Article
Plant Sciences
Atanu Chatterjee, Ritu Khanra, Moitreyee Chattopadhyay, Santanu Ghosh, Ranabir Sahu, Gouranga Nandi, Himangshu Sekhar Maji, Pranabesh Chakraborty
Summary: Cyperus tegetum extract, traditionally used in treating skin cancers, was studied for its anti-inflammatory, analgesic, and anticancer properties in mice. The extract showed significant effects on tumor growth, area, and weight in tumorigenesis study, indicating its potential as a promising compound to reduce skin cancer risk.
JOURNAL OF ETHNOPHARMACOLOGY
(2022)
Article
Pharmacology & Pharmacy
Adnan A. Bekhit, Sherry N. Nasralla, Eman J. El-Agroudy, Nahla Hamouda, Ahmed Abd El-Fattah, Salma A. Bekhit, Kikuko Amagase, Tamer M. Ibrahim
Summary: This study evaluates the therapeutic activity and adverse drug reactions of a newly synthesized pyrazole derivative, compound AD732, and compares it to standard agents. The results show that AD732 has higher anti-inflammatory and analgesic effects compared to standard agents, without ulcerogenic effects and minimal detrimental effects on renal function. AD732 may be a safer and more effective molecule with promising potential for pain and inflammation management.
EUROPEAN JOURNAL OF PHARMACEUTICAL SCIENCES
(2022)
Article
Biochemistry & Molecular Biology
Somaia S. Abd El-Karim, Hanaa S. Mohamed, Mohamed F. Abdelhameed, Abd El-Galil E. Amr, Abdulrahman A. Almehizia, Eman S. Nossier
Summary: Compound 5, 10, 15, 17, 21, and 22 showed promising anti-inflammatory and analgesic activities with good gastrointestinal safety profiles, making them potential candidates for drug development. Molecular docking study helped rationalize their binding affinities and interactions with TNF-alpha.
BIOORGANIC CHEMISTRY
(2021)
Article
Biochemistry & Molecular Biology
Ruo-Mei Rui, Cheng-Run Tang, Chun-Tao Zhang, Wen-Kai Pan, Kai Gan, Rong-Hua Luo, Zi-Qian Wei, Fan-Shun Jing, Si-Ming Huang, Liu-Meng Yang, Yi-Ming Li, Yue-Ping Wang, Wei-Lie Xiao, Hong-Bing Zhang, Yong-Tang Zheng, Yan-Ping He
Summary: Both HIV and DENV pose serious threats to human life, health, and the social economy. However, no successful vaccines have been developed for either. This study developed novel compounds with potent anti-HIV and anti-DENV activity, and discussed the impact of C-6 substituents on their activity.
BIOORGANIC CHEMISTRY
(2022)
Article
Microbiology
Clemens Moeller, Lena Heinbockel, Patrick Garidel, Thomas Gutsmann, Karl Mauss, Gunther Weindl, Satoshi Fukuoka, Dominik Loser, Timm Danker, Klaus Brandenburg
Summary: This study analyzed the toxic behavior of Aspidasept and Aspidasept II and their part structures in various cellular models, as well as conducting electrophysiological experiments targeting the hERG channel and experiments on mouse neurobehavior and local lymph nodes. The data provided conclusive information about the potential toxic effects of these peptides, specifying a therapeutic window for their clinical application.
Article
Plant Sciences
Layza Fernanda Gomes Bezerra, Ana Paula Sant Anna da Silva, Rebeca Xavier da Cunha, Joao Ricardhis Saturnino de Oliveira, Mateus Domingues de Barros, Vycttor Mateus de Melo Alves da Silva, Vera Lucia de Menezes Lima
Summary: This study investigated the antioxidant, anti-inflammatory, analgesic, and antipyretic activity of Mimosa acutistipula leaves. The results showed that the leaves contain phenolic compounds and exhibit antioxidant and anti-inflammatory effects. It can be used for the treatment of alopecia and pharyngitis.
JOURNAL OF ETHNOPHARMACOLOGY
(2023)
Article
Biochemistry & Molecular Biology
Mohammad Ashiqur Rahman Bhuiyan Shovo, Marzia Rahman Tona, Jannatul Mouah, Fayza Islam, Md. Helal Uddin Chowdhury, Tuhin Das, Arkajyoti Paul, Duygu Agagunduz, Md. Masudur Rahman, Bin Emran, Raffaele Capasso, Jesus Simal-Gandara
Summary: Molineria capitulata is an ornamental plant traditionally used to treat chronic diseases; a study found that its leaf extract has antioxidant, anti-inflammatory, thrombolytic, and analgesic activities, with computational analysis showing strong binding affinity of its components to receptors.
CURRENT ISSUES IN MOLECULAR BIOLOGY
(2021)
Article
Chemistry, Multidisciplinary
Dodda Bhargavi, Srihari Konduri, Jyothi Prashanth, Malladi Sireesha, Koya Prabhakara Rao
Summary: A couple of series of heterocyclic-based urea and thiourea derivatives were synthesized and confirmed by various spectroscopy and analysis methods. The majority of these compounds displayed moderate-to-good anti-inflammatory activity, which was further analyzed through molecular docking studies using Cyclooxygenase-2 as the receptor.
Article
Pharmacology & Pharmacy
Saraswati Patel, Jyoti Shukla, Smita Jain, Vartika Paliwal, Neetika Tripathi, Sarvesh Paliwal, Swapnil Sharma
Summary: This study evaluates the analgesic and anti-inflammatory activity of Tubocurarine (d-TC) and suggests its repositioning in the treatment of pain and inflammation-related issues. The results showed significant inhibitory effects of d-TC on pain and inflammation in both in vitro and in vivo models, as well as good oral absorption capability.
BIOCHEMICAL PHARMACOLOGY
(2022)
Article
Plant Sciences
Mehmet Evren Okur, Ayse Esra Karadag, Yagmur Ozhan, Hande Sipahi, Sule Ayla, Benay Daylan, Suekran Kultur, Betuel Demirci, Fatih Demirci
Summary: The study demonstrates the antioxidant and anti-inflammatory properties of Phlomis rigida, as well as its positive effects on wound healing through both in vitro and in vivo experiments.
JOURNAL OF ETHNOPHARMACOLOGY
(2021)
Article
Chemistry, Physical
Refat El-Sayed, Ismail Althagafi, Moataz Morad, Salah M. El-Bahy, Nashwa El-Metwaly
Summary: The study synthesized substituted pyran, pyrimidine, and pyrazole derivatives as potential antimicrobial agents. Some of these compounds showed activities against bacteria, fungi, and cancer cells. Computational experiments supported the study and were in line with experimental aspects.
JOURNAL OF MOLECULAR STRUCTURE
(2021)
Article
Biochemistry & Molecular Biology
O. M. Hendawy, Hesham A. M. Gomaa, Sami Alzarea, Mutariah S. Alshammari, Fatma A. M. Mohamed, Yaser A. Mostafa, Ahmed H. Abdelazeem, Mostafa H. Abdelrahman, Laurent Trembleau, Bahaa G. M. Youssif
Summary: New series of COX-2/sEH inhibitors were synthesized to replace withdrawn COX-2 selective drugs, with promising analgesic, anti-inflammatory effects and lower cardiotoxicity. Compounds 20, 22, and 29 showed significant COX-2 inhibitory activity and were the most potent dual COX-2/sEH inhibitors, demonstrating good analgesic/anti-inflammatory effects and cardioprotective properties in vivo studies.
BIOORGANIC CHEMISTRY
(2021)
Review
Biochemistry & Molecular Biology
Maysa de Oliveira Barbosa, Polrat Wilairatana, Giovana Mendes de Lacerda Leite, Gyllyandeson de Araujo Delmondes, Lucas Yure Santos da Silva, Silvio Caetano Alves Jr, Lindaiane Bezerra Rodrigues Dantas, Daniel Souza Bezerra, Izabel Cristina Santiago Lemos de Beltrao, Diogenes de Queiroz Dias, Jaime Ribeiro-Filho, Cicero Francisco Bezerra Felipe, Henrique Douglas Melo Coutinho, Irwin Rose Alencar de Menezes, Marta Regina Kerntopf Mendonca
Summary: This study systematically reviewed the Plectranthus species with anti-inflammatory and analgesic potential. It identified 12 species indicated for the treatment of different inflammatory conditions and pain. However, further experiments and preclinical testing are needed to ensure their safe and effective use.
Article
Pharmacology & Pharmacy
Yan-Qing Xie, Jing-Yao Huang, Yun-Xiu Chen, Qian Zhou, Qi-Xiu Zhou, Zhu-Ya Yang, Shi-Kui Xu, Wen-Hong Tan, Lu Liu
Summary: This study investigates the metabolites in the bark and leaves of Streblus indicus for their anti-inflammatory and analgesic effects. The results provide scientific evidence for the traditional use of S. indicus and offer a theoretical foundation for the development of new anti-inflammatory and analgesic drugs.
FRONTIERS IN PHARMACOLOGY
(2023)
Review
Chemistry, Physical
Atamjit Singh, Danish Malhotra, Karanvir Singh, Renu Chadha, Preet Mohinder Singh Bedi
Summary: Thiazole derivatives are important heterocycles in medicinal chemistry, with widespread biological activities. This review summarizes recent advancements in the medicinal chemistry of thiazole derivatives, including marketed drugs, therapeutic candidates, synthesis methods, biological significances, and structure-activity relationships.
JOURNAL OF MOLECULAR STRUCTURE
(2022)
Article
Instruments & Instrumentation
Tinku, Mohd. Mujeeb, Abdul Ahad, Mohd. Aqil, Waseem Ahmad Siddiqui, Abul Kalam Najmi, Mymoona Akhtar, Apeksha Shrivastava, Abdul Qadir, Thasleem Moolakkadath
Summary: This study successfully optimized rubiadin-loaded niosomes using Box-Behnken design for the management of diabetic nephropathy in Wistar rats. The optimized formulation showed significant anti-diabetic activity and improvement in biochemical parameters in Wistar rats. The findings suggest that the prepared RLN formulation has potential for the management of STZ-NA-induced DN.
DRUG DELIVERY AND TRANSLATIONAL RESEARCH
(2022)
Review
Chemistry, Organic
Garvit Satija, Barkha Sharma, Anish Madan, Ashif Iqubal, Mohammad Shaquiquzzaman, Mymoona Akhter, Suhel Parvez, Mohammad Ahmed Khan, Mohammad Mumtaz Alam
Summary: Benzimidazole, a bicyclic aromatic compound, is an important pharmacophore for various bioactive heterocyclic compounds with numerous pharmacological activities. Recent research has focused on its potential as anticancer agents and the structure-activity relationships of compounds containing benzimidazole rings.
JOURNAL OF HETEROCYCLIC CHEMISTRY
(2022)
Article
Chemistry, Organic
Lalit Mohan Nainwal, Mohammad Shaququzzaman, Mymoona Akhter, Asif Husain, Suhel Parvez, Sharba Tasneem, Ashif Iqubal, Mohammad Mumtaz Alam
Summary: The sulfur-containing cyanopyrimidine derivative 4g showed promising broad-spectrum anticancer activity, with high growth inhibition against various cancer cell lines. These derivatives exhibited anticancer activity through different targets, indicating potential for further optimization to develop more effective multi-targeting anticancer agents.
JOURNAL OF HETEROCYCLIC CHEMISTRY
(2022)
Review
Chemistry, Medicinal
Sharba Tasneem, Mohammad Mumtaz Alam, Mohammad Amir, Mymoona Akhter, Suhel Parvez, Garima Verma, Lalit Mohan Nainwal, Ashif Equbal, Tarique Anwer, Mohammad Shaquiquzzaman
Summary: The regulation of genes through post-translational modification of proteins, known as "epigenetic" regulation, has been extensively studied for disease therapies, especially cancer chemotherapeutics. Histone deacetylases (HDACs) are important targets in epigenetic regulation and play a crucial role in balancing acetylation/deacetylation of lysine amino acids on histone/nonhistone proteins. HDAC inhibitors (HDACIs) are biologically active compounds that have become essential for cancer treatment due to their ability to induce cell cycle arrest, differentiation, and apoptosis in tumor cells.
MINI-REVIEWS IN MEDICINAL CHEMISTRY
(2022)
Review
Cell Biology
Barkha Sharma, Garvit Satija, Anish Madan, Mansi Garg, M. Mumtaz Alam, M. Shaquiquzzaman, Suruchi Khanna, Prachi Tiwari, Suhel Parvez, Ashif Iqubal, Syed Ehtaishamul Haque, Mohammad Ahmed Khan
Summary: Alzheimer's disease is a complex neurodegenerative disorder with unclear etiology and pathology. Recent research has highlighted the involvement of inflammasomes, particularly the NLRP3 inflammasome, in the disease. NLRP3 is a critical receptor involved in immune responses and has been found to play a significant role in various immunological and neurological disorders. Inhibiting the activity of the NLRP3 inflammasome has been suggested as a promising approach for preventing and treating Alzheimer's disease.
Article
Chemistry, Medicinal
Azizah M. Malebari, Gabriela Duffy Morales, Brendan Twamley, Darren Fayne, Mohemmed Faraz Khan, Eavan C. McLoughlin, Niamh M. O'Boyle, Daniela M. Zisterer, Mary J. Meegan
Summary: This study describes the synthesis, characterization, and mechanism of action of a series of 3-fluoro and 3,3-difluoro substituted beta-lactams as analogues of the tubulin-targeting agent CA-4. These compounds showed potent activity in breast cancer cells and low toxicity in non-cancerous cells. Mechanistic studies demonstrated that these compounds inhibit tubulin polymerization and induce apoptosis, making them potential candidates for the development of novel cancer therapeutics.
Article
Chemistry, Medicinal
Shweta Sharma, Mohd. Hafizur Rehman Ansari, Kalicharan Sharma, Rajesh K. Singh, Shakir Ali, Mohd. Mumtaz Alam, Mohd. Shaqiquzamman Zaman, Prawez Alam, Mymoona Akhter
Summary: In this study, a series of analogues were synthesized and evaluated, and KB-23, KB-22, and KB-06 showed promising antihyperglycemic potential in both in vitro and in vivo studies, making them potential starting points for the development of antidiabetic agents.
FUTURE MEDICINAL CHEMISTRY
(2023)
Article
Chemistry, Inorganic & Nuclear
Neelima Shrivastava, Shah Alam Khan, Mohammad Mumtaz Alam, Mymoona Akhtar, Apeksha Srivastava, Asif Husain
Summary: To discover potential anticancer agents, hybrid compounds were synthesized by combining thiazolidinone and pyrazole scaffolds. Among these compounds, 2-(1,3-diphenyl-1H-pyrazol-4-yl)-3-phenyl thiazolidin-4-one (4a) showed the most potency with a docking score of -9.307 and a binding score of -66.46, as well as good ADME parameters. In vitro studies indicated that compound 4a exhibited the highest inhibition against lung cancer (NCI-H23) cell lines with a moderate inhibition rate of 31.01%. Molecular docking analysis revealed that these hybrid compounds bind well to the active site of peroxisome proliferator-activated receptors-gamma (PPAR-gamma). Doxorubicin was used as a positive control. It can be concluded that compound 4a, with a pyrazole-thiazolidinone ring system, has the potential to be developed as an anticancer agent.
ZEITSCHRIFT FUR NATURFORSCHUNG SECTION B-A JOURNAL OF CHEMICAL SCIENCES
(2023)
Article
Biochemistry & Molecular Biology
Shaista Amin, Khursheed A. Sheikh, Ashif Iqubal, Mohammad Ahmed Khan, M. Shaquiquzzaman, Sharba Tasneem, Suruchi Khanna, A. K. Najmi, Mymoona Akhter, Anzarul Haque, Tarique Anwer, M. Mumtaz Alam
Summary: Despite advancements in Diabetes mellitus management, designing and synthesizing drug molecules that effectively improve hyperglycemia and associated complications in diabetic patients remains challenging. In this study, pyrimidine-thiazolidinedione derivatives were synthesized, characterized, and evaluated for their anti-diabetic properties. The synthesized compounds were analyzed using various techniques, including NMR, FTIR, and Mass Spectrometry. In-silico ADME studies confirmed the compounds met Lipinski's rule of five. In-vivo evaluation in diabetic rats showed that compounds 6e and 6m significantly reduced blood glucose levels without causing weight gain. Biochemical and histopathological analyses further supported the anti-diabetic effects of these compounds. Based on these findings, pyrimidine-based thiazolidinedione derivatives could be considered as novel anti-diabetic agents with minimal side effects.
BIOORGANIC CHEMISTRY
(2023)
Article
Biochemistry & Molecular Biology
Darakhshan Parveen, Anwesha Das, Shaista Amin, M. Mumtaz Alam, Mymoona Akhter, Mohammad Ahmed Khan, Ruhi Ali, Tarique Anwer, Khursheed A. Sheikh, Faizul Azam, M. Shaquiquzzaman
Summary: COVID-19 is caused by SARS-CoV-2 virus and dexamethasone is widely used for its treatment. Estrogen and Estetrol, which possess immunoenhancer properties, were tested as potential treatments for COVID-19. Molecular docking and simulations showed that these test ligands have drug-like properties and better binding potential than Dexamethasone. MD Simulation revealed that the interactions of these ligands are similar to drugs with in vitro anticovid activity. Further in vitro and in vivo studies are needed to confirm their potential against COVID-19.
JOURNAL OF BIOMOLECULAR STRUCTURE & DYNAMICS
(2023)
Article
Chemistry, Multidisciplinary
Md. Zeeshan Rasheed, Rehana Khatoon, Faizia Talat, Mohammad Mumtaz Alam, Heena Tabassum, Suhel Parvez
Summary: This study investigated the therapeutic effect of melatonin against rotenone-induced toxicity in the Drosophila model of PD. It found that melatonin reduced mortality and climbing ability of Drosophila and alleviated oxidative stress and mitochondrial dysfunctions.
Article
Chemistry, Medicinal
Sharba Tasneem, M. Mumtaz Alam, Suhel Parvez, Farah Pinky, Farah Khan, Manika Garg, Mohd. Amir, Mymoona Akhter, Shaista Amin, Mohammad Ahmed Khan, Mohammad Shaquiquzzaman
Summary: In this study, the authors synthesized and evaluated 27 novel coumarin-based amide derivatives for their HDAC1 inhibitory activity. They found that two of the compounds showed better activity than existing drugs. These coumarin derivatives exhibited promising potential as anticancer agents and should be further developed.
FUTURE MEDICINAL CHEMISTRY
(2023)
Article
Chemistry, Multidisciplinary
Mohemmed Faraz Khan, Shubhangi Kandwal, Darren Fayne
Summary: Computer-aided drug design (CADD) has revolutionized the traditional physical testing methods in drug discovery. However, CADD still faces limitations and challenges. A software platform called DataPype has been developed to streamline data processing and integrate various CADD tools, enhancing the drug discovery process.
Article
Medicine, General & Internal
Mohd Ishaq, Mohemmed Faraz Khan, Garima Verma, Akshoo Rathi, Mohammad Adil, Mohammad Faizan, Abul Kalam Najmi, Mohd Akhtar, Omkulthom Al Kamaly, Samar Zuhair Alshawwa, Abdelaaty A. Shahat, Abdulsalam Alhalmi
Summary: This study demonstrates the significant cardio-protective effects of curcumin nanoemulsion through the inhibition of ACE activity and antioxidant properties.
MEDICINA-LITHUANIA
(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)
