Article
Chemistry, Physical
Lukasz Popiolek, Sylwia Szeremeta, Anna Biernasiuk, Monika Wujec
Summary: This research describes the synthesis and in vitro antimicrobial activity study of a series of 2,4,6-trimethylbenzenesulfonyl hydrazones. The study confirmed the potential application of obtained derivatives as antimicrobial agents, with derivative 24 showing the highest activity among the tested compounds.
Article
Chemistry, Physical
Archna Yadav, C. P. Kaushik, Mukesh Kumar
Summary: A series of hydrazones tethered 1,4-disubstituted 1,2,3-triazoles were synthesized from novel N-substituted alkynes derived from benzohydrazides and benzyl bromides through Cu(I) catalyzed 1,3-dipolar cycloaddition reaction. The synthesized compounds were characterized by various spectroscopic techniques and the crystal structure of one compound was determined by X-ray crystallography. The compounds were evaluated for their antimicrobial and antitubercular activities, and two compounds showed promising results. Molecular docking studies and in-silico ADME studies were also conducted to understand the mode of action and the potential of the synthesized triazoles as drug agents.
JOURNAL OF MOLECULAR STRUCTURE
(2023)
Article
Chemistry, Multidisciplinary
Fernando Carrasco, Wilfredo Hernandez, Oscar Chupayo, Patricia Sheen, Mirko Zimic, Jorge Coronel, Celedonio M. Alvarez, Sergio Ferrero, Sandra Oramas-Royo, Evgenia Spodine, Jesus M. Rodilla, Juan Z. Davalos
Summary: Eight new phenylisoxazole isoniazid derivatives were synthesized and showed moderate antituberculous activity, especially exhibiting potential for use against resistant strains of Mycobacterium tuberculosis.
JOURNAL OF CHEMISTRY
(2021)
Article
Biochemistry & Molecular Biology
Trung-Anh Le, Yong Guo, Jun-Nian Zhou, Jiaqi Yan, Hongbo Zhang, Tan-Phat Huynh
Summary: A novel chemical functionalization of guar gum (GG) by benzoic acid (BA) has been reported, with the product characterized using various analysis techniques. The presence of conjugated BA on GG-BA with grafting density of 5.5% was confirmed, and showed good biocompatibility towards mouse embryonic fibroblasts (MEF) and human mammary epithelial cells (MCF-10A). GG-BA shows promising potential for the development of biomaterials like bioadhesives, hydrogels, and coacervates.
INTERNATIONAL JOURNAL OF BIOLOGICAL MACROMOLECULES
(2022)
Article
Chemistry, Organic
Siwei Wang, Chaochao Xie, Yu Zhu, Guofu Zi, Zhanbin Zhang, Guohua Hou
Summary: An efficient Ni-(S,S)-Ph-BPE complex has been developed for the asymmetric hydrogenation of cyclic N-acyl hydrazones, leading to the formation of various chiral cyclic hydrazines with high yields and enantioselectivities of over 99%. The hydrogenation reaction can proceed smoothly on a gram scale with low catalyst loading (S/C = 3000) without a decrease in enantioselectivity, and it can be applied to the asymmetric synthesis of a RIP-1 kinase inhibitor.
Article
Materials Science, Multidisciplinary
Shun-Ping Zhao, Xin-Yue Zuo, Yu Guo, Jie Wang, Rong-Yi Huang, Qiao Qiao
Summary: The synthesis and investigation of benzoic acid intercalated kaolinite compound were conducted to explore its preparation methods, intercalation mechanisms, and dielectric properties. The results revealed that high pressure, suitable precursor, and solvent were crucial for obtaining the desired compound. The benzoic acid molecules were arranged in an inclined monolayer between kaolinite layers, and the compound exhibited a low dielectric constant, making it suitable for semiconductor industry as a low-k material.
MATERIALS TODAY COMMUNICATIONS
(2022)
Article
Engineering, Environmental
Rickson Jun Jay Chia, Woei Jye Lau, Norhaniza Yusof, Ahmad Fauzi Ismail, Ana Loncaric Bozic
Summary: Researchers enhanced the performance of MIL-100(Fe) for As(V) adsorption by introducing benzoic acid as a modulator, creating vacancy defects in the structure. The modified adsorbent showed larger surface area and pore size, resulting in improved adsorption capacity for As(V). However, the presence of competing compounds such as carbonate and phosphate anions needs to be addressed for effective adsorption.
JOURNAL OF ENVIRONMENTAL CHEMICAL ENGINEERING
(2023)
Review
Multidisciplinary Sciences
Ibrahim Mhaidat, Fadel Alwedian, Taher Ababneh, Ayman Shdefat, Hasan Tashtoush
Summary: New photophysical and antioxidant materials of trimesic trihydrazide derivatives were synthesized by one-pot stage and characterized using spectroscopic techniques. The absorption and emission spectral characteristics, antioxidant activities, and antimicrobial activities of the derivatives were investigated. Molecular geometries of the derivatives were fully optimized using density functional theory calculations.
Article
Chemistry, Medicinal
Vaclav Pflegr, Lilla Horvath, Jirina Stolarikova, Adrian Pal, Jana Kordulakova, Szilvia Bosze, Jarmila Vinsova, Martin Kratky
Summary: Novel compounds based on isoniazid scaffold were designed and synthesized with increased lipophilicity for improved antitubercular activity. The compounds exhibited excellent activity against susceptible and resistant strains of Mycobacterium tuberculosis, potentially inhibiting enoyl-acyl carrier protein reductase and showing promising prospects for drug discovery in tuberculosis treatment.
EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
(2021)
Article
Chemistry, Multidisciplinary
Martin Linden, Silja Hofmann, Antonia Herman, Nicole Ehler, Robin M. M. Baer, Siegfried R. R. Waldvogel
Summary: This study presents the first electrochemical approach for the direct synthesis of pyrazolines and pyrazoles from easily accessible hydrazones and dipolarophiles. The method allows for large-scale production and even conversion of highly sensitive alkenes. The use of a biphasic system with sodium iodide as a supporting electrolyte and mediator is cost-effective. Mechanistic insight is provided by the isolation of key intermediates, and the synthesis of a commercial herbicide safener further highlights the significance of this reaction.
ANGEWANDTE CHEMIE-INTERNATIONAL EDITION
(2023)
Article
Chemistry, Medicinal
Muharrem Kalayci, Cuneyt Turkes, Mustafa Arslan, Yeliz Demir, Sukru Beydemir
Summary: This study designed novel multitarget drugs for Alzheimer's disease treatment and validated their effects through experiments and in silico monitoring. The results indicated that 6c, 6e, and 6f were the most promising derivatives in this series, showing potential for AD treatment with good multifunctional inhibition.
ARCHIV DER PHARMAZIE
(2021)
Article
Chemistry, Multidisciplinary
Asma Sardar, Obaid-ur-Rahman Abid, Saima Daud, Basit Ali Shah, Wardah Shahid, Muhammad Ashraf, Mahvish Fatima, Safa Ezzine, Abdul Wadood, Azam Shareef, Hanan A. Al-Ghulikah, Siham A. Alissa
Summary: Inflammation is the immune system's response to tissue dysfunction or homeostatic imbalance, involving the COX and LOX pathways. This study synthesized a series of diclofenac acid and naproxen-bearing hydrazones and evaluated their inhibitory potential against the 15-LOX enzyme. The compounds showed varying degrees of inhibitory potential, with compounds 7c and 7f being the most potent. Additionally, these compounds demonstrated low cytotoxicity in cells.
ARABIAN JOURNAL OF CHEMISTRY
(2022)
Article
Chemistry, Multidisciplinary
Ruediger W. Seidel, Adrian Richter, Richard Goddard, Peter Imming
Summary: This article provides a comprehensive account of a potential new class of drugs for tuberculosis treatment called 8-nitro-4H-benzo[e][1,3]thiazin-4-ones. These compounds are potent antitubercular agents with a novel mechanism of action. The review includes synthesis, structures and reactivity, mechanism of action, in vitro activity and structure-activity relationships, as well as physicochemical and pharmacokinetic properties. It also summarizes in vivo models and clinical studies, addressing bioavailability issues and the challenge of potentially toxic nitroaromatic moiety, and suggests possible directions for further research through chemical modification.
CHEMICAL COMMUNICATIONS
(2023)
Article
Chemistry, Multidisciplinary
Kevin de Aquino Dias, Marcus Vinicius Pinto Pereira Junior, Leandro Helgueira Andrade
Summary: A polymer-bound organocatalyst for Baeyer-Villiger reaction and phenol oxidation under continuous flow conditions has been described for the first time. This catalyst showed high catalytic activities, selectivities, recyclability, and productivity, enabling the generation of a novel approach for the synthesis of benzoquinones from beta-O-4 lignin models.
Article
Chemistry, Medicinal
Vaclav Pflegr, Jirina Stolarikova, Jarmila Vinsova, Martin Kratky
Summary: A total of 23 N-(cyclo)alkyl-2-(2-isonicotinoylhydrazineylidene)propanamides and their analogues were designed, synthesized, and evaluated as potential antimycobacterial compounds. These compounds showed low minimum inhibitory concentrations (MIC) against both Mycobacterium tuberculosis and nontuberculous mycobacteria, and exhibited even lower MIC values compared to parent isonicotinohydrazide.
CURRENT TOPICS IN MEDICINAL CHEMISTRY
(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
Oncology
Ankit Kumar Singh, Adarsh Kumar, Suresh Thareja, Pradeep Kumar
Summary: Melanomas, accounting for only 4% of skin cancers, have a mortality rate higher than 50% of other skin cancers. Genetic and environmental alterations are risk factors for melanoma development. The RAS/RAF/MEK/ERK or MAPK pathway is activated in melanoma, with BRAF mutations found in 80-90% of cases. Understanding melanoma pathogenesis, BRAF conformations, and the problems with current FDA-approved inhibitors is crucial for new drug discovery and improving treatment effectiveness.
ANTI-CANCER AGENTS IN MEDICINAL CHEMISTRY
(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)
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)
