Article
Agriculture, Multidisciplinary
Luwei Li, Deyou Yang, Heng Li, Guangyou Chen, Peng Lei, Yanqing Gao, Juntao Feng
Summary: Developing fungicides from active botanical skeletons is an effective method to combat plant pathogens with resistance. In this study, novel a-methylene-?-butyrolactone (MBL) derivatives were designed based on the antifungal molecule carabrone found in Carpesium macrocephalum. These compounds were synthesized and evaluated for their inhibitory activity against pathogenic fungi. Compound 38 exhibited the highest activity, surpassing the commercial fungicide famoxadone. The mode of action was identified to involve cell deformation, reduction of intracellular mitochondria, thickening of the cell wall, and increased cell membrane permeability.
JOURNAL OF AGRICULTURAL AND FOOD CHEMISTRY
(2023)
Article
Chemistry, Medicinal
Dmitry A. Makarov, Sergey D. Negrya, Maxim V. Jasko, Inna L. Karpenko, Pavel N. Solyev, Vladimir O. Chekhov, Dmitry N. Kaluzhny, Olga V. Efremenkova, Byazilya F. Vasilyeva, Alexander O. Chizhov, Darya A. Avdanina, Alexander A. Zhgun, Sergey N. Kochetkov, Liudmila A. Alexandrova
Summary: The emergence of drug-resistant strains of pathogenic microorganisms necessitates the creation of new drugs. In this study, a series of uridine derivatives with extended substituents at the C-5 position were obtained and their antimicrobial properties and solubility were explored. It was found that these new ribonucleoside derivatives have significantly higher solubility in water than their 2'-deoxy analogues and effectively inhibit the growth of several drug-resistant Gram-positive bacteria.
Article
Chemistry, Organic
Leila Emami, Soghra Khabnadideh, Zahra Faghih, Aida Solhjoo, Saba Malek, Amir Mohammadian, Masoumeh Divar, Zeinab Faghih
Summary: Thirteen novel Schiff base derivatives were synthesized and their cytotoxic activities against tumor cells and normal cells were evaluated. One of the compounds, M-12, showed high activity and was found to bind to VEGFR-2 and JNK3-MAP kinase. Based on the in vitro experiments and in silico predictions, M-12 could be a promising candidate for future anticancer studies.
JOURNAL OF HETEROCYCLIC CHEMISTRY
(2022)
Article
Microbiology
Ashley L. Cunningham, Orhi Esarte Palomero, Bradley J. Voss, M. Stephen Trent, Bryan W. Davies
Summary: Otilonium bromide, a poorly absorbed oral medication used for irritable bowel syndrome, has been found to have broad-spectrum antibacterial and antifungal activity, including against multidrug-resistant strains. This suggests that otilonium bromide could be a new option for intestinal antimicrobial therapy targeting enteric pathogens.
ANTIMICROBIAL AGENTS AND CHEMOTHERAPY
(2021)
Review
Biochemistry & Molecular Biology
Tianxi Li, Lulu Li, Fangyuan Du, Lei Sun, Jichao Shi, Miao Long, Zeliang Chen
Summary: This review focuses on antifungal peptides isolated from various microorganisms, outlining their antifungal activity, toxic effects, and mechanisms of action, as well as common solutions to mitigate their toxicity. This work serves as a useful reference for further clinical research and the development of safe antifungal drugs with high efficiencies and broad application spectra.
Article
Agriculture, Multidisciplinary
Adriana C. de Faria, Joyce K. Dare, Elaine F. F. da Cunha, Matheus P. Freitas
Summary: This study investigates the molecular level of modified sulfonylureas to determine their antifungal and herbicidal activities, and provides guidance for the design of new agrochemical candidates using molecular modeling and computational methods.
JOURNAL OF AGRICULTURAL AND FOOD CHEMISTRY
(2022)
Article
Chemistry, Physical
Sana Saffour, Amal A. AL-Sharabi, Asaf Evrim Evren, Meral Yilmaz Cankilic, Leyla Yurttas
Summary: In this study, thirteen new compounds were synthesized and evaluated for their antifungal and antimicrobial activities. One compound exhibited the best activity and selectivity against Yersinia enterocolitica. Additionally, all compounds showed good activity against filamentous fungi.
JOURNAL OF MOLECULAR STRUCTURE
(2024)
Article
Microbiology
Xinying Duan, Li Zhang, Hongyan Si, Jie Song, Peng Wang, Shangxing Chen, Hai Luo, Xiaoping Rao, Zongde Wang, Shengliang Liao
Summary: This study synthesized 37 camphor derivatives and evaluated their antifungal effects. Some compounds showed strong antifungal activity, with broad-spectrum activity against multiple fungi. The study also discovered molecular structure features associated with antifungal activity. These findings provide a theoretical basis for the high-value use of camphor and the development of novel antifungal drugs.
Article
Biochemistry & Molecular Biology
Hasan Aydin, Suleyman Akocak, Nebih Lolak, Ugur Uslu, Ahmet Sait, Serol Korkmaz, Ayse Parmaksiz, Onur Ceylan, Abdulbaki Aksakal
Summary: Multidrug resistance (MDR) poses challenges in the treatment of infections and cancer. Research and development studies are crucial in preventing MDR. This study focused on investigating the effects of multi-target triazene compounds on various activities related to bacteria, fungi, viruses, cytotoxicity, and larvicidal efficacy. Novel derivatives of 1,3-diaryltriazene-substituted sulfadiazine (SDZ) were synthesized and characterized, showing potential as multitargeted agents. These compounds exhibited antibacterial, antifungal, antiviral, cytotoxic, and larvicidal activities.
JOURNAL OF BIOCHEMICAL AND MOLECULAR TOXICOLOGY
(2023)
Article
Pharmacology & Pharmacy
Shabnam Yavari, Kayode Olaifa, Darya Shafiee, Reza Rasuli, Mehdi Shafiee
Summary: Microorganisms are emerging contaminants in the environment and pose significant risks to public health. Conventional disinfection methods are often ineffective and have drawbacks. This study presents a method to synthesize nanomaterials with antimicrobial properties and demonstrates their effectiveness against Escherichia coli and Candida albicans. The synthesized nanomaterials show potential for biomedical applications.
INTERNATIONAL JOURNAL OF PHARMACEUTICS
(2023)
Article
Biochemistry & Molecular Biology
Mauricio Osorio, Marcela Carvajal, Alejandra Vergara, Estefania Butassi, Susana Zacchino, Carolina Mascayano, Margarita Montoya, Sophia Mejias, Marcelo Cortez-San Martin, Yesseny Vasquez-Martinez
Summary: Prenylated flavonoids are important natural compounds with significant biological activity, particularly in antimicrobial functions. Compounds 11, 12, and 13 showed strong inhibitory activity against human pathogenic fungi and clinical isolated Staphylococcus aureus MRSA, indicating the key structural requirements for antibacterial activity. Additionally, the combination of prenylated flavonoids with commercial antibiotics significantly enhanced the antibacterial activity against drug-resistant bacteria.
INTERNATIONAL JOURNAL OF MOLECULAR SCIENCES
(2021)
Review
Microbiology
Abdelmoneim K. Abdalla, Mutamed M. Ayyash, Amin N. Olaimat, Tareq M. Osaili, Anas A. Al-Nabulsi, Nagendra P. Shah, Richard Holley
Summary: Exopolysaccharides (EPSs) are metabolites synthesized and excreted by various microorganisms, playing important biological functions in interactions between bacteria and their environments, protection against hostile conditions, and evasion of immune responses. Numerous studies have shown the broad antimicrobial activities of EPS against pathogenic microbes. This review focuses on the in vitro and in vivo antimicrobial activities of different EPSs against foodborne bacterial, fungal, and viral pathogens, as well as the mechanisms of action and methods of measurement.
FRONTIERS IN MICROBIOLOGY
(2021)
Review
Chemistry, Medicinal
Yan-Yan Ding, Han Zhou, Bao-Qi Peng-Deng, Bao-Qi Zhang, Zhi-Jun Zhang, Guang-Han Wang, Shao-Yong Zhang, Zheng-Rong Wu, Yi-Rong Wang, Ying-Qian Liu
Summary: Since the isolation of the first natural carbazole alkaloid, murrayanine, from Mwraya Spreng, carbazole alkaloid derivatives have attracted wide attention for their anti-tumor, anti-viral, and anti-bacterial activities. Recent research has shown that carbazole alkaloids and their derivatives exhibit diverse biological activities. This study provides the first comprehensive description of the antifungal and antibacterial activities of carbazole alkaloids in the past decade (2012-2022), including both natural and partially synthesized compounds. The challenges and problems faced by this class of alkaloids are also summarized. This paper will facilitate further exploration of carbazole alkaloids.
EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
(2023)
Review
Chemistry, Multidisciplinary
Varish Ahmad, Mohammad Omaish Ansari
Summary: Graphene and its nanocomposites have attracted significant interest due to their efficient antimicrobial properties. Graphene has found applications in tissue engineering and has been successfully conjugated with existing drugs to improve therapeutic efficacy. This review discusses the antimicrobial potential, synthesis, and toxicity of graphene-based nanomaterials in biological systems.
Article
Biochemistry & Molecular Biology
Philipe de Oliveira Fernandes, Joao Paulo A. Martins, Eduardo B. de Melo, Renata Barbosa de Oliveira, Thales Kronenberger, Vinicius Goncalves Maltarollo
Summary: The study suggests that aliphatic substituents at the hydrazone moiety are crucial for the antifungal activity of thiazolylhydrazones. Modern techniques were used to create QSAR models with high predictive power, supporting the design of new antifungal compounds.
JOURNAL OF BIOMOLECULAR STRUCTURE & DYNAMICS
(2022)
Article
Biochemistry & Molecular Biology
Laxmi Banjare, Yogesh Singh, Sant Kumar Verma, Atul Kumar Singh, Pradeep Kumar, Shashank Kumar, Akhlesh Kumar Jain, Suresh Thareja
Summary: This study investigated a series of biphenyl bearing molecules with a wide range of aromatase inhibitory activity using a multifaceted approach including 3D-QSAR analysis, molecular docking, molecular dynamic simulations, and pharmacophore mapping. The results showed that the force field-based 3D-QSAR model was the best in terms of fitness, and the generated pharmacophoric features were able to explain the variation in biological activity. The findings offer guidance for designing potent biphenyl derivatives as aromatase inhibitors.
JOURNAL OF BIOMOLECULAR STRUCTURE & DYNAMICS
(2023)
Article
Biochemistry & Molecular Biology
Yogesh Singh, Kulkarni Swanand Sanjay, Pradeep Kumar, Satwinder Singh, Suresh Thareja
Summary: This study investigated the pharmacophoric features and inhibitory potency of HIF-1 alpha inhibitors through three-dimensional quantitative structural activity relationship and pharmacophore mapping. It was found that indazole derivatives have the potential to be effective inhibitors of HIF-1 alpha, and molecular docking and molecular dynamics simulations confirmed the binding efficiency and stability of the most potent compound. The developed models and analysis techniques can be used to design selective lead molecules for the treatment of cancer.
JOURNAL OF BIOMOLECULAR STRUCTURE & DYNAMICS
(2023)
Review
Chemistry, Medicinal
Maneesh Guleria, Pradeep Kumar, Suresh Thareja
Summary: Background: Cancer is the second-leading cause of death worldwide, with an estimated 9.6 million deaths in 2018. PARP-1 is an enzyme and protein family involved in various cellular processes, including DNA repair and gene regulation. This article summarizes synthetic PARP-1 inhibitors reported in the past decade and highlights the need for further research on effective and safe PARP-1 inhibitors for cancer treatment.
LETTERS IN DRUG DESIGN & DISCOVERY
(2023)
Review
Chemistry, Medicinal
Gunjan Bisht, Ankit Kumar Singh, Adarsh Kumar, Pradeep Kumar
Summary: Background bacteria lead to various infectious diseases and millions of deaths each year. Plant-derived secondary metabolites possess antibacterial activity and can decrease resistance through inhibition of biofilm formation, efflux pump inhibition, attenuation of bacterial virulence, and immunomodulation activity.
NATURAL PRODUCTS JOURNAL
(2023)
Article
Biochemistry & Molecular Biology
Avadh Biharee, Arpita Yadav, Kailash Jangid, Yogesh Singh, Swanand Kulkarni, Devesh M. Sawant, Pradeep Kumar, Suresh Thareja, Akhlesh Kumar Jain
Summary: Flavonoids have shown potential as excellent anti-tubulin agents for cancer treatment, and this study provides strong evidence for their effectiveness through in silico ADMET analysis, molecular docking, and molecular dynamics simulation.
JOURNAL OF BIOMOLECULAR STRUCTURE & DYNAMICS
(2023)
Review
Oncology
Aditya Raj, Adarsh Kumar, Ankit Kumar Singh, Harshwardhan Singh, Suresh Thareja, Pradeep Kumar
Summary: PI3K controls cellular functions and is an important target for anticancer treatment. Quinazoline derivatives have shown promise as PI3K inhibitors and several compounds are currently in clinical trials. This study provides information on synthetic approaches, mechanisms of action, and structure-activity relationship analysis of quinazoline derivatives to aid in the design of better and isoform-selective PI3K inhibitors for researchers in the field.
ANTI-CANCER AGENTS IN MEDICINAL CHEMISTRY
(2023)
Review
Biochemistry & Molecular Biology
Neha Bhatia, Rakesh Khator, Swanand Kulkarni, Yogesh Singh, Pradeep Kumar, Suresh Thareja
Summary: The discovery of MDM2 and MDM2-p53 interaction inhibitors has revolutionized anticancer research due to their involvement in about 50% of cancer cases globally. In addition to inhibiting MDM2, targeting the interaction between MDM2 and p53 has proven to be an effective strategy for anticancer drug development. Both natural and synthetic molecules have shown promising MDM2 inhibitory potential. This review focuses on the pathophysiology of the MDM2-p53 interaction loop, characteristics of the active site, and the efficacy of various inhibitors from recent patents.
CURRENT MEDICINAL CHEMISTRY
(2023)
Review
Biochemistry & Molecular Biology
Rasti Sahu, Ankit Kumar Singh, Adarsh Kumar, Kuldeep Singh, Pradeep Kumar
Summary: The nature of phages was controversial, but in 1940 the dispute was resolved and their activity and application continued to develop in the Soviet Union and Eastern Europe. Bacteriophages were first used in 1919 to treat bacterial illnesses. Bacteriophages have different levels of complexity, ranging from simple spherical viruses to more complicated ones with larger genome sizes.
CURRENT PHARMACEUTICAL BIOTECHNOLOGY
(2023)
Review
Biochemistry & Molecular Biology
Ankit Kumar Singh, Adarsh Kumar, Harshwardhan Singh, Pankaj Sonawane, Prateek Pathak, Maria Grishina, Jagat Pal Yadav, Amita Verma, Pradeep Kumar
Summary: Metal complexes have attracted attention in cancer therapy due to their unique characteristics. The discovery of cisplatin in 1965 was a significant breakthrough and led to the development of metal-based anticancer drugs. Many metal-based compounds are being studied for their potential anticancer properties, with some already approved by the FDA or undergoing clinical trials. This study highlights the mode of action of metallic complexes and reviews the progress of metal-based complexes with potential anticancer activities, such as platinum, ruthenium, and iron.
CHEMISTRY & BIODIVERSITY
(2023)
Review
Chemistry, Medicinal
Adarsh Kumar, Ankit Kumar Singh, Harshwardhan Singh, Veena Vijayan, Deepak Kumar, Jashwanth Naik, Suresh Thareja, Jagat Pal Yadav, Prateek Pathak, Maria Grishina, Amita Verma, Habibullah Khalilullah, Mariusz Jaremko, Abdul-Hamid Emwas, Pradeep Kumar
Summary: Cancer is a major healthcare challenge worldwide, calling for the development of safer and target-specific anticancer drugs. This study summarizes the use of nitrogen-containing heterocycles in cancer treatment, providing insights into their pharmacological properties and mechanisms of action.
Review
Biochemistry & Molecular Biology
Ankit Kumar Singh, Adarsh Kumar, Sahil Arora, Raj Kumar, Amita Verma, Habibullah Khalilullah, Mariusz Jaremko, Abdul-Hamid Emwas, Pradeep Kumar
Summary: This review examines the structure, replication cycle, reverse transcription, and drug targets of HIV-1. It focuses on nucleoside reverse transcriptase inhibitors (NRTIs) and non-nucleoside reverse transcriptase inhibitors (NNRTIs), including their mechanisms of action, FDA-approved drugs, drugs in clinical trials, resistance and adverse effects, molecular docking studies, and highly active antiretroviral therapy (HAART).
CHEMICAL BIOLOGY & DRUG DESIGN
(2023)
Article
Biochemistry & Molecular Biology
Akanksha Sharma, Adarsh Kumar, Ankit Kumar Singh, Harshwardhan Singh, K. Jayaram Kumar, Pradeep Kumar
Summary: This study evaluated the photoprotective, antioxidant, and antibacterial properties of Ruellia tuberosa leaf extracts. The results showed that the methanol extract of R. tuberosa had high total phenolic content, while the acetic acid extract had the highest total flavonoid content. The methanol extract exhibited effective antioxidant activity and the methanol, ethyl acetate, and methanol-chloroform extracts showed effective antibacterial activity against E. coli. In silico docking studies identified phytochemicals that showed good docking scores and drug likeness properties against various proteins.
CHEMISTRY & BIODIVERSITY
(2023)
Article
Biochemistry & Molecular Biology
Teja Ram, Ankit Kumar Singh, Prateek Pathak, Adarsh Kumar, Harshwardhan Singh, Maria Grishina, Jurica Novak, Pradeep Kumar
Summary: MEK mutations are common in various types of cancer, and the design of compounds with structural resemblance to FDA-approved MEK inhibitors has shown promise. Through chemical synthesis and computational studies, compound S15 was found to be the most potent against cancer cells, while compounds S1 and S5 were comparable to the standard drug trametinib.
JOURNAL OF BIOMOLECULAR STRUCTURE & DYNAMICS
(2023)
Review
Chemistry, Multidisciplinary
Adarsh Kumar, Kuber Kumar Bhagat, Ankit Kumar Singh, Harshwardhan Singh, Tanuja Angre, Amita Verma, Habibullah Khalilullah, Mariusz Jaremko, Abdul-Hamid Emwas, Pradeep Kumar
Summary: This study focuses on pyrido[2,3-d]pyrimidine derivatives as anticancer agents, which have emerged as a promising scaffold in medicinal chemistry with a broad spectrum of activities. The study covers the inhibition mechanisms, structure-activity relationship, and signaling pathways of these derivatives against various cancer targets. The review provides a comprehensive medicinal and pharmacological profile of pyrido[2,3-d]pyrimidines and offers insights for designing new selective, effective, and safe anticancer agents.
Article
Biochemistry & Molecular Biology
Priyanka Bajpai, Ankit Kumar Singh, Shivanada Kandagalla, Phool Chandra, Vimlendu Kumar Sah, Pradeep Kumar, Maria Grishina, Om Prakash Verma, Prateek Pathak
Summary: Tuberculosis is a deadly disease that claims the lives of approximately 2 million people annually. This study synthesized and tested the anti-tuberculosis activity of different oxazoline/amide derivatives. Based on their computational and biological study, two compounds (2d and 3e) showed comparable antitubercular activity to the standard drug.
JOURNAL OF BIOMOLECULAR STRUCTURE & DYNAMICS
(2023)
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)