Article
Biochemistry & Molecular Biology
Sergio M. Marques, Lucie Supolikova, Lenka Molcanova, Karel Smejkal, David Bednar, Iva Slaninova
Summary: In this study, a computational approach was used to construct the full-length three-dimensional structure of human P-gp and refine it with molecular dynamics. Through docking experiments, certain natural flavonoids were identified as effective P-gp inhibitors, increasing the accumulation of doxorubicin in cancer cells and enhancing its antiproliferative activity.
Article
Biochemistry & Molecular Biology
Mahmoud A. A. Ibrahim, Khlood A. A. Abdeljawaad, Laila A. Jaragh-Alhadad, Hesham Farouk Oraby, Mohamed A. M. Atia, Othman R. Alzahrani, Gamal A. H. Mekhemer, Mahmoud F. Moustafa, Ahmed M. Shawky, Peter A. Sidhom, Alaa H. M. Abdelrahman
Summary: The development of multidrug resistance (MDR) caused by overexpression of P-glycoprotein (P-gp/ABCB1/MDR1) is the main reason for the failure of chemotherapy in carcinoma treatment. An in silico study was conducted to discover potential P-gp inhibitors by assessing the binding energies of 512 drug candidates. Five promising drug candidates, valspodar, dactinomycin, elbasvir, temsirolimus, and sirolimus, showed strong binding energies against P-gp transporter and displayed good pharmacokinetic properties. These results indicate their potential as prospective P-gp inhibitors and require further in vitro/in vivo investigations.
JOURNAL OF BIOMOLECULAR STRUCTURE & DYNAMICS
(2023)
Article
Biochemistry & Molecular Biology
Liadys Mora Lagares, Yunierkis Perez-Castillo, Nikola Minovski, Marjana Novic
Summary: P-gp is an important protein involved in drug efflux and multidrug resistance. Molecular dynamics simulations can provide valuable insights into the binding behavior and conformational changes of P-gp in the presence of different compounds.
INTERNATIONAL JOURNAL OF MOLECULAR SCIENCES
(2022)
Article
Chemistry, Medicinal
Conghui Wang, Meng Gao, Shuqi Liu, Zongji Zou, Ruiyin Ren, Chen Zhang, Hao Xie, Jingxian Sun, Yupeng Qi, Qi Qu, Zhihua Song, Gangqiang Yang, Hongbo Wang
Summary: The study demonstrated that pyxinol derivatives can serve as modulators against Pgp-mediated cancer multidrug resistance. The synthesized pyxinol derivatives linked to amino acid residues effectively reversed MDR in KBV cells, with compound 3c showing the best activity.
EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
(2021)
Article
Pharmacology & Pharmacy
Sofija Jovanovic Stojanov, Epole N. Ntungwe, Jelena Dinic, Ana Podolski-Renic, Milica Pajovic, Patricia Rijo, Milica Pesic
Summary: Coleon U, a natural compound not recognized as a substrate of P-glycoprotein, has equal efficacy against sensitive and multidrug-resistant cancer cells. It delays the decrease in P-glycoprotein activity by decreasing mitochondrial membrane potential and inhibiting P-glycoprotein expression.
Article
Biochemistry & Molecular Biology
Ewa Zeslawska, Waldemar Tejchman, Annamaria Kincses, Gabriella Spengler, Wojciech Nitek, Grzegorz Zuchowski, Ewa Szymanska
Summary: Multidrug resistance (MDR) is a major reason for the failure of anticancer and antiviral chemotherapies. In this study, a series of newly synthesized 5-arylidenerhodanines were investigated for their ability to inhibit the ABCB1 efflux pump in mouse T-lymphoma cancer cells. Compounds with a triphenylamine moiety and the carboxyl group showed strong inhibitory effects, with over 17-fold higher potency than verapamil. The cytotoxic and antiproliferative effects of these compounds on T-lymphoma cells were also examined.
INTERNATIONAL JOURNAL OF MOLECULAR SCIENCES
(2022)
Article
Chemistry, Medicinal
David S. P. Cardoso, Nikoletta Szemeredi, Gabriella Spengler, Silva Mulhovo, Daniel J. V. A. dos Santos, Maria-Jose U. Ferreira
Summary: The study reported a monoterpene indole alkaloid Dregamine isolated from Tabernaemontana elegans, which underwent chemical transformations to produce azines and semicarbazones with various substituents. These derivatives exhibited potent multidrug resistance (MDR) reversal activity, especially those containing aromatic substituents in the azine moieties.
Article
Biochemistry & Molecular Biology
Shafi Mahmud, Md. Jahirul Islam, Md. Rimon Parves, Md. Arif Khan, Lamiya Tabussum, Sinthyia Ahmed, Md. Ackas Ali, Sayo O. Fakayode, Mohammad A. Halim
Summary: This study aimed to identify potent inhibitors of P-glycoprotein using computational approaches. Two compounds showed promising anti-tumor activity with acceptable pharmacokinetic properties, and molecular docking and dynamics simulations verified their stable binding with P-glycoprotein. Principal component analysis and QSAR modeling provided insights into the interactions and predictive capabilities of the drug candidates.
JOURNAL OF BIOMOLECULAR STRUCTURE & DYNAMICS
(2022)
Article
Biochemistry & Molecular Biology
Parisa Shahpouri, Havva Mehralitabar, Mitra Kheirabadi, Sakineh Kazemi Noureini
Summary: This study utilized pharmacoinformatic tools to investigate the potential of coumarin derivatives as MRP1 inhibitors. The results showed that Lig. No. 4 had the best binding score and may partially competitively inhibit MRP1 by interfering with ATP entrance to NBDs and altering the conformation of MRP1.
JOURNAL OF BIOMOLECULAR STRUCTURE & DYNAMICS
(2023)
Article
Chemistry, Physical
Linna Liang, Wendi Huo, Bei Wang, Lingzhi Cao, Haoran Huo, Yixin Liu, Yi Jin, Xinjian Yang
Summary: Tumor multidrug resistance is a major cause of chemotherapy failure, and reversing tumor multidrug resistance is crucial for increasing the sensitivity of tumor cells to chemodrugs. The self-assembled DNAzyme nanoflowers can efficiently reverse multidrug resistance, enhance drug loading capacity, and suppress P-glycoprotein expression.
JOURNAL OF COLLOID AND INTERFACE SCIENCE
(2022)
Article
Biochemistry & Molecular Biology
Catia A. Bonito, Ricardo J. Ferreira, Maria-Jose U. Ferreira, Jean-Pierre Gillet, M. Natalia D. S. Cordeiro, Daniel J. V. A. dos Santos
Summary: In this study, the impact of four P-gp mutations on drug-binding and efflux-related signal-transmission mechanism was evaluated. The repacking of the transmembrane helices induced by mutations and ligands indicates P-gp's sensitivity to perturbations in the transmembrane region. Changes in drug-binding were observed as a consequence of transmembrane helices repacking, but were not always correlated with alterations in ligand binding mode and affinity. The changes in drug efflux are mostly related to changes in drug specificity rather than effects on signal-transmission mechanism.
JOURNAL OF BIOMOLECULAR STRUCTURE & DYNAMICS
(2023)
Article
Biochemistry & Molecular Biology
Julia Schaefer, Vincent Julius Kloesgen, Ejlal A. Omer, Onat Kadioglu, Armelle T. Mbaveng, Victor Kuete, Andreas Hildebrandt, Thomas Efferth
Summary: Cancer therapy is often hindered by drug resistance and severe side effects. Phytochemicals are a valuable resource for developing less toxic drugs. Bioinformatics can simplify the drug development process. This study analyzed 375 phytochemicals and identified six compounds with potential anticancer activity and P-gp inhibition.
INTERNATIONAL JOURNAL OF MOLECULAR SCIENCES
(2023)
Retraction
Oncology
S. Mohana, M. Ganesan, N. Rajendra Prasad, D. Ananthakrishnan, D. Velmurugan
Summary: A correction to this paper has been published and is accessible through the original article.
Article
Food Science & Technology
Jeronimo Laiolo, Cecilia L. Barbieri, Mariana B. Joray, Priscila A. Lanza, Sara M. Palacios, D. Mariano A. Vera, Maria C. Carpinella
Summary: The study identified betulin as an effective agent to inhibit P-gp-mediated multidrug resistance, increasing intracellular accumulation of anticancer drugs and sensitizing MDR leukemia cells to Dox. Docking studies revealed betulin's tight binding to key regions of P-gp, mimicking tariquidar's contacts without toxicity. These findings suggest that betulin may be a promising candidate for developing more effective and less toxic chemotherapy agents.
FOOD AND CHEMICAL TOXICOLOGY
(2021)
Article
Agriculture, Multidisciplinary
Md Yousof Ali, Sumera Zaib, Susoma Jannat, Imtiaz Khan
Summary: Ginsenoside derivatives exhibit significant inhibitory effects on ACE, with protopanaxatriol, protopanaxadiol, and ginsenoside Rh2 showing the most potent inhibition. Molecular docking studies confirmed that ginsenosides inhibit ACE through hydrogen bonds and hydrophobic interactions. Additionally, ginsenosides also stimulate glucose uptake in insulin-resistant cells and have antioxidant properties.
JOURNAL OF AGRICULTURAL AND FOOD CHEMISTRY
(2021)
Article
Chemistry, Medicinal
Francesca S. Abatematteo, Philip D. Mosier, Mauro Niso, Leonardo Brunetti, Francesco Berardi, Fulvio Loiodice, Marialessandra Contino, Benjamin Delprat, Tangui Maurice, Antonio Laghezza, Carmen Abate
Summary: The sigma-1 receptor is important in physiological and pathological processes, and the phenoxyalkylpiperidine compounds show potential as high-affinity agonists. Compound 1a, in particular, exhibits strong activity and warrants further investigation.
EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
(2022)
Article
Chemistry, Medicinal
Mariagrazia Rullo, Marco Cipolloni, Marco Catto, Carolina Colliva, Daniela Valeria Miniero, Tiziana Latronico, Modesto de Candia, Tiziana Benicchi, Anna Linusson, Nicola Giacche, Cosimo Damiano Altomare, Leonardo Pisani
Summary: In this study, bioisosteric replacements of important functional groups (H/F and CH2OH/CF2H) in coumarin derivatives were investigated to explore their effects on inhibitory potency and drug-likeness. The results showed that compound 15 exhibited strong inhibitory activities against both AChE and MAO B, along with good water solubility and oral bioavailability. It has the potential to be a neuroprotective agent.
JOURNAL OF MEDICINAL CHEMISTRY
(2022)
Article
Biochemistry & Molecular Biology
Margherita Mastromarino, Mauro Niso, Carmen Abate, Ewgenij Proschak, Mariam Dubiel, Holger Stark, Marian Castro, Enza Lacivita, Marcello Leopoldo
Summary: Long-chain arylpiperazine scaffold is a versatile template for designing CNS drugs targeting serotonin and dopamine receptors. This study synthesized and evaluated ten new arylpiperazine derivatives with affinity profiles at serotonin and dopamine receptors, aiming to treat ASD or psychosis. The new compounds incorporated antioxidant fragments to counteract oxidative stress. Compound 12a showed an affinity profile compatible with antipsychotic activity, while compound 9b had an affinity profile consistent with ASD studies. Both compounds also had antioxidant properties.
Article
Biochemistry & Molecular Biology
Rosalba Leuci, Leonardo Brunetti, Antonio Laghezza, Luca Piemontese, Antonio Carrieri, Leonardo Pisani, Paolo Tortorella, Marco Catto, Fulvio Loiodice
Summary: A new series of aryloxyacetic acids were synthesized and tested as agonists for peroxisome proliferator-activated receptors (PPARs) and inhibitors for fatty acid amide hydrolase (FAAH). Some compounds showed interesting dual activity, which could potentially be used as a new therapeutic strategy for Alzheimer's disease (AD). These compounds also exhibited moderate activity against acetylcholinesterase (AChE) and had some inhibitory effect on A beta peptide aggregation, suggesting the feasibility of simultaneous multi-target activity towards PPARs, FAAH, and AChE. This pharmacological profile represents a promising line of research for the development of novel treatments for AD.
Article
Chemistry, Medicinal
Fredrik Ekstrom, Andrea Gottinger, Nina Forsgren, Marco Catto, Luca G. Iacovino, Leonardo Pisani, Claudia Binda
Summary: Multitarget directed ligands (MTDLs) are a promising approach to tackle the complexity of multifactorial pathologies. In the treatment of Alzheimer's disease, the synergistic inhibition of monoamine oxidase B (MAO B) and acetylcholinesterase (AChE) is believed to have a potentiated effect. Compound 1 showed tight-binding inhibition of MAO B and shape complementarity with the AChE enzymatic gorge, providing structural templates for the development of dual MAO B and AChE inhibitors.
ACS MEDICINAL CHEMISTRY LETTERS
(2022)
Article
Chemistry, Medicinal
Robert W. Garvey, Enza Lacivita, Mauro Niso, Beata Duszynska, Paul E. Harris, Marcello Leopoldo
Summary: This study reports the design, synthesis, and characterization of two novel fluorescent probes for the 5-HT1A receptor. One of the probes has the ability to selectively label the 5-HT1A receptor in pancreatic islet cells and shows useful properties for further characterization of this receptor's role.
Article
Chemistry, Medicinal
Margherita Mastromarino, Maria Favia, Igor A. Schepetkin, Lylia N. Kirpotina, Ewa Trojan, Mauro Niso, Antonio Carrieri, Monika Leskiewicz, Magdalena Regulska, Massimiliano Darida, Francesco Rossignolo, Stefano Fontana, Mark T. Quinn, Agnieszka Basta-Kaim, Marcello Leopoldo, Enza Lacivita
Summary: Formyl peptide receptor 2 (FPR2) agonists, including the newly identified ureidopropanamide derivatives, show promising potential in resolving inflammation and treating neurodegenerative disorders with underlying chronic neuroinflammation. Computational studies provide insights into the interactions between these compounds and FPR2. In vitro and in vivo experiments demonstrate the anti-inflammatory effects and improved mitochondrial function of selected compounds.
JOURNAL OF MEDICINAL CHEMISTRY
(2022)
Article
Biochemistry & Molecular Biology
Dario P. Anobile, Mauro Niso, Adrian Puerta, Stephanie M. Fraga Rodrigues, Francesca S. Abatematteo, Amir Avan, Carmen Abate, Chiara Riganti, Elisa Giovannetti
Summary: A new sigma-2 receptor ligand FA4 was synthesized and evaluated for its anti-proliferative, pro-apoptotic, and anti-migratory activity on PDAC primary cell cultures. The results showed that FA4 effectively inhibited the aggressive and chemoresistant behavior of PDAC, with significant antiproliferative and antimigratory effects.
Review
Chemistry, Multidisciplinary
Leonardo Pisani, Marco Catto, Giovanni Muncipinto, Orazio Nicolotti, Antonio Carrieri, Mariagrazia Rullo, Angela Stefanachi, Francesco Leonetti, Cosimo Altomare
Summary: The coumarin core is a recurring structural motif that can be used to design biologically active small molecules with diverse pharmacological activities.
FRONTIERS IN CHEMISTRY
(2022)
Article
Biochemistry & Molecular Biology
Bashar M. Thejer, Vittoria Infantino, Anna Santarsiero, Ilaria Pappalardo, Francesca S. Abatematteo, Sarah Teakel, Ashleigh Van Oosterum, Robert H. Mach, Nunzio Denora, Byung Chul Lee, Nicoletta Resta, Rosanna Bagnulo, Mauro Niso, Marialessandra Contino, Bianca Montsch, Petra Heffeter, Carmen Abate, Michael A. Cahill
Summary: Sigma-2 receptor (S2R) is functionally associated with both transmembrane protein TMEM97 and translocator protein (TSPO). This study provides evidence of the interaction between S2R and TSPO, as well as the physical colocalization of TMEM97 and TSPO in certain cancer cells. Additionally, the role of S2R-interacting partner PGRMC1 was clarified. This is the first suggestion of a functional interaction between TSPO and TMEM97, which can be influenced by S2R ligands.
INTERNATIONAL JOURNAL OF MOLECULAR SCIENCES
(2023)
Article
Chemistry, Medicinal
Francesca Serena Abatematteo, Maria Majellaro, Bianca Montsch, Ruben Prieto-Diaz, Mauro Niso, Marialessandra Contino, Angela Stefanachi, Chiara Riganti, Giuseppe Felice Mangiatordi, Pietro Delre, Petra Heffeter, Eddy Sotelo, Carmen Abate
Summary: Sigma receptor subtypes, sigma 1 and sigma 2, are potential targets for cancer and Alzheimer's disease therapy. Novel specific fluorescent ligands have been developed, including compounds 19 (sigma pan affinity) and 29 (sigma 2 selective), which show specificity for sigma 2 receptors and can be used as powerful tools for studying these receptors.
JOURNAL OF MEDICINAL CHEMISTRY
(2023)
Article
Chemistry, Medicinal
Mariagrazia Rullo, Gabriella La Spada, Daniela Valeria Miniero, Andrea Gottinger, Marco Catto, Pietro Delre, Margherita Mastromarino, Tiziana Latronico, Sara Marchese, Giuseppe Felice Mangiatordi, Claudia Binda, Anna Linusson, Grazia Maria Liuzzi, Leonardo Pisani
Summary: A series of 5-substituted-1H-indazoles were designed and tested as inhibitors of human monoamine oxidase A and B through a hybridization strategy. Among the modifications, the introduction of 1,2,4-oxadiazole ring based on bioisostere returned the most potent and selective inhibitor for MAO B. The inhibitory mechanism of compound 20 on hMAO B was investigated through molecular docking simulations, enzymatic kinetics analysis, and thermal stability curves.
EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
(2023)
Article
Biochemistry & Molecular Biology
Marco Paolino, Mariagrazia Rullo, Samuele Maramai, Modesto de Candia, Leonardo Pisani, Marco Catto, Claudia Mugnaini, Antonella Brizzi, Andrea Cappelli, Massimo Olivucci, Federico Corelli, Cosimo D. Altomare
Summary: Neurodegenerative diseases are complex disorders characterized by protein misfolding, oxidative stress, and neuroinflammation, resulting in neuronal loss and cognitive dysfunction. In this study, the researchers designed and synthesized a library of cinnamic acid-inspired compounds that can modulate their activity under light irradiation. These compounds showed selective inhibition of acetylcholinesterase and monoamine oxidase B, which are associated with Alzheimer's disease. Molecular docking studies were conducted to understand the differences in inhibitory potency between the E and Z diastereomers of the best-performing compound. These findings provide a potential avenue for the development of innovative multitarget photo-switch drugs for neurodegenerative diseases.
RSC MEDICINAL CHEMISTRY
(2022)
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)