Article
Chemistry, Medicinal
Rong-Zhen Wu, Huai-Yu Zhou, Jing-Feng Song, Qiao-Hong Xia, Wei Hu, Xiao-Dong Mou, Xun Li
Summary: This paper summarizes the current research status and prospects for more effective and safer chemotherapeutic drugs for chronic latent toxoplasmosis infection caused by the Toxoplasma parasite. The emphasis is on possible molecular biotargets and the binding modes and structure-activity relationship profiles of corresponding inhibitors. The information provided in this paper is expected to help in the further identification of more effective chemotherapeutic interventions for preventing and treating zoonotic infections caused by Toxoplasma gondii.
JOURNAL OF MEDICINAL CHEMISTRY
(2021)
Article
Chemistry, Multidisciplinary
Andres F. Yepes, Jorge Quintero-Saumeth, Wilson Cardona-Galeano
Summary: This study focused on proposing a plausible action mechanism by which the active compounds inhibit T. cruzi growth by targeting DHFR. Computational approaches revealed potential pharmacokinetic properties for the top-three active compounds. The results suggest that these active hybrids could be a privileged scaffold for future anti-Chagas drug development.
Article
Biochemistry & Molecular Biology
Ivan Beltran-Hortelano, Veronica Alcolea, Maria Font, Silvia Perez-Silanes
Summary: This article provides an overview of validated targets involved in various pathways of the Trypanosoma cruzi parasite and explores the molecular basis for finding new effective treatments for Chagas disease. The review also compiles all reported inhibitors against these targets, serving as a reference for future research in this field.
BIOORGANIC & MEDICINAL CHEMISTRY
(2022)
Article
Biochemistry & Molecular Biology
Han Wu, Hongtong Chen, Jungan Zhang, Xinxin Hu, Chunyang Xie, Weiting Cao, Ziqi Zhao, Zengshuo Xiao, Yixin Ren, Luyao Dong, Peiyi Sun, Xuefu You, Xinyi Yang, Wei Hong, Hao Wang
Summary: This study found that 1,3-diamino-7H-pyrrolo[3,2-f]quinazoline (PQZ) compounds exhibited strong antibacterial activities against A. baumannii, especially multidrug-resistant strains. These compounds showed better antibacterial effects compared to traditional antibiotics, and their combination with inhibitors reduced the required dosage and prevented resistance. These findings suggest that PQZ compounds could be a promising scaffold for the development of folate-metabolism inhibitors against multidrug-resistant A. baumannii.
Article
Biochemistry & Molecular Biology
Adullah Alotaibi, Godwin U. Ebiloma, Roderick Williams, Ibrahim A. Alfayez, Manal J. Natto, Sameah Alenezi, Weam Siheri, Malik AlQarni, John O. Igoli, James Fearnley, Harry P. De Koning, David G. Watson
Summary: Ethanolic extracts of temperate zone propolis from the UK and Poland exhibited anti-trypanosomal activity, with compounds like naringenin 4 ',7-dimethyl ether and 4 '-methoxykaempferol showing the highest activity. Different compounds were isolated and characterized, showing varying levels of activity against drug-resistant strains of T. brucei and L. mexicana, without a clear structure-activity relationship observed. Multiple compounds from temperate propolis have anti-kinetoplastid activity.
Article
Biochemistry & Molecular Biology
Ali Mijoba, Esteban Fernandez-Moreira, Nereida Parra-Gimenez, Sandra Espinosa-Tapia, Zuleyma Blanco, Hegira Ramirez, Jaime E. Charris
Summary: A series of benzocycloalkanone derivatives were synthesized as potential antimalarial and antitrypanosomal agents. The compounds were prepared through direct coupling of preformed 4-substituted benzaldehyde and indanone or tetralone substitutes using aldol condensation. Only three compounds showed significant antimalarial activity, while all compounds exhibited marginal activity as trypanocidals. Further investigation is warranted for this new class of Michael acceptor agents.
Article
Biochemistry & Molecular Biology
Katharina Possart, Fabian C. Herrmann, Joachim Jose, Thomas J. Schmidt
Summary: This article investigates the drug treatment of tropical diseases caused by parasites. Through enzyme analysis and computational screening, several compounds with dual inhibitory effects were identified, which could potentially be used for the development of new drugs.
Article
Multidisciplinary Sciences
Sara Teixeira de Macedo-Silva, Gonzalo Visbal, Gabrielle Frizzo Souza, Mayara Roncaglia dos Santos, Simon B. Cammerer, Wanderley de Souza, Juliany Cola Fernandes Rodrigues
Summary: This study found that benzylamines have anti-parasitic activity against Leishmania amazonensis and affect the structure of the cell membrane and mitochondria by blocking the sterol synthesis pathway. These results suggest that benzylamines may be promising pharmaceutical leads for the treatment of leishmaniasis.
SCIENTIFIC REPORTS
(2022)
Article
Pharmacology & Pharmacy
Christian Espinosa-Bustos, Mariana Ortiz Perez, Alonzo Gonzalez-Gonzalez, Ana Maria Zarate, Gildardo Rivera, Javier A. Belmont-Diaz, Emma Saavedra, Mauricio A. Cuellar, Karina Vazquez, Cristian O. Salas
Summary: In this study, a series of new amino naphthoquinone derivatives were synthesized and evaluated for their activity against Trypanosoma cruzi strains. Compounds 2e and 7j showed the lowest IC50 values and 7j exhibited higher activity and selectivity than the reference drug benznidazole. Molecular docking studies revealed that 7j had a good interaction profile on T. cruzi trypanothione reductase (TcTR) and it was predicted to have a favorable pharmacokinetic profile for oral administration.
Article
Engineering, Chemical
Sarang S. Nath
Summary: A novel approach based on graph theory is used to identify the complete set of thermodynamically consistent sub-cyclic routes that produce a net positive reaction flux in the dihydrofolate reductase (DHFR) network. The method also selects the minimal set of linearly independent rate equations (mechanisms) from the net positive flux cycles. By quantifying the steady-state flux through these sub-cycles, the sub-cycle that generates the maximum flux is determined as the most probable mechanism of the pathway. This analysis is applied to both wild-type and mutant Escherichia coli DHFR systems, providing insights into the kinetic mechanism of complex cyclic reaction networks.
INDUSTRIAL & ENGINEERING CHEMISTRY RESEARCH
(2022)
Article
Immunology
Maria Angelica Burgos-Reyes, Lidia Baylon-Pacheco, Patricia Espiritu-Gordillo, Silvia Galindo-Gomez, Victor Tsutsumi, Jose Luis Rosales-Encina
Summary: Leishmaniasis, caused by intracellular protozoan parasite Leishmania, is a challenging disease to treat. A potential vaccine candidate, the LmxMBA gene, was identified and tested in a murine model, showing reduced lesion size and parasitic load. Vaccination with pVAX1::LmxMBA induced a T helper 1 response characterized by increased IgG2a/IgG1 ratio and lymphoproliferative response, supporting it as a preventive strategy against L. mexicana infection.
JOURNAL OF IMMUNOLOGY RESEARCH
(2021)
Article
Biochemistry & Molecular Biology
Elena R. Lozovsky, Rachel F. Daniels, Gavin D. Heffernan, David P. Jacobus, Daniel L. Hartl
Summary: The study revealed that chemically related drugs exhibit similar adaptive topographies, and higher-order interactions are likely to be of little value as an advisory tool in the choice of lead compounds for drug development.
MOLECULAR BIOLOGY AND EVOLUTION
(2021)
Article
Chemistry, Medicinal
Elisabetta Di Bello, Beatrice Noce, Rossella Fioravanti, Clemens Zwergel, Sergio Valente, Dante Rotili, Giulia Fianco, Daniela Trisciuoglio, Marina M. Mourao, Policarpo Sales, Suzanne Lamotte, Eric Prina, Gerald F. Spath, Cecile Haberli, Jennifer Keiser, Antonello Mai
Summary: Neglected tropical diseases (NTDs) cause significant morbidity and mortality worldwide. Current antiparasitic drugs have limitations and the use of epigenetic drugs has been suggested as a strategy for NTD treatment. In this study, potential drugs were identified for further development and optimization.
ACS INFECTIOUS DISEASES
(2022)
Article
Biochemistry & Molecular Biology
Claudia Lopez-Lira, Ricardo A. Tapia, Alejandra Herrera, Michel Lapier, Juan D. Maya, Jorge Soto-Delgado, Allen G. Oliver, A. Graham Lappin, Eugenio Uriarte
Summary: The design and synthesis of new 2-phenyl(pyridinyl)benzimidazolequinones and their 5-phenoxy derivatives demonstrate potent anti-Trypanosoma cruzi activity. Compound 11a shows significantly higher activity compared to nifurtimox. Molecular docking studies suggest that these compounds could have a multitarget profile.
BIOORGANIC CHEMISTRY
(2021)
Article
Biochemistry & Molecular Biology
Kyung-Hwa Baek, Trong-Nhat Phan, Satish R. Malwal, Hyeryon Lee, Zhu-Hong Li, Silvia N. J. Moreno, Eric Oldfield, Joo Hwan No
Summary: SQ109 is an anti-tubercular drug candidate that has shown potent activity against protozoan parasites including Leishmania, Trypanosoma cruzi, and Toxoplasma gondii in vitro. It has demonstrated efficacy in mouse models of T. cruzi and T. gondii infections, but moderate efficacy in models of Trypanosoma brucei and Leishmania donovani infections. Metabolites of SQ109 also exhibit activity against protozoan parasites in vitro.
Article
Biochemistry & Molecular Biology
Elena Sthephanie Castro-Silva, Martiniano Bello, Martha Cecilia Rosales-Hernandez, Jose Correa-Basurto, Maricarmen Hernandez-Rodriguez, Daniel Villalobos-Acosta, Juan Vicente Mendez-Mendez, Alan Estrada-Perez, Jesus Murillo-Alvarez, Mauricio Munoz-Ochoa
Summary: This study found that fucosterol extracted from an algal source has inhibitory effects on A beta(1-42) aggregation, which could potentially prevent the development of Alzheimer's disease.
JOURNAL OF BIOMOLECULAR STRUCTURE & DYNAMICS
(2021)
Article
Biochemistry & Molecular Biology
M. J. Fragoso-Vazquez, D. Mendez-Luna, M. C. Rosales-Hernandez, G. R. Luna-Palencia, A. Estrada-Perez, Benedicte Fromager, I Vasquez-Moctezuma, J. Correa-Basurto
Summary: The study evaluated the hybrid compound Gln-VPA using various methods, showing its anti-proliferative effects and inhibition of glutaminase activity in HeLa cells. LC-MS metabolomics studies indicated that Gln-VPA and DON have different biological targets in the cell death mechanism.
MOLECULAR DIVERSITY
(2021)
Article
Biochemistry & Molecular Biology
Alberto Martinez-Munoz, Jose Correa-Basurto, Martiniano Bello
Summary: In this study, the mechanism of how indomethacin forms complexes with folate-G4-PAMAM dendrimer was explored using ligand diffusion molecular dynamic simulations (LDMDSs) and molecular mechanics-generalized-born surface area (MMGBSA) approach. The results showed that the folate-G4-PAMAM dendrimer can bind indomethacin more effectively, indicating better encapsulation.
JOURNAL OF BIOMOLECULAR STRUCTURE & DYNAMICS
(2022)
Article
Chemistry, Medicinal
David Mendez-Luna, Loreley Araceli Morelos-Garnica, Juan Benjamin Garcia-Vazquez, Martiniano Bello, Itzia Irene Padilla-Martinez, Manuel Jonathan Fragoso-Vazquez, Alfonso Duenas Gonzalez, Nuria De Pedro, Jose Antonio Gomez-Vidal, Humberto Lubriel Mendoza-Figueroa, Jose Correa-Basurto
Summary: The study designed and synthesized three new compounds with high affinity for the GPER binding site, which showed growth inhibitory activity in cancer cell lines without side effects. In silico studies revealed the binding modes and energetic features of the compounds on GPER, indicating potential for new compounds with growth inhibitory activities against nonconventional GPER cell models.
Article
Multidisciplinary Sciences
Yudibeth Sixto-Lopez, Jose Correa-Basurto, Martiniano Bello, Bruno Landeros-Rivera, Jose Antonio Garzon-Tiznado, Sarita Montano
Summary: The SARS-CoV-2 virus has three lineages circulating worldwide, two of which have been found with three mutations among the Mexican population; these mutations significantly affect the structural behavior of the S protein and its binding with inhibitors; further experimental studies are needed to explore the clinical implications of these effects.
SCIENTIFIC REPORTS
(2021)
Review
Biochemistry & Molecular Biology
Leticia Guadalupe Fragoso-Morales, Jose Correa-Basurto, Martha Cecilia Rosales-Hernandez
Summary: Alzheimer's disease is a major human dementia characterized by memory loss associated with oxidative stress in brain cells. Overexpression of NADPH oxidase in AD leads to the production of large amounts of reactive oxygen species, damaging brain cells and vasculature, making it a potential therapeutic target for AD.
Article
Cell Biology
Yudibeth Sixto-Lopez, Emilie Marhuenda, Juan Benjamin Garcia-Vazquez, Manuel Jonathan Fragoso-Vazquez, Martha Cecilia Rosales-Hernandez, Oscar Zacarias-Lara, David Mendez-Luna, Jose Antonio Gomez-Vidal, David Cornu, Bakalara Norbert, Jose Correa-Basurto
Summary: Glioblastoma multiforme accounts for 70% of primary malignancies of the central nervous system, with a median survival after treatment of around 15 months. Research has identified HDAC inhibitors as showing antiproliferative properties in 3D cultures, suggesting they may be a key target for future therapeutic studies.
CELLULAR AND MOLECULAR NEUROBIOLOGY
(2022)
Article
Biochemistry & Molecular Biology
Ozvaldo Linares-Anaya, Alcives Avila-Sorrosa, Francisco Diaz-Cedillo, Luis Angel Gil-Ruiz, Jose Correa-Basurto, Domingo Salazar-Mendoza, Adrian L. Orjuela, Jorge Ali-Torres, Maria Teresa Ramirez-Apan, David Morales-Morales
Summary: Two benzo[d][1,3]azoles 2-substituted with benzyl- and allyl-sulfanyl groups, BTA-1 and BMZ-2, showed promising cytotoxic activities against six human cancer cell lines in vitro. BMZ-2 exhibited comparable inhibitory effects to tamoxifen in some cases and displayed low cytotoxicity against healthy cells. Computational molecular docking studies revealed the affinity and possible interactions of both compounds with the tamoxifen binding site on ER alpha and GPER receptors.
Article
Multidisciplinary Sciences
R. Flores-Mejia, M. J. Fragoso-Vazquez, L. G. Perez-Blas, A. Parra-Barrera, S. S. Hernandez-Castro, A. R. Estrada-Perez, J. Rodrigues, E. Lara-Padilla, A. Ortiz-Morales, J. Correa-Basurto
Summary: The study investigates the chemical structure, cytotoxicity, and antiproliferative effects of G4-PAMAM, as well as its intracellular localization in the HMC-1 and K-562 cell lines. The results show that G4-PAMAM generates multivalent mass spectrum values and exhibits antiproliferative activity in both tumor cell lines. Additionally, the dendrimers were found in the cytoplasm and nucleus of the studied tumor cells.
SCIENTIFIC REPORTS
(2021)
Article
Chemistry, Medicinal
Ulises Martinez-Ortega, Diego Figueroa-Figueroa, Francisco Hernandez-Luis, Rodrigo Aguayo-Ortiz
Summary: This study conducted molecular dynamics simulations of the interaction between masitinib (MST) and SARS-CoV-2 main protease (M-pro), identifying factors influencing the stability of the complex and providing valuable insights for the design of new MST analogs as potential treatments for COVID-19.
Article
Chemistry, Medicinal
Astrid Rivera-Antonio, Martha Cecilia Rosales-Hernandez, Irving Balbuena-Rebolledo, Jose Martin Santiago-Quintana, Jessica Elena Mendieta-Wejebe, Jose Correa-Basurto, Juan Benjamin Garcia-Vazquez, Efren Venancio Garcia-Baez, Itzia I. Padilla-Martinez
Summary: A novel synthesis method for (E)-2-hydroxy-alpha-aminocinnamic acids was reported, demonstrating their antioxidant properties and ability to scavenge free radicals, inhibit MPO, with low cytotoxicity. The compounds show promising potential for further exploration as therapeutic agents for chronic diseases related to MPO activity.
Article
Chemistry, Multidisciplinary
Eduardo Hernandez-Vazquez, Samuel Estrada-Soto, Norma Lumbreras-Zavala, Martin Mundo-Campuzano, Fabiola Chavez-Silva, Rafael Villalobos-Molina, Francisco Hernandez-Luis
Summary: Pre-formulating 1,5-diarylpyrazoles with polyvinylpyrrolidone enhances their antidiabetic activity and improves lipidic profile and antidyslipidemic properties. Pre-formulation also enhances the antihyperglycemic activity of the dehalogenated pyrazole without causing hypoglycemia.
Article
Chemistry, Medicinal
Marcela A. Lopez-Sanchez, Maria del Carmen Garcia-Rodriguez, Rodrigo Aguayo-Ortiz, Estefani Hernandez-Cruz, Diego I. Figueroa-Figueroa, Francisco Hernandez-Luis
Summary: In this study, a new series of quinazolin-2,4,6-triamine derivatives were synthesized and evaluated for their potential biological activities as xanthine oxidase inhibitors, superoxide scavengers, and toxicological profile screening. Among the synthesized compounds, B1 showed better inhibitory activity against bovine xanthine oxidase compared to allopurinol. Furthermore, B1, B2, and B13 exhibited superior superoxide scavenging effects compared to allopurinol. In terms of cytotoxicity, B1 was found to be less toxic than methotrexate on HCT15 cancer cells. Apoptosis studies on mice cells showed that B1 and B2 had similar effects to CrO3 in inducing apoptosis, while the effect of B13 was similar to DMSO and the control group. Lastly, B1, B2, and B13 did not induce genotoxicity in a micronuclei murine model when compared to CrO3.
Article
Chemistry, Multidisciplinary
Cesar Mendoza-Martinez, Michail Papadourakis, Salome Llabres, Arun A. Gupta, Paul N. Barlow, Julien Michel
Summary: In this study, the selectivity of a drug-like small molecule in modulating the disorder-to-order transition of a protein is investigated. The results show that the molecule induces order in a specific region of the protein, shifting the balance of the protein complex. This research is of significance in targeting intrinsically disordered regions in medicinal chemistry.
Review
Medicine, General & Internal
Norma Del C. Galindo-Sevilla, Nilson A. Contreras-Carreto, Araceli Rojas-Bernabe, Javier Mancilla-Ramirez
Summary: The COVID-19 pandemic has raised concerns among mothers and breastfeeding women about the possible transmission of the virus through breast milk. However, there is no evidence of vertical transmission, and the risk of horizontal transmission to infants is similar to the general population. Breastfeeding may even have a beneficial effect on the clinical course of COVID-19 in newborns.
GACETA MEDICA DE MEXICO
(2021)
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)
