wenqing Cai, Baoxin Zhang
Summary: Inhibiting TrxR activity to induce tumor cell apoptosis is a significant therapeutic strategy. Piperine, a natural product, has shown potential in suppressing tumor cell proliferation. To develop a compound with higher activity, we synthesized 22 Piperine analogs and found that B5 had significant cytotoxicity and inhibited TrxR activity. Further investigation revealed B5's selective inhibition of TrxR activity by binding to Sec residues, leading to cellular oxidative stress and apoptosis.
BIOORGANIC CHEMISTRY
(2023)
Article
Biochemistry & Molecular Biology
Dongzhu Duan, Yanru Wang, Dabo Pan, Xiaojie Jin, Yunyun Yan, Peng Song, Le Wang, Jian Xiao, Zihua Wang, Xiaoling Wang
Summary: Sinomenine, a new inhibitor for TrxR, demonstrates anticancer activity by decreasing thiols content, increasing reactive oxygen species levels, and inducing oxidative stress-mediated cancer cell apoptosis. Knockdown of TrxR1 enhances cell sensitivity to sinomenine.
BIOORGANIC CHEMISTRY
(2022)
Article
Biochemistry & Molecular Biology
Zhongren Xu, Jianqiang Xu, Shibo Sun, Wei Lin, Yongming Li, Qiuyue Lu, Fuwei Li, Zhibin Yang, Yunlong Lu, Wukun Liu
Summary: Immunogenic cell death (ICD) is an immunostimulatory form of cell death that can reengage the tumor-specific immune system. This study identified micheliolide as a potential ICD inducer and showed that its effects were mediated by the generation of reactive oxygen species (ROS) and endoplasmic reticulum stress (ERS).
Article
Biochemistry & Molecular Biology
Hecheng Wang, Shibo Sun, Yan Ren, Rui Yang, Jianli Guo, Yu Zong, Qiuxian Zhang, Jing Zhao, Wei Zhang, Weiping Xu, Shui Guan, Jianqiang Xu
Summary: Cadmium is a toxic heavy metal that poses severe hazards to human health. Selenium has been found to reduce cadmium toxicity, but it is unclear whether this protective effect is related to selenoproteins in nerve cells. This study found that cadmium inhibited the activity of selenoprotein thioredoxin reductase 1 (TrxR1) and decreased its expression, causing cellular oxidative stress. Selenium supplementation ameliorated cadmium-induced cytotoxicity by increasing cellular TrxR activity and upregulating TrxR1 protein level. This study sheds light on the mechanism of cadmium-induced cytotoxicity and the role of TrxR1 in selenium-mitigated cytotoxicity of cadmium in neuroblast cells.
BIOLOGICAL TRACE ELEMENT RESEARCH
(2023)
Article
Biochemistry & Molecular Biology
Junmin Zhang, Qianhe Xu, Hong-Ying Yang, Minghao Yang, Jianguo Fang, Kun Gao
Summary: Natural products have diverse structures and novelty, leading to unique physiological activities and new action mechanisms, making them important sources for innovative drugs and lead compounds. This study demonstrates that Santamarine targets TrxR to weaken cellular antioxidative function, inducing tumor cell oxidative stress-mediated apoptosis. TrxR plays a key role in the physiological effect of Santamarine on cells, revealing a previously unrecognized mechanism of antitumor activity.
FRONTIERS IN MOLECULAR BIOSCIENCES
(2021)
Article
Agriculture, Multidisciplinary
Ya-Long Zheng, Zhi-Shan Tu, Hong-Mei Cui, Shuai Yan, De-Chen Duan, Wei Tang, Fang Dai, Bo Zhou
Summary: In this study, a redox-based strategy was proposed to intervene in the reprogramming of cancer cell energy metabolism by inhibiting mitochondrial antioxidant enzyme TrxR2 to generate reactive oxygen species (ROS). The strategy induced a preferential energy crisis and selectively killed cancer cells with high antitumor efficacy in vivo.
JOURNAL OF AGRICULTURAL AND FOOD CHEMISTRY
(2022)
Article
Pharmacology & Pharmacy
Gaopan Dong, Xiaohan Ye, Shumei Wang, Wenhua Li, Rong Cai, Lupei Du, Xiaodong Shi, Minyong Li
Summary: This study reports a novel TrxR inhibitor Au-24 and its inhibitory ability to hepatocellular carcinoma in vitro and in vivo. Au-24 suppresses the proliferation of HepG2 cells through regulating multiple signaling pathways and inducing oxidative stress. In vivo experiments demonstrate that Au-24 is more effective than the traditional drug AA1 in inhibiting tumor growth.
PHARMACOLOGICAL RESEARCH
(2022)
Article
Pharmacology & Pharmacy
Xuefeng Liu, Yihua Wang, Yalong Zheng, Dechen Duan, Fang Dai, Bo Zhou
Summary: This study found that 6-DHS, a compound found in ginger, has antiangiogenic activity and its ability to inhibit angiogenesis is dependent on the presence and number of Michael acceptor units. 6-DHS inhibits angiogenesis by generating reactive oxygen species, which is important for preventing tumor growth and metastasis.
EUROPEAN JOURNAL OF PHARMACOLOGY
(2022)
Article
Biochemistry & Molecular Biology
Xiuli Chen, Shibo Sun, Sheng Huang, Han Yang, Qing Ye, Lin Lv, Yanshan Liang, Jinjun Shan, Jianqiang Xu, Wukun Liu, Tonghui Ma
Summary: Gold(I) selenium N-heterocyclic carbene complexes H7 and H8 exhibit stronger antibacterial effects against multidrug-resistant Gram-negative bacteria by irreversibly inhibiting the activity of TrxR and inducing oxidative stress. In vivo experiments demonstrate that H7 and H8 have better antibacterial activity than auranofin, and can promote wound healing and prolong the survival time of patients with Carbapenem-resistant Acinetobacter baumannii induced peritonitis.
Article
Pharmacology & Pharmacy
Ines Marmol, Javier Quero, Paula Azcarate, Elena Atrian-Blasco, Carla Ramos, Joana Santos, Maria Concepcion Gimeno, Maria Jesus Rodriguez-Yoldi, Elena Cerrada
Summary: This paper describes the synthesis of new N-heterocyclic carbene (NHC) gold(I) derivatives and their screening for antimicrobial and anticancer activities. The compounds showed greater activity against bacteria than against colon cancer cells. The mechanism of action of one of the compounds, 1b, was evaluated and it was found to inhibit dihydrofolate reductase (DHFR) activity in E. coli cells and cause structural changes in the bacteria.
Article
Biochemistry & Molecular Biology
Xia Ying Cui, Sun Hyang Park, Woo Hyun Park
Summary: Auranofin, a thioredoxin reductase inhibitor, has anti-cancer effects in lung cancer cells by increasing ROS levels and depleting GSH.
Article
Biochemistry & Molecular Biology
Yue Zhang, Shibo Sun, Weiping Xu, Rui Yang, Yijia Yang, Jianli Guo, Kun Ma, Jianqiang Xu
Summary: Shikonin induces cancer cell death by inhibiting the antioxidant activity of selenoenzyme thioredoxin reductase 1 (TrxR1). Shikonin modification of TrxR1 leads to the production of superoxide anions and ROS-dependent necroptosis. KEAP1-mutant NSCLC cells exhibit resistance to shikonin, but NADPH depletion or inhibition of glucose-6-phosphate dehydrogenase (G6PD) can overcome this resistance.
FREE RADICAL BIOLOGY AND MEDICINE
(2022)
Review
Chemistry, Medicinal
Ying Sun, Yunlong Lu, Mianli Bian, Zhibin Yang, Xiaoyan Ma, Wukun Liu
Summary: The Pt(II) and Au(III) Schiff-base complexes as potential antitumor agents have shown remarkable biological activities and good stability. They act through different mechanisms, providing a feasible solution for improving the side effects of metal chemotherapy.
EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
(2021)
Review
Chemistry, Inorganic & Nuclear
Sai Zhao, Zhibing Yang, Guizhi Jiang, Sheng Huang, Mianli Bian, Yunlong Lu, Wukun Liu
Summary: NHCs have been introduced as a new platform for the development of anticancer metal complexes, with platinum NHC complexes showing comparable activities to cisplatin and exhibiting different mechanisms of action, including the induction of biochemical hallmarks of immunogenic cell death (ICD) as a type II ICD inducer. These features make them promising candidates in the field of anticancer research.
COORDINATION CHEMISTRY REVIEWS
(2021)
Review
Pharmacology & Pharmacy
Yuanhao Liu, Yunlong Lu, Zhongren Xu, Xiaoyan Ma, Xiuli Chen, Wukun Liu
Summary: Multidrug resistance is a significant issue in antibiotic clinical application, leading researchers to explore the potential of auranofin and other gold complexes as antibacterial agents. These advances offer a new perspective on the treatment of bacterial infections.
DRUG DISCOVERY TODAY
(2022)
Article
Chemistry, Medicinal
Mianli Bian, Rong Fan, Zhibin Yang, Yanan Chen, Zhongren Xu, Yunlong Lu, Wukun Liu
Summary: The research introduces a new Pt(II)-NHC complex termed 2c, which exhibits potent anticancer activities in HCC cells and can induce cell death, potentially activating genes.
The study suggests that 2c is a type II ICD inducer, capable of inducing cell death in HCC cells by causing endoplasmic reticulum stress and generating reactive oxygen species.
JOURNAL OF MEDICINAL CHEMISTRY
(2022)
Editorial Material
Chemistry, Multidisciplinary
Lei Guo, Jyotirmayee Mohanty, Wukun Liu, Taner Yonar, Hongyan Sun, Tsuyoshi Minami, Jafar Soleymani, Basem Moosa, Qianxiong Zhou
FRONTIERS IN CHEMISTRY
(2021)
Article
Chemistry, Medicinal
Qimeng Xiao, Yuanhao Liu, Guizhi Jiang, Yuan Liu, Yan Huang, Wukun Liu, Zhenbo Zhang
Summary: In this study, a novel gold compound (Complex 10) was designed and synthesized, which showed strong anti-EC activity and outperformed the existing drug auranofin in cell, organoid, and xenograft models. Mechanistically, Complex 10 suppressed the expression of key proteins involved in EC development. These findings suggest the potential of Complex 10 as a treatment option for EC.
EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
(2022)
Article
Chemistry, Medicinal
Miao Luo, Xiaoyan Ma, Weiling Jiang, Jun Zhang, Wukun Liu, Shuang Wei, Huiguo Liu
Summary: The upregulation of lipid metabolism is a common characteristic change in tumor cells. This study investigated the effects of phosphanegold(I) thiolate complexes on the regulation of lipid metabolism in lung cancer cells. The complexes inhibited lung cancer cell growth, impaired mitochondrial structure and function, reduced endogenous fatty acid and phospholipid synthesis, and induced apoptosis in lung cancer cells.
EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
(2022)
Article
Biochemistry & Molecular Biology
Zhongren Xu, Jianqiang Xu, Shibo Sun, Wei Lin, Yongming Li, Qiuyue Lu, Fuwei Li, Zhibin Yang, Yunlong Lu, Wukun Liu
Summary: Immunogenic cell death (ICD) is an immunostimulatory form of cell death that can reengage the tumor-specific immune system. This study identified micheliolide as a potential ICD inducer and showed that its effects were mediated by the generation of reactive oxygen species (ROS) and endoplasmic reticulum stress (ERS).
Article
Biochemistry & Molecular Biology
Xiuli Chen, Shibo Sun, Sheng Huang, Han Yang, Qing Ye, Lin Lv, Yanshan Liang, Jinjun Shan, Jianqiang Xu, Wukun Liu, Tonghui Ma
Summary: Gold(I) selenium N-heterocyclic carbene complexes H7 and H8 exhibit stronger antibacterial effects against multidrug-resistant Gram-negative bacteria by irreversibly inhibiting the activity of TrxR and inducing oxidative stress. In vivo experiments demonstrate that H7 and H8 have better antibacterial activity than auranofin, and can promote wound healing and prolong the survival time of patients with Carbapenem-resistant Acinetobacter baumannii induced peritonitis.
Article
Chemistry, Multidisciplinary
Yunlong Lu, Yuanhao Liu, Zhenlin Liang, Xiaoyan Ma, Lijuan Liu, Zhenfan Wen, Iogann Tolbatov, Alessandro Marrone, Wukun Liu
Summary: In this study, a bioorthogonal catalyst, Pd(PPh3)2Cl2, was used to convert the stable N-heterocyclic carbene (NHC)-gold(I)-alkyne complex 5 to its active species in biological environments. The active species effectively inhibits thioredoxin reductase (TrxR) and exhibits significant anticancer bioactivity in hepatocellular carcinoma (HCC).
CHINESE CHEMICAL LETTERS
(2023)
Article
Chemistry, Medicinal
Yunlong Lu, Chao Liu, Xin Wang, Lijuan Liu, Zhihao Zhao, Zhenlin Liang, Yuanhao Liu, Zhenfan Wen, Qianming Du, Wukun Liu
Summary: Although endocrine therapies have shown good responses in ER+ breast cancer patients, drug resistance remains an issue. Researchers developed a new class of orally bioavailable fluorine-substituted SERDs, one of which (27b) shows excellent pharmacokinetic profiles and potential as an orally available SERD for clinical use.
EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
(2023)
Article
Chemistry, Medicinal
Zhongren Xu, Qiuyue Lu, Min Shan, Guizhi Jiang, Yuanhao Liu, Zhibin Yang, Yunlong Lu, Wukun Liu
Summary: Inflammation promotes ovarian cancer development, and chemoresistance is a major challenge in its treatment. A series of gold(I) complexes derived from NSAIDs were synthesized, and complex B3 (Npx-Au) exhibited higher antitumor activity than cisplatin and other gold(I) complexes. Npx-Au induced oxidative stress and the DAMPs process by inhibiting TrxR activity. Mechanistic studies showed simultaneous downregulation of COX-2 and PD-L1 after Npx-Au treatment. Interestingly, in vivo experiments demonstrated that Npx-Au treatment stimulated immune response by reducing PD-L1 expression, inducing DC maturation, and increasing T cell infiltration. Overall, Npx-Au elicited immunogenic cell death and showed promise as a strategy for chemotherapy combined with immunotherapy in treating ovarian cancer.
JOURNAL OF MEDICINAL CHEMISTRY
(2023)
Article
Chemistry, Medicinal
Zhenlin Liang, Lijuan Liu, Yanyu Zhou, Wukun Liu, Yunlong Lu
Summary: Breast cancer, the most prevalent cancer in women, has been treated with endocrine therapy drugs, such as tamoxifen, since 1977. However, drug resistance and side effects remain challenges in the treatment of ER+ breast cancer. Metal complexes, particularly platinum complexes, have shown promising antitumor activities and may provide new opportunities for the treatment of ER+ breast cancer.
JOURNAL OF MEDICINAL CHEMISTRY
(2023)
Article
Chemistry, Medicinal
Zhibin Yang, Mianli Bian, Lin Lv, Xingyu Chang, Zhenfan Wen, Fuwei Li, Yunlong Lu, Wukun Liu
Summary: In this study, a series of novel NHC-Au(I) complexes derived from 4,5-diarylimidazole and glycyr-rhetinic acid (GA) were designed and synthesized. Among them, complex 4C exhibited excellent tumor targeting and antitumor activity, inducing immunogenic cell death (ICD) in hepatocellular carcinoma (HCC) cells. Furthermore, 4C effectively inhibited TrxR enzyme activity, increased reactive oxygen species (ROS) expression, disrupted redox homeostasis, caused mitochondrial dysfunction and endoplasmic reticulum stress (ERS), and led to the release of damage-associated molecular patterns (DAMPs) in HCC cells. Importantly, 4C showed a strong ICD-inducing effect in a vaccination mouse model and activated antitumor immunity in a tumor-bearing C57BL/6 mouse model, consistent with the in vitro results. In conclusion, Au(I) complexes with HCC-targeted capability have the potential for effective tumor immunotherapy.
JOURNAL OF MEDICINAL CHEMISTRY
(2023)
Review
Chemistry, Multidisciplinary
Yunlong Lu, Xiaoyan Ma, Xingyu Chang, Zhenlin Liang, Lin Lv, Min Shan, Qiuyue Lu, Zhenfan Wen, Ronald Gust, Wukun Liu
Summary: Metal complexes, particularly gold complexes, have shown significant antitumor activities and potential as alternative chemotherapy agents due to their different mechanism of action and ability to induce immunogenic cell death. This review comprehensively summarizes the recent progress and mechanism of action of gold (I) and gold (III) complexes.
CHEMICAL SOCIETY REVIEWS
(2022)
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)
