Article
Chemistry, Medicinal
Andrea Angeli, Mariana Pinteala, Stelian S. Maier, Alessandra Toti, Lorenzo Di Cesare Mannelli, Carla Ghelardini, Silvia Selleri, Fabrizio Carta, Claudiu T. Supuran
Summary: This study evaluated the inhibitory effects of telluride-containing compounds on human carbonic anhydrase enzymes, with some compounds showing significant toxic effects against breast cancer cells. Under both normoxic and hypoxic conditions, these compounds demonstrated good efficacy in killing cancer cells.
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
(2021)
Article
Biochemistry & Molecular Biology
Andrea Angeli, Victor Kartsev, Anthi Petrou, Mariana Pinteala, Volodymyr Brovarets, Sergii Slyvchuk, Stepan Pilyo, Athina Geronikaki, Claudiu T. Supuran
Summary: Carbonic anhydrases play a crucial role in living organisms and a series of new compounds were synthesized and tested as potential inhibitors in this study. Some of the derivatives showed interesting inhibitory activity towards tumor-associated isoforms. Computational procedures were also used to investigate the binding mode of these compounds within the active site.
INTERNATIONAL JOURNAL OF MOLECULAR SCIENCES
(2021)
Article
Chemistry, Medicinal
Damiano Tanini, Simone Carradori, Antonella Capperucci, Lucrezia Lupori, Susi Zara, Marta Ferraroni, Carla Ghelardini, Lorenzo Di Cesare Mannelli, Laura Micheli, Elena Lucarini, Fabrizio Carta, Andrea Angeli, Claudiu T. Supuran
Summary: The new organochalcogenides with sulfonamide moiety act as potent inhibitors of CA isoforms, particularly hCA II and VII, showing potent neuropathic pain attenuating effects. They also enhance the anticancer drugs' capability in counteracting breast cancer MCF7 cell viability. The simultaneous anti-neuropathic pain and antiproliferative effects of the new chalcogenide-based CA inhibitors represent an innovative approach for managing side effects associated with clinically platinum drugs as antitumor agents.
EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
(2021)
Article
Chemistry, Medicinal
Andrea Petreni, Alexandra Iacobescu, Natalia Simionescu, Anca-Roxana Petrovici, Andrea Angeli, Adrian Fifere, Mariana Pinteala, Claudiu T. Supuran
Summary: Solid tumors are challenging to treat due to their specific hypoxic microenvironment. Carbonic Anhydrase IX (CA IX) is a key enzyme in regulating and maintaining this condition, making it a promising target for tumor therapy. Researchers have synthesized selective CA IX inhibitors for targeted delivery of cytotoxic organotellurium scaffolds and found that one of the inhibitors exhibited potent cytotoxic effects against malignant melanoma and hepatocellular carcinoma.
EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
(2022)
Article
Biochemistry & Molecular Biology
Andrea Angeli, Marta Ferraroni, Alessandro Bonardi, Claudiu T. Supuran, Alessio Nocentini
Summary: Carbonic anhydrases (CAs) are important zinc metalloenzymes that catalyze the hydration of carbon dioxide. They play crucial roles in various biological processes and can be targeted for the treatment of diseases like glaucoma, obesity, and cancer. In this study, we report the co-crystallization of a N-nitro sulphonamide derivative with human CA II, revealing the binding site and mode of inhibition. This knowledge could aid in the development of more potent and selective CA inhibitors.
JOURNAL OF ENZYME INHIBITION AND MEDICINAL CHEMISTRY
(2023)
Article
Biochemistry & Molecular Biology
Andrea Angeli, Victor Kartsev, Anthi Petrou, Mariana Pinteala, Volodymyr Brovarets, Roman Vydzhak, Svitlana Panchishin, Athina Geronikaki, Claudiu T. Supuran
Summary: A series of novel benzenesulfonamides incorporating pyrazole- and pyridazinecarboxamides decorated with bulky moieties were synthesized and investigated for their inhibitory effects on various human carbonic anhydrase isoforms. Isoform-selective inhibitors were obtained, with a computational approach employed to explain the observed selectivity, potentially useful in drug design for developing inhibitors with pharmacological applications such as antiglaucoma, diuretic, antitumor, or anti-cerebral ischemia drugs.
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
Biochemistry & Molecular Biology
Haytham O. Tawfik, Moataz A. Shaldam, Alessio Nocentini, Rofaida Salem, Hadia Almahli, Sara T. Al-Rashood, Claudiu T. Supuran, Wagdy M. Eldehna
Summary: Carbonic anhydrases (CAs) are potential targets for developing anticancer agents. This study focuses on designing selective inhibitors for cancer-related hCA IX/XII isoforms, and a new series of coumarin derivatives were synthesized for this purpose. The results show that the prepared coumarins displayed inhibition activity on hCA IX/XII isoforms and exhibited antitumor activity on NCI-59 human cancer types.
JOURNAL OF ENZYME INHIBITION AND MEDICINAL CHEMISTRY
(2022)
Article
Biochemistry & Molecular Biology
Toni C. Denner, Andrea Angeli, Marta Ferraroni, Claudiu T. Supuran, Rene Csuk
Summary: Sulfonamides have inhibitory effects on carbonic anhydrases, and sulfonamides with biphenyl- and benzylphenyl substitutions show high selectivity for the treatment of hypoxic cancers and potential applications in treating cerebral edema.
Article
Biochemistry & Molecular Biology
Andrea Angeli, Marta Ferraroni, Fabrizio Carta, Cecile Haeberli, Jennifer Keiser, Gabriele Costantino, Claudiu T. Supuran
Summary: The limited options for treating schistosomiasis necessitate the discovery of alternative drugs. This study successfully inhibited the growth of Schistosoma mansoni using new PZQ derivatives, but further optimization is still needed.
JOURNAL OF ENZYME INHIBITION AND MEDICINAL CHEMISTRY
(2022)
Article
Biochemistry & Molecular Biology
Nora Astrain-Redin, Niccolo Paoletti, Daniel Plano, Alessandro Bonardi, Paola Gratteri, Andrea Angeli, Carmen Sanmartin, Claudiu T. Supuran
Summary: In the search for new cancer treatments, organoselenium compounds and carbonic anhydrase inhibitors have shown promise. Selenium-containing compounds, especially selenols, have demonstrated potent inhibition of tumor-associated CA isoforms. In this study, selenoesters combining NSAIDs and natural product fragments were evaluated as nonclassical inhibitors of tumor-associated CA isoforms.
JOURNAL OF ENZYME INHIBITION AND MEDICINAL CHEMISTRY
(2023)
Article
Chemistry, Medicinal
Andrea Angeli, Laura Micheli, Rita Turnaturi, Lorella Pasquinucci, Carmela Parenti, Vincenzo Alterio, Anna Di Fiore, Giuseppina De Simone, Simona Maria Monti, Fabrizio Carta, Lorenzo Di Cesare Mannelli, Carla Ghelardini, Claudiu T. Supuran
Summary: Through synthesis and evaluation of multiple compounds, this study identified a candidate drug with selective affinity for MOR and potent analgesic effect, as well as strong inhibition of several cytosolic CA isoforms. Compared to fentanyl, this compound maintained stable analgesic effect at a higher dose, with fewer withdrawal symptoms and glial cell activation.
EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
(2023)
Article
Biochemistry & Molecular Biology
Doretta Cuffaro, Riccardo Di Leo, Lidia Ciccone, Alessio Nocentini, Claudiu T. Supuran, Elisa Nuti, Armando Rossello
Summary: Carbonic anhydrases (CAs) are enzymes that catalyze the hydration of carbon dioxide, playing important roles in physiological processes. This study investigated a new series of isoxazoline-based amino alcohols as CA activators and found that compounds 3 and 5 showed the best activation effects towards hCA VII, with submicromolar affinity and good selectivity over hCA I. These newly identified CA activators have potential therapeutic applications in aging, epilepsy, and neurodegeneration.
JOURNAL OF ENZYME INHIBITION AND MEDICINAL CHEMISTRY
(2023)
Review
Biochemistry & Molecular Biology
Mateusz Kciuk, Adrianna Gielecinska, Somdutt Mujwar, Mariusz Mojzych, Beata Marciniak, Rafal Drozda, Renata Kontek
Summary: Carbonic anhydrases IX and CAXII play crucial roles in cancer and have become a focus in anticancer drug design. This offers an opportunity to develop new targeted therapies with fewer side effects.
JOURNAL OF ENZYME INHIBITION AND MEDICINAL CHEMISTRY
(2022)
Article
Biochemistry & Molecular Biology
Hasan Yakan, Gurkan Bilir, Sukriye Cakmak, Omer Tas, Nalan Turkoz Karakullukcu, Ercan Soydan, Halil Kutuk, Coskun Guclu, Murat Senturk, Tayfun Arslan, Seyhan Ozturk, Ercument Aksakal, Deniz Ekinci
Summary: A series of sulfenimide derivatives were synthesized via an efficient, simple and eco-friendly method and were found to be effective inhibitors of human and bovine carbonic anhydrase enzymes. The structures of the derivatives were confirmed by various techniques. These compounds showed strong inhibitory activity at low micromolar concentrations on human isoforms, while only four derivatives inhibited the bovine enzyme. One of the derivatives, the bromo derivative, was found to be the strongest inhibitor for all three enzymes. This study provides valuable contributions to further investigations on carbonic anhydrase inhibition in medicinal chemistry.
JOURNAL OF ENZYME INHIBITION AND MEDICINAL CHEMISTRY
(2023)
Article
Chemistry, Medicinal
Laura De Luca, Andrea Angeli, Federico Ricci, Claudiu T. Supuran, Rosaria Gitto
Summary: In recent years, the use of multistep hybrid computational protocols in drug discovery of enzyme inhibitors has gained attention. This study successfully generated pharmacophore models for hCA VA inhibitors using a combination of ligand- and structure-based approaches. Virtual screening on a database of commercially available sulfonamides resulted in the identification of several potential inhibitors.
ARCHIV DER PHARMAZIE
(2023)
Article
Chemistry, Medicinal
Vikas Sharma, Rajiv Kumar, Andrea Angeli, Claudiu T. Supuran, Pawan K. Sharma
Summary: In this study, a series of novel 1,2,3-triazole benzenesulfonamide compounds were designed and synthesized, and their inhibitory effects on human carbonic anhydrase were tested. The results showed that these compounds displayed variable inhibition constants against different isoforms of carbonic anhydrase, with some compounds exhibiting strong inhibitory potency. Computational simulations revealed the interactions between these compounds and the binding sites of carbonic anhydrase. The study emphasizes the importance of the synthesized 1,2,3-triazole compounds as building blocks for developing carbonic anhydrase inhibitor drugs.
ARCHIV DER PHARMAZIE
(2023)
Editorial Material
Chemistry, Medicinal
Claudiu T. Supuran
FUTURE MEDICINAL CHEMISTRY
(2023)
Article
Biochemistry & Molecular Biology
Andrea Angeli, Anthi Petrou, Victor Kartsev, Boris Lichitsky, Andrey Komogortsev, Clemente Capasso, Athina Geronikaki, Claudiu T. Supuran
Summary: Carbonic anhydrases play a crucial role in the CO2 hydration reaction in all living organisms and have potential as antiinfective targets. Griseofulvin and usnic acid sulfonamides were synthesized and evaluated as potential CA inhibitors. These compounds showed interesting inhibitory activity against various isoforms of CA, as well as a fungal enzyme. Computational studies were performed to understand the binding mode of these compounds in the active site of human CAs.
INTERNATIONAL JOURNAL OF MOLECULAR SCIENCES
(2023)
Article
Chemistry, Medicinal
Andrea Angeli, Laura Micheli, Fabrizio Carta, Marta Ferraroni, Tracey Pirali, Asia Fernandez Carvajal, Antonio Ferrer Montiel, Lorenzo Di Cesare Mannelli, Carla Ghelardini, Claudiu T. Supuran
Summary: We have reported a series of compounds that have the potential to manage oxaliplatin-induced neuropathy (OINP) by modulating human Carbonic Anhydrases (hCAs) and Transient Receptor Potential Vanilloid 1 (TRPV1). These compounds showed effective inhibition activity against the main hCAs involved in OINP in vitro, and some of them exhibited moderate agonism of TRPV1. In vivo evaluation of promising derivatives demonstrated potent and persistent antihypersensitivity effects in a mouse model of OINP.
JOURNAL OF MEDICINAL CHEMISTRY
(2023)
Article
Biochemistry & Molecular Biology
Andrea Angeli, Marta Ferraroni, Alessandro Bonardi, Claudiu T. Supuran, Alessio Nocentini
Summary: Carbonic anhydrases (CAs) are important zinc metalloenzymes that catalyze the hydration of carbon dioxide. They play crucial roles in various biological processes and can be targeted for the treatment of diseases like glaucoma, obesity, and cancer. In this study, we report the co-crystallization of a N-nitro sulphonamide derivative with human CA II, revealing the binding site and mode of inhibition. This knowledge could aid in the development of more potent and selective CA inhibitors.
JOURNAL OF ENZYME INHIBITION AND MEDICINAL CHEMISTRY
(2023)
Article
Biochemistry & Molecular Biology
Nora Astrain-Redin, Niccolo Paoletti, Daniel Plano, Alessandro Bonardi, Paola Gratteri, Andrea Angeli, Carmen Sanmartin, Claudiu T. Supuran
Summary: In the search for new cancer treatments, organoselenium compounds and carbonic anhydrase inhibitors have shown promise. Selenium-containing compounds, especially selenols, have demonstrated potent inhibition of tumor-associated CA isoforms. In this study, selenoesters combining NSAIDs and natural product fragments were evaluated as nonclassical inhibitors of tumor-associated CA isoforms.
JOURNAL OF ENZYME INHIBITION AND MEDICINAL CHEMISTRY
(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
Chemistry, Medicinal
Lalit Vats, Priyanka Arya, Rajiv Kumar, Simone Giovannuzzi, Neera Raghav, Claudiu T. Supuran, Pawan K. Sharma
Summary: This study synthesized and tested 28 novel compounds for their inhibition potential against cathepsin B and hCA isoforms, and found that one compound exhibited better and more selective inhibition against the cancer-associated hCA IX.
FUTURE MEDICINAL CHEMISTRY
(2023)
Editorial Material
Chemistry, Medicinal
Francesco Fiorentino, Fabrizio Carta, Dante Rotili, Antonello Mai, Claudiu T. Supuran
FUTURE MEDICINAL CHEMISTRY
(2023)
Article
Biochemistry & Molecular Biology
Anastasija Balasova, Aleksandrs Pustenko, Alessio Nocentini, Daniela Vullo, Claudiu T. Supuran, Raivis Zalubovskis
Summary: A range of 3H-1,2-benzoxaphosphepine 2-oxide aryl derivatives were synthesized in five steps from salicylaldehydes. These compounds showed selective inhibition against cancer-associated CA IX and XII, with the fluorine-containing analogues being the most potent inhibitors. SAR analysis indicated that 7- and 8-substituted aryl derivatives were more effective inhibitors of CA IX and XII than 9-substituted derivatives.
JOURNAL OF ENZYME INHIBITION AND MEDICINAL CHEMISTRY
(2023)
Article
Biochemistry & Molecular Biology
Deepak Shilkar, Mohd Usman Mohd Siddique, Silvia Bua, Sabina Yasmin, Mrunali Patil, Ajay Kumar Timiri, Claudiu T. Supuran, Venkatesan Jayaprakash
Summary: A series of phthalimide-capped benzene sulphonamides (1-22) were evaluated for their inhibitory activity against carbonic anhydrase I (hCA I) and carbonic anhydrase II (hCA II). Compound 1 showed potent inhibitory activity against both hCA I (Ki = 28.5 nM) and hCA II (Ki = 2.2 nM), with 10 and 6 times higher potency than the standard inhibitor, acetazolamide. Molecular docking and MD simulations were performed to understand the atomic level interactions responsible for the selectivity of compound 1 towards hCA II.
JOURNAL OF ENZYME INHIBITION AND MEDICINAL CHEMISTRY
(2023)
Article
Chemistry, Medicinal
Andrea Angeli, Marta Ferraroni, Carlotta Granchi, Filippo Minutolo, Xiaozhuo Chen, Pratik Shriwas, Emilio Russo, Antonio Leo, Silvia Selleri, Fabrizio Carta, Claudiu T. Supuran
Summary: In this study, a set of compounds with glucosyl and galactosyl moieties were designed and developed. Their ability to enhance GLUT1 mediated glucose intake in non-small-cell lung cancer cells and inhibit carbonic anhydrase isoforms associated with uncontrolled seizures in epilepsy was evaluated. The binding mode of compound 8 with hCA II was determined by X-ray crystallography. Among the selected derivatives, compound 4b effectively suppressed the occurrence of uncontrolled seizures in an in vivo induced maximal electroshock model, providing a novel pharmacological approach for managing GLUT1-DS associated diseases.
JOURNAL OF MEDICINAL CHEMISTRY
(2023)
Article
Chemistry, Medicinal
Marjan Sobati, Morteza Abdoli, Alessandro Bonardi, Paola Gratteri, Claudiu T. Supuran, Raivis Zalubovskis
Summary: A series of novel sulfonamide-incorporated α-aminophosphonate derivatives were synthesized, utilizing a one-pot, two-step FeCl3-catalyzed coupling reaction. These compounds were tested for inhibition against four different isoforms of carbonic anhydrase, including human cytosolic (h) hCA I and II (off-targets), as well as transmembrane cancer-related hCA IX and XII (targets). Among the synthesized compounds, derivative 23 exhibited the highest selectivity towards the cancer-associated isoforms over the off-target hCA I and hCA II, and the binding mode of both enantiomers R and S was investigated using in silico studies.
ACS MEDICINAL CHEMISTRY LETTERS
(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)
