Article
Chemistry, Multidisciplinary
Ahmed A. Noser, Ihsan A. Shehadi, Aboubakr H. Abdelmonsef, Maha M. Salem
Summary: A series of novel pyrazolinone chalcones were synthesized and screened for their ability to inhibit cancer proliferation and metastasis. Compound 6b exhibited the highest binding energy and most effective cytotoxic impact, inhibiting the PI3K/Akt and Raf-1/ERK1/2 signaling pathways.
Article
Cell Biology
Tao Ma, Yan Chen, Zhi-Gang Yi, Jia Liu, Yan-Hong Li, Jun Bai, Wen-Ting Tie, Mei Huang, Xiao-Feng Zhu, Ji Wang, Juan Du, Xiu-Qin Zuo, Qin Li, Fan-Li Lin, Liu Tang, Jing Guo, Hong-Wen Xiao, Qian Lei, Xiao-Li Ma, Li-Juan Li, Lian-Sheng Zhang
Summary: This study reveals that NORAD acts as an oncogene in multiple myeloma and exerts its effects through the BMP6/P-ERK1/2 axis. Knockdown of NORAD promotes apoptosis and induces cell cycle arrest, while inhibiting cell proliferation in multiple myeloma.
CELLULAR SIGNALLING
(2022)
Article
Chemistry, Organic
Kapil Kumar Goel, Satyendra Kumar Rajput, Prince Prashant Sharma, Monalisa Mukherjee, Rajeev Kharb
Summary: Malignant behavior and abnormal cellular functions in cancer have posed challenges for treatment. Two compounds with potent cytotoxicity were discovered, targeting tubulin polymerization for cancer treatment.
Article
Chemistry, Inorganic & Nuclear
Li Hong-Xia, Qian Yu-Mei, Xu Li-Sheng
Summary: This study focused on designing and synthesizing a series of quinazoline derivatives targeting EGFR, evaluating their anticancer activity and apoptosis-inducing capacity on various tumor cell lines. The results showed that compound 4a exhibited the strongest anticancer activity and apoptosis-inducing ability, indicating its potential as a promising anticancer drug targeting EGFR.
CHINESE JOURNAL OF STRUCTURAL CHEMISTRY
(2021)
Article
Chemistry, Multidisciplinary
Marwa F. Ahmed, Amany S. Khalifa, Emad M. Eed
Summary: Novel quinazoline derivatives show promising antitumor potential against HCT116 and MCF-7 cell lines, with the most active product exhibiting enzyme inhibitory activity against VEGFR-2. It triggers apoptosis and G2/M phase cell cycle arrest, as well as upregulates BAX and caspase-3 expression while downregulating Bcl-2 expression based on gene expression data.
RUSSIAN JOURNAL OF GENERAL CHEMISTRY
(2021)
Article
Chemistry, Multidisciplinary
Rui Chen, Ziyue Wang, Lihong Liu, Zhengying Pan
Summary: The study developed a series of photocaged ERK inhibitors which can be selectively activated by UV irradiation to release a highly potent ERK inhibitor. The inhibitor demonstrated anticancer activity in multiple cancer cell lines and a zebrafish xenograft model, providing a new strategy for precise cancer therapy.
CHEMICAL COMMUNICATIONS
(2022)
Article
Food Science & Technology
Hyeon-Ju Lee, Se-Young Oh, Inho Jo
Summary: This study found that Zearalenone induces endothelial cell apoptosis through activation of an ERK1/2/p53/caspase 3 signaling pathway via release of Ca2+ from the endoplasmic reticulum, independent of reactive oxygen species production and estrogen receptor activation.
Article
Oncology
Jianyou Gu, Wenjie Huang, Junfeng Zhang, Xianxing Wang, Tian Tao, Ludi Yang, Yao Zheng, Songsong Liu, Jiali Yang, Liwei Zhu, Huaizhi Wang, Yingfang Fan
Summary: TMPRSS4 is upregulated in pancreatic cancer and associated with poor prognosis, serving as an independent risk factor in PDAC. It promotes cellular proliferation and inhibits apoptosis, possibly through activating the ERK1/2 signaling pathway. This study suggests TMPRSS4 as a potential prognostic biomarker and therapeutic target for pancreatic cancer.
FRONTIERS IN ONCOLOGY
(2021)
Article
Biochemistry & Molecular Biology
Cai-Wen Fan, Mei-Shan Li, Xi-Xi Song, Li Luo, Jing-Chen Jiang, Jia-Zi Luo, Heng-Shan Wang
Summary: A series of 2-oximino-2-indolylacetamide derivatives were designed, synthesized and evaluated for their anti-tumour effects. Among them, 4d exhibited the most potent antiproliferative effect in vitro on the tested human cancer cells. It induced cell apoptosis, mitochondrial dysfunction, autophagosome formation, and cell death through ferroptosis. It also activated ROS/MAPK and inhibited AKT/mTOR and STAT3 signaling pathways.
BIOORGANIC & MEDICINAL CHEMISTRY
(2023)
Review
Chemistry, Organic
Parul Grover, Monika Bhardwaj, Garima Kapoor, Lovekesh Mehta, Roma Ghai, K. Nagarajan
Summary: Heterocyclic compounds, especially nitrogen-containing heterocycles like quinazoline, play a significant role in medicinal chemistry due to their diverse biological activities. Quinazoline is an important pharmacophore in medicinal chemistry with wide spectrum of biological properties and demonstrated anticancer activity against different types of cancer. Recent advances in quinazoline-based molecules as anticancer agents are highlighted, including both in-vitro and in-vivo models used in research.
CURRENT ORGANIC CHEMISTRY
(2021)
Article
Biochemistry & Molecular Biology
Mei Li, Daoping Wang, Qing Li, Fang Luo, Ting Zhong, Hongshan Wu, Liang Xiong, Meitao Yuan, Mingzhi Su, Yanhua Fan
Summary: In this study, new 6-(imidazo[1,2-a]pyridin-6-yl)quinazoline derivatives were designed, synthesized, and characterized. In the in vitro anticancer assay, most of the synthetic compounds showed strong inhibitory activity against various tumor cell lines. Compound 13k exhibited the highest potency, with IC50 values ranging from 0.09 μM to 0.43 μM against all tested cell lines. Furthermore, compound 13k induced cell cycle arrest and apoptosis in HCC827 cells by inhibiting PI3Kα.
INTERNATIONAL JOURNAL OF MOLECULAR SCIENCES
(2023)
Article
Oncology
Zeinab Faghfoori, Mohammad Hasan Faghfoori, Amir Saber, Azimeh Izadi, Ahmad Yari Khosroushahi
Summary: The study showed that different species of bifidobacteria exhibit anticancer activity on colorectal cancer cells by regulating the expression of anti-apoptotic and pro-apoptotic genes, potentially contributing to the prevention and treatment of colorectal cancer. Further research is needed to fully understand the mechanisms behind apoptosis induction by bifidobacteria species.
CANCER CELL INTERNATIONAL
(2021)
Article
Plant Sciences
Xu Chen, Zhiyu Zhang, Xiaowei Zhang, Zhi Jia, Jun Liu, Xinpei Chen, Aiqing Xu, Xue Liang, Guangping Li
Summary: This study found that paeonol (PAE) improves cardiac function in mice with heart failure caused by transverse aortic constriction (TAC) by regulating the ERK1/2/JNK pathway, and it has a protective effect on myocardial injury and apoptosis.
PHARMACEUTICAL BIOLOGY
(2022)
Article
Biochemistry & Molecular Biology
Ashish Ranjan Dwivedi, Vijay Kumar, Vikash Prashar, Akash Verma, Naveen Kumar, Jyoti Parkash, Vinod Kumar
Summary: A series of morpholine substituted quinazoline derivatives have been synthesized and evaluated for their cytotoxic potential against several cancer cell lines. Among them, AK-3 and AK-10 showed significant cytotoxic activity against three different cell lines and were found to inhibit cell proliferation in the G1 phase of the cell cycle through apoptosis.
RSC MEDICINAL CHEMISTRY
(2022)
Article
Cardiac & Cardiovascular Systems
Ziying Chen, Flora Gordillo-Martinez, Lei Jiang, Pengcheng He, Wanzi Hong, Xuebiao Wei, Katherine A. Staines, Vicky E. Macrae, Chunxiang Zhang, Danqing Yu, Xiaodong Fu, Dongxing Zhu
Summary: The study suggests that zinc may act as a novel inhibitor of CAVD by regulating GPR39-dependent ERK1/2 signaling pathway to inhibit cell calcification, and zinc transporter ZIP13 and ZIP14 play important roles in regulating cell calcification and osteogenic differentiation. Zinc supplementation could be a potential therapeutic strategy for CAVD.
CARDIOVASCULAR RESEARCH
(2021)
Review
Engineering, Environmental
Caiyan Yue, Long Chen, Heng Zhang, Jinshu Huang, Hao Jiang, Hu Li, Song Yang
Summary: Water pollution is a pressing global environmental issue due to the presence of toxic organic pollutants. Photocatalysis, particularly using metal-organic frameworks (MOFs), has shown great promise for organic pollutant removal in wastewater treatment. This review summarizes recent advances in MOF-based photocatalysts, including preparation strategies, modification techniques, and applications for organic pollutant degradation. The working mechanisms, heterojunctions, and key parameters affecting the photocatalytic degradation process are also discussed. The future outlook and challenges of MOF materials for removing organic pollutants from water are emphasized.
ENVIRONMENTAL SCIENCE-WATER RESEARCH & TECHNOLOGY
(2023)
Article
Chemistry, Multidisciplinary
Yujiao Zhang, Zhao Hu, Heng Zhang, Hu Li, Song Yang
Summary: A novel Covalent organic skeleton/metal oxide (COF/MOx) Z scheme heterojunction was constructed for selective oxidation of nitric oxide (NO). The optimized COF/TiO2 catalyst exhibited excellent NO removal rate (64.5%) under visible-light irradiation due to improved light absorption, efficient separation of photoexcited electron-hole pairs, and activation of O-2 by uniform COF coating. The selectivity towards nitrate (NO3-) was improved to 99.9% by enhancing the generation of superoxide radicals as the main reactive species and limiting the production of intermediate nitrogen dioxide (NO2). This study demonstrates the potential of the Z scheme heterojunction for universal applications.
ADVANCED FUNCTIONAL MATERIALS
(2023)
Article
Chemistry, Physical
Zhengyi Li, Peng Zhou, Min Zhou, Hao Jiang, Hu Li, Shengqi Liu, Heng Zhang, Song Yang, Zehui Zhang
Summary: In this study, a new bifunctional indium hydroxide material was developed for the high-efficiency synthesis of urea from CO2 and nitrogenous pollutants. The material, with dual active sites and facet and defect engineering, showed selective catalytic activity for the conversion of CO2 and NO3-, leading to improved urea synthesis efficiency.
APPLIED CATALYSIS B-ENVIRONMENT AND ENERGY
(2023)
Article
Engineering, Environmental
Hongmei Xiang, Jiao Meng, Wubin Shao, Dan Zeng, Jin Ji, Peiyi Wang, Xiang Zhou, Puying Qi, Liwei Liu, Song Yang
Summary: The excessive use and eco-unfriendly behavior of traditional pesticide formulations have serious drawbacks. In this study, a scalable and sustainable biopolymer-based core-shell nanocarrier loaded with an anti-viral candidate agent was developed for plant disease management. The nanocarrier exhibited enhanced UV resistance, improved foliar surface wettability, and activated host plant defense responses.
CHEMICAL ENGINEERING JOURNAL
(2023)
Article
Engineering, Environmental
Xiang Tan, Hongguo Wu, Heng Zhang, Hu Li, Song Yang
Summary: A renewed heterogeneous catalyst, PtSA/NC-AMP, consisting of both Pt single atoms and nanoclusters supported by Al(PO3)3, was developed for efficient hydrogenative scission of alkyl/aryl C-O bonds in lignin derivatives and oxygenated aryl/alkyl compounds, resulting in the formation of arenes and alkanes, respectively. The relay catalytic process based on the finite size effect, where Pt single atoms and nanoclusters play different roles, contributes to the excellent reactivity of PtSA/NC-AMP. Furthermore, the size-dependent strong metal-support interaction of Pt-Al(PO3)3 enhances the reactivity and stability of PtSA/NC-AMP. This study provides a reference for the multi-step upgrading of biomass involving targeted alkyl/aryl C-O bond cleavage.
CHEMICAL ENGINEERING JOURNAL
(2023)
Article
Biochemistry & Molecular Biology
Puying Qi, Na Wang, Taihong Zhang, Yumei Feng, Xiang Zhou, Dan Zeng, Jiao Meng, Liwei Liu, Linhong Jin, Song Yang
Summary: Anti-virulence strategies are effective for controlling bacterial diseases by targeting virulence factors. In this study, a series of dehydroabietic acid derivatives were synthesized and evaluated for their antibacterial activity. Compound 2b showed promising antibacterial activity against Xanthomonas oryzae pv. oryzae and effective control of bacterial leaf blight in rice. It also suppressed various virulence factors. These compounds can serve as lead compounds for developing novel bactericides.
INTERNATIONAL JOURNAL OF MOLECULAR SCIENCES
(2023)
Article
Agriculture, Multidisciplinary
Dan Zeng, Shuai-Shuai Liu, Wu-Bin Shao, Tai-Hong Zhang, Pu-Ying Qi, Hong-Wu Liu, Xiang Zhou, Li-Wei Liu, Heng Zhang, Song Yang
Summary: This study synthesized 35 new 1,3,4-oxadiazole derivatives and evaluated their anti-phytopathogenic activities. Compound C-7 showed excellent antibacterial activity in vitro and acceptable activity in vivo against rice bacterial leaf blight. Moreover, C-7 could indirectly reduce the inducible expression of host SWEET genes, alleviating nutrient supply in the infection process of phytopathogenic bacteria. The study highlights the potential of 1,3,4-oxadiazole-based agrochemicals in controlling plant bacterial diseases.
JOURNAL OF AGRICULTURAL AND FOOD CHEMISTRY
(2023)
Article
Agronomy
Bin-Xin Yang, Zhen-Xing Li, Shuai-Shuai Liu, Jie Yang, Pei-Yi Wang, Hong-Wu Liu, Xiang Zhou, Li-Wei Liu, Zhi-Bing Wu, Song Yang
Summary: Two series of novel cinnamic acid derivatives were designed and synthesized to explore alternative agrochemicals for controlling plant virus and bacterial diseases. The bioassay results showed that these derivatives exhibited excellent antiviral competence, with compound A(5) demonstrating remarkable protective effects against tobacco mosaic virus. This research provides a foundation for the practical application of cinnamic acid derivatives in pesticide exploration.
PEST MANAGEMENT SCIENCE
(2023)
Article
Energy & Fuels
Jinyu Tan, Dayong Yu, Junfa Yuan, Hongguo Wu, Hangyu Luo, Heng Zhang, Xiaobing Li, Hu Li, Song Yang
Summary: A novel ternary deep eutectic solvent (DES) was designed for wheat straw pretreatment, which achieved non-condensed lignin and high-yield fermentable sugars. The introduction of ethylene glycol into the DES protected lignin structure and improved enzymatic digestibility of cellulose. Trichosporon cutaneum cultivated in the waste liquid and residue hydrolysate produced 8.7 g microbial lipid per 100 g wheat straw, surpassing previous reports.
Article
Biochemistry & Molecular Biology
Zhenxing Li, Binxin Yang, Yue Ding, Jiao Meng, Jinhong Hu, Xiang Zhou, Liwei Liu, Zhibing Wu, Song Yang
Summary: Plant diseases caused by malignant and refractory phytopathogenic viruses have been effectively inhibited by novel eugenol derivatives targeting the tobacco mosaic virus helicase. Compound 2 t showed superior binding capability and impressive anti-viral activity, outperforming commercial drugs.
INTERNATIONAL JOURNAL OF BIOLOGICAL MACROMOLECULES
(2023)
Article
Agriculture, Multidisciplinary
Wu-Bin Shao, Rong-Shuang Luo, Jiao Meng, Xiao-Kang Lv, Hong-Mei Xiang, Wan-Lin Xiao, Xiang Zhou, Li-Wei Liu, Zhi-Bing Wu, Song Yang
Summary: Phenothiazine derivatives showed excellent bioactivity against different bacteria and demonstrated potential as pesticide candidates for plant diseases. Compound C-2 had high effectiveness against rice leaf blight, outperforming commonly used pesticides.
JOURNAL OF AGRICULTURAL AND FOOD CHEMISTRY
(2023)
Article
Agronomy
Zhen-Xing Li, Jin-Hong Hu, Rong-Shuang Luo, Tai-Hong Zhang, Yue Ding, Xiang Zhou, Li-Wei Liu, Zhi-Bing Wu, Song Yang
Summary: This study established an efficient screening platform based on natural alkaloids to discover novel compounds targeting TMV helicase. Rutaecarpine from Evodia rutaecarpa (Juss.) Benth showed excellent TMV helicase inhibitory properties (Kd = 1.1 μm, IC50 = 227.24 μm) and demonstrated strong anti-TMV activity. Molecular docking and dynamic simulations revealed that Rutaecarpine could stably bind to the active pockets of the helicase through hydrogen bonding and hydrophobic interactions with low binding energy (ΔG(bind) = -17.8 kcal/mol).
PEST MANAGEMENT SCIENCE
(2023)
Article
Chemistry, Inorganic & Nuclear
Li-Long Zhang, Yaqiong Su, Dandan Chen, Hongguo Wu, Feng Xu, Hu Li, Song Yang
Summary: NOx is used as an oxidant for direct selective conversion of methane into methanol, but the interconversion of NOx compounds and the easy formation of O-2 have posed challenges in determining its effectiveness. This study proposes a new cooperative multi-functional mechanism strategy using dual oxidants (NO and N2O) to enhance catalytic performance. Compared with normal mechanisms, this strategy shows stronger CH4 adsorption and thermodynamic favorability. It is expected to inspire further research in DSCMM and other catalytic systems.
INORGANIC CHEMISTRY FRONTIERS
(2023)
Article
Chemistry, Physical
Li-Long Zhang, Ji Zheng, Jinxing Gu, Zhuochun Huang, Linguo Lu, Hu Li, Zhongfang Chen, Song Yang
Summary: This study investigated 11 phosphotungstic acid-supported single-atom catalysts (SACs) and found that Os-1/PTA SACs exhibited superior catalytic activity for the purification of methane and hydrogen, with the ease of oxidation following the CO > H-2 > CH4 order. It selectively removed CO in water and MeOH without consuming H-2, due to strong Os-PTA interactions and charge transfer mechanism.
JOURNAL OF MATERIALS CHEMISTRY A
(2023)
Review
Polymer Science
Wenfeng Zhao, Qinmei Ge, Hu Li, Nan Jiang, Shangwei Chen, Song Yang, Hang Cong
Summary: Using organic polymers as catalysts for CO2 photoreduction is a highly promising approach to addressing energy and environmental issues, due to their outstanding CO2 adsorption capacity, photochemical performance, and tunable structure.
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)
