Article
Chemistry, Medicinal
Rehab F. Ahmed, Walaa R. Mahmoud, Nagwa M. Abdelgawad, Marwa A. Fouad, Mona F. Said
Summary: This study designed a series of novel carbonic anhydrase inhibitors and evaluated their inhibitory activity and anticancer activity. Compounds 4b, 5b, 5d, 5e, 6b, 9b, 9e, and 11b showed significant inhibitory activity against both CA isoforms, while compound 6e exhibited significant cytostatic activity against multiple cancer cell lines, suggesting its potential as a promising anticancer drug.
EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
(2023)
Article
Biochemistry & Molecular Biology
Morteza Abdoli, Viviana De Luca, Clemente Capasso, Claudiu T. Supuran, Raivis Zalubovskis
Summary: A series of novel compounds were synthesized and evaluated for their inhibition of eukaryotic and human carbonic anhydrases. The results showed good inhibition against some target enzymes and weaker inhibition against others. These findings are important for the search for potential antifungal drugs.
INTERNATIONAL JOURNAL OF MOLECULAR SCIENCES
(2022)
Article
Biochemistry & Molecular Biology
Saeid Hadi Ali Janvand, Lucy Kate Ladefoged, Asta Zubriene, Andrius Sakalauskas, Gunna Christiansen, Virginija Dudutiene, Birgit Schiott, Daumantas Matulis, Vytautas Smirnovas, Daniel E. Otzen
Summary: Fluorinated sulfonamide compounds can inhibit the formation of amyloid fibrils, potentially providing therapeutic effects against amyloid-related disorders such as Parkinson's, Alzheimer's, and type 2 diabetes, possibly by maintaining insulin in its native monomeric state.
INTERNATIONAL JOURNAL OF BIOLOGICAL MACROMOLECULES
(2023)
Article
Chemistry, Physical
Rahman Abdizadeh, Keihan Ghatreh-Samani, Farzin Hadizadeh, Tooba Abdizadeh
Summary: In this study, various molecular modeling techniques were used to investigate isatin-based benzenesulfonamide derivatives as CA IX inhibitors. The models showed significant statistical findings for CA IX inhibition and provided valuable insights for improving the binding affinity and structure-activity relationship. Furthermore, the study identified important residues in the active site of CA IX and essential structural features for enhancing inhibitory activity, leading to the design of potential new inhibitors with improved activity for cancer treatment.
JOURNAL OF MOLECULAR STRUCTURE
(2021)
Article
Biochemistry & Molecular Biology
Haytham O. Tawfik, Amany Belal, Mohammed A. S. Abourehab, Andrea Angeli, Alessandro Bonardi, Claudiu T. Supuran, Mervat H. El-Hamamsy
Summary: This study reported the design and synthesis of two series of twenty-two benzenesulfonamides incorporating the s-triazine moiety, which successfully suppressed hCA IX and exhibited significant anticancer activity in various cancer cell lines.
JOURNAL OF ENZYME INHIBITION AND MEDICINAL CHEMISTRY
(2022)
Article
Chemistry, Medicinal
Mehtap Tugrak, Halise Inci Gul, Yeliz Demir, Ilhami Gulcin
Summary: A series of novel compounds with potential and selective inhibitory effects on human carbonic anhydrase I and II were synthesized, demonstrating promise as candidate drugs for treating glaucoma. Some compounds showed significant inhibitory effects against the target proteins, highlighting their potential for further investigation as lead compounds in alleviating glaucoma symptoms.
ARCHIV DER PHARMAZIE
(2021)
Article
Chemistry, Medicinal
Assem H. Eldeeb, Mahmoud F. Abo-Ashour, Andrea Angeli, Alessandro Bonardi, Deena S. Lasheen, Eman Z. Elrazaz, Alessio Nocentini, Paola Gratteri, Hatem A. Abdel-Aziz, Claudiu T. Supuran
Summary: New series of benzenesulfonamide and benzoic acid derivatives were designed and synthesized as carbonic anhydrase inhibitors using tail/dual tail approach. The benzenesulfonamide derivatives showed moderate to potent inhibitory activity with selectivity toward hCA II, while the benzoic acid analogues mostly exhibited no activity or weak activity. Fold-in-fold-out modifications were used to optimize the designed compounds.
EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
(2021)
Article
Biochemistry & Molecular Biology
Hossam Nada, Ahmed Elkamhawy, Magda H. Abdellattif, Andrea Angeli, Chang Hoon Lee, Claudiu T. Supuran, Kyeong Lee
Summary: In this study, a series of 4-anilinoquinazoline-based benzenesulfonamides were designed and synthesized as potential carbonic anhydrase inhibitors (hCAIs). These compounds showed high inhibitory activity and have potential applications in the treatment of epilepsy, glaucoma, and cancer.
JOURNAL OF ENZYME INHIBITION AND MEDICINAL CHEMISTRY
(2022)
Article
Chemistry, Medicinal
Mohamed A. Abdelrahman, Hany S. Ibrahim, Alessio Nocentini, Wagdy M. Eldehna, Alessandro Bonardi, Hatem A. Abdel-Aziz, Paola Gratteri, Sahar M. Abou-Seri, Claudiu T. Supuran
Summary: This study developed various coumarin derivatives as potential carbonic anhydrase inhibitors, with the dual-tail approach achieving good activity and selectivity towards CA IX/XII. Non-sulfonamide coumarin derivatives demonstrated excellent activity and selectivity against hCA IX/XII, while molecular modelling studies provided insights into their binding interactions with CA isoforms.
EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
(2021)
Article
Biochemistry & Molecular Biology
Ahmed Elkamhawy, Jiyu Woo, Hossam Nada, Andrea Angeli, Tarek M. Bedair, Claudiu T. Supuran, Kyeong Lee
Summary: In this study, a novel series of indole-based benzenesulfonamides were designed and synthesized as potential carbonic anhydrase inhibitors. The synthesized compounds were evaluated for their activity against different carbonic anhydrase isoforms, and compound 2a showed the most potent inhibition against the hCA II isoform with high selectivity.
INTERNATIONAL JOURNAL OF MOLECULAR SCIENCES
(2022)
Article
Biochemistry & Molecular Biology
Samet Poyraz, H. Ali Dondas, Cem Yamali, Samet Belveren, Yeliz Demir, Sabriye Aydinoglu, Naciye Yaktubay Dondas, Tugba Taskin-Tok, Senanur Tas, Mahmut Ulger, Jose M. Sansano
Summary: The synthesis and biological assessment of novel multi-functionalized pyrrolidine-containing benzenesulfonamides were reported. These compounds showed antimicrobial, antifungal, CAs inhibition, AChE inhibition, and DNA-binding effects. The most potent CAs inhibitor was compound 3b, while compounds 6a and 6b showed remarkable AChE inhibition effects. Additionally, compounds 6a-6c had moderate antituberculosis effects. The study also included molecular docking studies to evaluate the interaction of selected compounds against enzymes (CAs and AChE).
JOURNAL OF BIOMOLECULAR STRUCTURE & DYNAMICS
(2023)
Article
Chemistry, Medicinal
Andrea Angeli, Victor Kartsev, Anthi Petrou, Mariana Pinteala, Roman M. Vydzhak, Svitlana Y. Panchishin, Volodymyr Brovarets, Viviana De Luca, Clemente Capasso, Athina Geronikaki, Claudiu T. Supuran
Summary: A series of sulfanilamide derivatives containing heterocyclic carboxamide moieties were evaluated as CA inhibitors against several isoforms of human CA, with some showing selectivity towards hCA II and hCA XII. Molecular docking of some compounds on isoforms hCA II and XII was performed to understand their interaction with active site amino acid residues, rationalizing the reported inhibitory activity.
Article
Chemistry, Medicinal
Lalit Vats, Kiran Siwach, Andrea Angeli, Prerna Bikal, Jitender Kumar Bhardwaj, Claudiu T. Supuran, Pawan K. Sharma
Summary: In this study, novel benzenesulfonamide derivatives were synthesized and screened for their inhibitory effects on human carbonic anhydrase (hCA) isoforms. The compounds showed strong inhibition of the tumor-associated isoform hCA IX and moderate inhibition of the glaucoma-associated isoform hCA II. Compound 6Ac exhibited higher inhibitory activity than the standard drug acetazolamide. Selective hCA IX inhibitors also showed better apoptotic efficacy in goat ovarian cells.
ARCHIV DER PHARMAZIE
(2023)
Article
Chemistry, Medicinal
Ozlem Akgul, Srishti Singh, Jacob T. Andring, Robert McKenna, Silvia Selleri, Fabrizio Carta, Andrea Angeli, Claudiu T. Supuran
Summary: A series of taurine substituted sulfonamide derivatives with ureido moiety at the tail section were synthesized as selective inhibitors of tumor associated human Carbonic Anhydrase (CA) IX and XII. These derivatives showed a strong dependence on the presence of ureido moiety and demonstrated highly stabilized ligand-protein complex with specific amino acid residues in both hCA II and hCA IX-mimic.
EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
(2021)
Article
Chemistry, Multidisciplinary
Liucija Urbelyte, Martynas Bagdonas, Birute Grybaite, Rita Vaickelioniene, Aurelija Mickeviciute, Vilma Michailoviene, Daumantas Matulis, Vytautas Mickevicius, Asta Zubriene
Summary: A series of new benzenesulfonamide derivatives with alpha-amino acid moiety were synthesized and evaluated for their binding affinity to human carbonic anhydrase isozymes. The introduction of chloro substituents at 3,5-positions on the benzenesulfonamide ring increased the affinity for all carbonic anhydrases. Some derivatives showed low nanomolar affinity to CA VB, an isozyme implicated in diseases of the central nervous system and obesity.
Article
Biochemistry & Molecular Biology
Morteza Abdoli, Alessandro Bonardi, Claudiu T. Supuran, Raivis Zalubovskis
Summary: A one-pot two-step protocol was developed for the synthesis of novel 4-cyanamidobenzenesulfonamides, which showed effective inhibition towards both human and bacterial carbonic anhydrase enzymes.
JOURNAL OF ENZYME INHIBITION AND MEDICINAL CHEMISTRY
(2023)
Article
Chemistry, Medicinal
Mahmoud A. Ragab, Wagdy M. Eldehna, Alessio Nocentini, Alessandro Bonardi, Hazem E. Okda, Bahaa Elgendy, Tarek S. Ibrahim, Mohammad M. Abd-Alhaseeb, Paola Gratteri, Claudiu T. Supuran, Ahmed A. Al-Karmalawy, Mohamed Elagawany
Summary: In the current medical era, the traditional single target inhibition paradigm of drug discovery is being replaced by the multi-target design concept. A novel series of 4-(5-amino-pyrazol-1-yl)benzenesulfonamide derivatives was designed and synthesized as potential multi-target anti-inflammatory agents. The compounds showed inhibitory activities against COX-2, 5-LOX, and carbonic anhydrase (CA) isoforms, suggesting their potential application in treating inflammatory diseases with a multi-target approach.
EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
(2023)
Article
Biochemistry & Molecular Biology
Morteza Abdoli, Viviana De Luca, Clemente Capasso, Claudiu T. T. Supuran, Raivis Zalubovskis
Summary: A library of novel thiazolone-benzenesulphonamides was synthesized and evaluated for their inhibitory activity against human cytosolic carbonic anhydrases and bacterial carbonic anhydrases. The prepared compounds 4a-4j showed low nanomolar range inhibition against all investigated hCAs. Compound 4d exhibited strong inhibition against bacterial MscCA beta with a K-I of 73.6 nM, much better than AAZ. The tested compounds showed medium inhibitory potency against StCA1 compared to the standard drug, while poorly inhibited StCA2.
JOURNAL OF ENZYME INHIBITION AND MEDICINAL CHEMISTRY
(2023)
Review
Infectious Diseases
Alessio Nocentini, Clemente Capasso, Claudiu T. Supuran
Summary: Resistance to antibiotic treatment occurs when microorganisms resist clinically approved antibiotics. Medication repurposing/repositioning is a strategy that can help find new antibiotics. Among them, Zn2+ ion binders, such as sulfonamides and their bioisosteres, are considered promising compounds for obtaining novel antibacterials.
Article
Medicine, Research & Experimental
Marketa Kovalova, Libor Havlicek, Stefan Djukic, Jana Skerlova, Miroslav Perina, Tomas Pospisil, Eva Reznickova, Pavlina Rezacova, Radek Jorda, Vladimir Krystof
Summary: Targeting cyclin-dependent kinase 7 (CDK7) with a new trisubstituted pyrazolo[4,3-d]pyrimidine derivative, LGR6768, inhibits CDK7 in the nanomolar range and shows favorable selectivity across the CDK family. LGR6768 affects cell cycle regulation and transcription by inhibiting the phosphorylation of cell cycle CDKs and the carboxy-terminal domain of RNA polymerase II. It limits leukemia cell proliferation and induces apoptosis through changes in protein and mRNA levels related to CDK7 inhibition.
BIOMEDICINE & PHARMACOTHERAPY
(2023)
Review
Chemistry, Medicinal
Marketa Kovalova, Joseph Peter Baraka, Vaclav Mik, Radek Jorda, Lei Luo, Hao Shao, Vladimir Krystof
Summary: CDK7 is a protein kinase that regulates the cell cycle and mRNA transcription, and it has emerged as a potential drug target in oncology. Six promising drug candidates have been evaluated in early clinical trials. This review analyzes patents published from 2018 to 2022 and provides an overview of CDK7 inhibitors as anticancer drugs, including their chemical structures, biochemical profiles, and developmental stages.
EXPERT OPINION ON THERAPEUTIC PATENTS
(2023)
Article
Biochemistry & Molecular Biology
Valentina Puca, Gabriele Turacchio, Beatrice Marinacci, Claudiu T. Supuran, Clemente Capasso, Pamela Di Giovanni, Ilaria D'Agostino, Simone Carradori, Rossella Grande
Summary: The World Health Organization has identified Helicobacter pylori as a high-priority pathogen requiring updated antibacterial treatments. This study investigated the potential of combining a CA inhibitor, carvacrol (CAR), amoxicillin (AMX), and a urease inhibitor (SHA) to develop a multiple-targeted anti-H. pylori therapy. The combinations of these compounds showed strong inhibition of H. pylori growth and biofilm formation, with CAR-AMX and CAR-SHA combinations demonstrating additive effects and AMX-SHA combination showing indifferent effects.
INTERNATIONAL JOURNAL OF MOLECULAR SCIENCES
(2023)
Article
Biochemistry & Molecular Biology
Zainab M. M. Elsayed, Hadia Almahli, Alessio Nocentini, Andrea Ammara, Claudiu T. T. Supuran, Wagdy M. M. Eldehna, Sahar M. M. Abou-Seri
Summary: In this study, a new series of non-classical CA inhibitors, 2-aryl-quinazolin-4-yl aminobenzoic acid derivatives, were designed and synthesized as potential anticancer candidates. The inhibitory activities of these compounds against different CA isoforms were evaluated, and selected compounds were further tested for their anti-proliferative activity against human cancer cell lines.
JOURNAL OF ENZYME INHIBITION AND MEDICINAL CHEMISTRY
(2023)
Article
Biochemistry & Molecular Biology
Morteza Abdoli, Alessandro Bonardi, Niccolo Paoletti, Ashok Aspatwar, Seppo Parkkila, Paola Gratteri, Claudiu T. Supuran, Raivis Zalubovskis
Summary: A library of structurally diverse N-((4-sulfamoylphenyl)carbamothioyl) amides was synthesized by selectively acylating 4-thioureidobenzenesulfonamide with various acyl chlorides. The inhibitory effects of these sulfonamides on human carbonic anhydrase (hCA) and bacterial beta-carbonic anhydrase from Mycobacterium tuberculosis (MtCA) were investigated in vitro and in silico. The compounds showed better inhibition against hCA I, hCA II, hCA VII, as well as MtCA1 and MtCA2, but poor inhibition against MtCA3.
Article
Chemistry, Medicinal
Shaik Mahammad Ghouse, Kareena Sinha, Alessandro Bonardi, Gaurav Pawar, Satyaveni Malasala, Srikanth Danaboina, Arifuddin Mohammed, Venkata M. Yaddanapudi, Claudiu T. Supuran, Srinivas Nanduri
Summary: Carbonic anhydrase isoforms IX and XII are highly expressed in hypoxic tumor cells and play a role in cancer onset and spread. Coumarin derivatives were found to selectively inhibit these isoforms, offering a promising strategy for anticancer therapy. This study identified 6-aminocoumarin sulfonamide and oxime ether derivatives as potent inhibitors of human carbonic anhydrase IX and XII. The results demonstrate the potential of these derivatives as selective inhibitors and provide a foundation for further development as anticancer agents.
ARCHIV DER PHARMAZIE
(2023)
Article
Chemistry, Medicinal
Ilaria D'Agostino, Susi Zara, Simone Carradori, Viviana De Luca, Clemente Capasso, Clemens H. M. Kocken, Anne-Marie Zeeman, Andrea Angeli, Fabrizio Carta, Claudiu T. Supuran
Summary: The hybrid compounds synthesized in this study, which combine the Artesunate core with a sulfonamide moiety, showed high inhibition potency against the protozoan PfCA, while exhibiting low cytotoxic effects on human cells, indicating a wide therapeutic window.
Article
Biochemistry & Molecular Biology
Ahmed A. Al-Karmalawy, Radwan Alnajjar, Ayman Abo Elmaaty, Faizah A. Binjubair, Sara T. Al-Rashood, Basma S. Mansour, Ahmed Elkamhawy, Wagdy M. Eldehna, Khaled Ahmed Mansour
Summary: This study found that seven compounds isolated from Jasminum humile showed inhibitory activity against SARS-CoV-2 M-pro in vitro and in silico. The total extract (T1) exhibited the most significant activity, while the fractions (Fr1 and Fr3) also showed good activity. Molecular docking revealed that five of the compounds had high affinities towards the M-pro target.
JOURNAL OF BIOMOLECULAR STRUCTURE & DYNAMICS
(2023)
Letter
Oncology
Yanira Zeyn, Kristin Hausmann, Melisa Halilovic, Mandy Beyer, Hany S. Ibrahim, Walburgis Brenner, Siavosh Mahboobi, Matthias Bros, Wolfgang Sippl, Oliver H. Kraemer
Article
Chemistry, Multidisciplinary
Joseph S. Saleh, Soha R. Abd El Hadi, Hany S. Ibrahim, Eman Z. Elrazaz, Khaled A. M. Abouzid
Summary: New thienopyrimidine derivatives were designed and synthesized as GSK-3 beta inhibitors based on the structure of the active binding site of the enzyme. Compound 6b and 6a showed moderate inhibitory activity against GSK-3 beta. Molecular docking study and ADME prediction suggested that the synthesized compounds may have limited ability to penetrate the blood brain barrier, reducing the chances of CNS side effects, but may also lead to drug-drug interactions.
Article
Chemistry, Multidisciplinary
Abdullah A. Elgazar, Ramadan A. El-Domany, Wagdy M. Eldehna, Farid A. Badria
Summary: In this study, the conjugation of theophylline with different natural compounds was investigated to develop new hybrids with dual activity against cholinergic and inflammatory pathways for the treatment of Alzheimer's disease. Two hybrids, acefylline-eugenol 6d and acefylline-isatin 19, showed potent inhibition of acetylcholinesterase (AChE) and significant anti-inflammatory effects. Molecular docking studies revealed their ability to interact with key targets involved in Alzheimer's disease. The compounds also demonstrated stability in simulated gastric and intestinal environments, indicating their potential for absorption into the bloodstream. These findings highlight the therapeutic potential of these hybrids and provide promising avenues for further development as treatments for Alzheimer's disease.
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)