Article
Chemistry, Multidisciplinary
Surendar Chitti, Kevin Van Calster, Davie Cappoen, Adinarayana Nandikolla, Yogesh Mahadu Khetmalis, Paul Cos, Banoth Karan Kumar, Sankaranarayanan Murugesan, Kondapalli Venkata Gowri Chandra Sekhar
Summary: In the search for new anti-mycobacterial agents, the importance of imidazo-[2,1-b]-thiazole and benzo-[d]-imidazo-[2,1-b]-thiazole carboxamide derivatives was revealed. Several series of novel derivatives were designed, predicted, and synthesized. The most active derivatives showed selective inhibition against Mycobacterium tuberculosis and no activity against non-tuberculous mycobacteria. Molecular docking and dynamics studies were also conducted to understand the binding pattern and stability of the protein-ligand complex.
Article
Chemistry, Medicinal
Menna A. Ewida, Heba A. Ewida, Mahmoud S. Ahmed, Heba Abdelrasheed Allam, Ramzia ElBagary, Riham F. George, Hanan H. Georgey, Hussein El-Subbagh
Summary: A series of imidazo[2,1-b]thiazole and benzo[d]imidazo[2,1-b]thiazole analogs were synthesized and evaluated for their inhibitory effects on IDO1, with several compounds showing promising activity. Molecular modeling simulations suggested that these analogs can chelate iron(III) within the IDO1 binding pocket and have better binding affinity through hydrophobic interactions.
ARCHIV DER PHARMAZIE
(2021)
Article
Biochemistry & Molecular Biology
Rawan M. Sbenati, Mohammad H. Semreen, Ahlam M. Semreen, Mahmoud K. Shehata, Fai M. Alsaghir, Mohammed El-Gamal
Summary: This article reviewed the potential anticancer properties of imidazo[2,1-b]thiazole derivatives, focusing on their biological characteristics and structure-activity relationship (SAR). Reports published in the literature from 2011 to 2020 were the main focus of this review.
BIOORGANIC & MEDICINAL CHEMISTRY
(2021)
Article
Chemistry, Organic
Huda K. Mahmoud, Sobhi M. Gomha, Thoraya A. Farghaly, Hanem M. Awad
Summary: The study synthesized four new series of thiazolylimidazothiazole derivatives and characterized their structures, evaluating their activity against human cancer cells in vitro. The promising results suggest the potential for further investigation into these novel compounds.
POLYCYCLIC AROMATIC COMPOUNDS
(2021)
Article
Biochemistry & Molecular Biology
Tianming Zhao, Yu Yang, Jing Yang, Youbao Cui, Zhi Cao, Daiying Zuo, Xin Zhai
Summary: Standard chemotherapy and personalized target therapies are commonly used in advanced nonsmall cell lung cancer patients, but multidrug resistance and tumor metastasis often lead to decreased efficacy, associated with epithelial-mesenchymal transition (EMT). The transcription factor Twist1 plays a key role in promoting EMT, MDR, and metastasis, making it a potential target for developing antitumor therapies. By designing novel benzo[d] imidazo[2,1-b]thiazole derivatives with 1,3,4-oxadiazole moiety based on the structure of Twist1 inhibitor harmine, a compound with superior anti-proliferative activity and Twist1 down-regulation potential was identified as a promising lead for antineoplastic treatment.
BIOORGANIC & MEDICINAL CHEMISTRY
(2021)
Article
Immunology
Collin J. Fitzpatrick, Rajini R. Mudhasani, Louis A. Altamura, Catherine E. Campbell, Julie P. Tran, Brett F. Beitzel, Aarthi Narayanan, Cynthia L. de la Fuente, Kylene Kehn-Hall, Jeffrey M. Smith, Connie S. Schmaljohn, Aura R. Garrison
Summary: This study utilized RPPA to compare global alterations in host proteome following infection with different strains of Junin virus (JUNV). Several phosphorylated proteins related to entry and early replication events were identified, and the alterations of three proteins (p38 MAPK, HSP27, and NF kappa B) were confirmed. Further research showed that inhibiting p38 MAPK or HSP27 reduced JUNV replication significantly.
FRONTIERS IN CELLULAR AND INFECTION MICROBIOLOGY
(2022)
Article
Chemistry, Medicinal
Huda K. Mahmoud, Abdelwahed R. Sayed, Marwa M. Abdel-Aziz, Sobhi M. Gomha
Summary: This study aims to synthesize bioactive hybrid pharmacophores and assess their antimycobacterial activity. The results showed that derivative 7b exhibited the most promising antimycobacterial activity among the tested compounds. The structure-activity relationship studies indicated that the substituent on the thiazole ring was related to the antimycobacterial activity.
MEDICINAL CHEMISTRY
(2022)
Article
Chemistry, Inorganic & Nuclear
Ai-hui Zhou, Tao Han, Peng-bin Si, Xiao-qing Liu, Ming-yu Teng, Guo-li Huang, Bo Liu, Qin Wang, Jie Zhang
Summary: Eight iridium complexes were synthesized for applications in organic optical function materials, using 3-methyl-6-(naphthalen-2-yl)-imidazo[2,1-b]thiazole (mn2mt) and 3-methyl-6-(naphthalene-1-yl)imidazo[2,1-b]thiazole (mn1mt) as primary ligands, and picolinic acid (pic), isoquinoline-3-carboxylic acid (3-IQA), quinoline-2-carboxylic acid (2-QA), and 2-(pyridin-2-yl)phenol (hppy) as auxiliary ligands. The structures, photoluminescence, and electrochemical properties of the complexes were thoroughly investigated. Additionally, LEDs based on InGaN chip excitation showed good performance when using the synthesized IrIII complexes as emitters.
JOURNAL OF ORGANOMETALLIC CHEMISTRY
(2023)
Article
Chemistry, Medicinal
Rahul Singh, Ravinder Kumar, Ashalata Roy, Pabitra Mohan Behera, Ankit K. Atri, Kushvinder Kumar, Debasis Manna, Anshuman Dixit, Madhuri T. Patil, R. Mankamna Kumari, Surendra Nimesh, Deepak B. Salunke
Summary: IDO1 enzyme plays a crucial role in the progression of various diseases, and researchers have designed and synthesized new fused heterocyclic compounds to target this enzyme. The potential inhibitory activity of these compounds was evaluated, and docking studies revealed specific interactions between the compounds and the enzyme pocket.
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
(2023)
Article
Chemistry, Physical
Efe Dogukan Dincel, Gozde Hasbal-Celikok, Tugba Yilmaz-Ozden, Nuray Ulusoy-Guzeldemirci
Summary: A series of novel hydrazinecarbothioamide and 1,2,4-triazole-3-thione derivatives of imidazo[2,1b]thiazole were synthesized and evaluated for their antioxidant activity. The compounds 4i, 4j, 4k, and 4n exhibited the highest antioxidant activity and displayed stability in molecular docking and dynamic simulations.
JOURNAL OF MOLECULAR STRUCTURE
(2022)
Article
Pharmacology & Pharmacy
Jonna B. Westover, Shibani Naik, Kevin W. Bailey, Luci Wandersee, Vidyasagar R. Gantla, Brady T. Hickerson, Ken McCormack, Greg Henkel, Brian B. Gowen
Summary: This study evaluated the efficacy of ARN-75039, a fusion inhibitor, against pathogenic JUNV in a guinea pig infection model. The compound showed significant protection even when administered 6 days after viral challenge, suggesting a potential therapeutic option for mammarenaviral hemorrhagic fevers. Additionally, combination treatment of ARN-75039 with favipiravir resulted in improved survival outcomes in JUNV-challenged guinea pigs.
ANTIVIRAL RESEARCH
(2022)
Article
Biochemistry & Molecular Biology
Faika Basoglu, Nuray Ulusoy-Guzeldemirci, Gulsen Akalin-Ciftci, Serap Cetinkaya, Abdulilah Ece
Summary: This study focused on synthesizing imidazo[2,1-b]thiazole derivatives, characterizing them, and investigating their cytotoxic and apoptotic effects on glioma C6 cancer cell line, as well as their anticancer activities against focal adhesion kinase. Results showed that compounds with specific structures exhibited higher anticancer activities and FAK inhibitory activities, with molecular docking studies revealing their binding modes and critical interactions with amino acid residues in the active site, providing insights into developing new inhibitors against FAK.
CHEMICAL BIOLOGY & DRUG DESIGN
(2021)
Article
Biochemistry & Molecular Biology
Menna A. Ewida, Heba A. Ewida, Mahmoud S. Ahmed, Heba Abdelrasheed Allam, Ramzia ElBagary, Riham F. George, Hanan H. Georgey, Hussein El-Subbagh
Summary: In this study, novel series of 3-methyl-imidazo [2,1-b] thiazole-based analogs targeting DHFR were synthesized and evaluated for their inhibitory profile. Compounds 22 and 23 showed potent inhibition towards DHFR, promising cytotoxicity against breast cancer cell lines, and significant therapeutic effects in animal models. Molecular modeling simulations supported the high affinity binding potential of these compounds towards DHFR, while ADMET study suggested favorable pharmacokinetic properties for further development as DHFR inhibitors.
BIOORGANIC CHEMISTRY
(2021)
Article
Crystallography
Mezna Saleh Altowyan, Saied M. Soliman, Matti Haukka, Nora Hamad Al-Shaalan, Aminah A. Alkharboush, Assem Barakat
Summary: A new spirooxindole hybrid engrafted imidazo[2,1-b]thiazole core structure was synthesized via [3+2] cycloaddition reaction. The absolute configuration was determined by single-crystal X-ray diffraction analysis. Hirshfeld and DFT calculations confirmed the crystal stability and correlation between calculated geometric parameters. TD-DFT and GIAO calculations were used to interpret the experimental UV-Vis and NMR spectra.
Review
Chemistry, Medicinal
Afnan Shahin, Seyed-Omar Zaraei, Shahed Alzuraiqi, Zahaa Abdulateef, Noora E. Abbas, Taleb H. Al-Tel, Mohammed El-Gamal
Summary: This article reviews the utilization of Imidazo[2,1-b]oxazole and 2,3-dihydroimidazo[2,1-b]oxazole ring systems as chemotherapeutic agents, with a focus on their biological activities and structure-activity relationships. It presents the antitubercular agent delamanid as one of the most important drugs in this class, providing detailed information on its structure-activity relationship, as well as preclinical and clinical trial data.
FUTURE MEDICINAL CHEMISTRY
(2023)
Article
Green & Sustainable Science & Technology
R. E. Coppola, D. Herranz, R. Escudero-Cid, N. Ming, N. B. D'Accorso, P. Ocon, G. C. Abuin
Article
Green & Sustainable Science & Technology
Jorge Bergamo, Ezequiel Rossi, Juan Martin Maffi, Laura De Angelis, Maria Ines Errea
SUSTAINABLE ENERGY TECHNOLOGIES AND ASSESSMENTS
(2020)
Article
Pharmacology & Pharmacy
Maria Natalia Pacho, Eugenio Nahuel Pugni, Johanna Briyith Diaz Sierra, Maria Laura Morell, Claudia Soledad Sepulveda, Elsa Beatriz Damonte, Cybele Carina Garcia, Norma Beatriz D'Accorso
Summary: The encapsulation of curcumin in PLGA nanoparticles showed promising antiviral activity against Zika virus, indicating that PLGA-CUR NPs are potential candidates for a drug formulation against human pathogenic flaviviruses.
JOURNAL OF PHARMACY AND PHARMACOLOGY
(2021)
Article
Polymer Science
Beatriz Guerrero-Leon, Graciela Corbino, Alain Dufresne, Maria Ines Errea, Norma D'Accorso, Nancy L. Garcia
Summary: The peel of Arapey Sweet Potato was utilized as a source of phenolic compounds for antioxidant activity, resulting in nanocapsules with high stability and thermal properties that demonstrated improved mechanical characteristics of PLA films when used as additives, suggesting potential applications for controlled release of antioxidants.
JOURNAL OF POLYMER RESEARCH
(2021)
Article
Energy & Fuels
Joana E. Tasque, Isabel N. Vega, Simon Marco, Pablo A. Raffo, Norma B. D'Accorso
Summary: The study compared the performance of polymer proppants synthesized with different fillers, and found that the composites prepared in presence of carbon black showed the most promising results, meeting the requirements for hydraulic fracturing with good conductivity and permeability similar to commercial polymeric and natural sand, as well as no generation of fines observed in the crushing test.
JOURNAL OF NATURAL GAS SCIENCE AND ENGINEERING
(2021)
Article
Polymer Science
Roxana E. Coppola, Fabricio N. Molinari, Norma B. D'Accorso, Graciela C. Abuin
Summary: The study presents a facile preparation method of an AEM using glutaraldehyde crosslinked polyvinyl alcohol nanofibers and poly[2-2'- (m-phenylene)-5-5' -bibenzimidazole] polymer reinforcement, showcasing good chemical stability and swelling resistance in a liquid alkaline water electrolyzer. The AEM exhibited high ionic conductivity and stable performance in terms of current density under different operating temperatures, indicating its potential as a cost-effective alternative material for electrolyzers.
POLYMERS FOR ADVANCED TECHNOLOGIES
(2021)
Article
Engineering, Chemical
Gabriel Lombardo, Mariana D. Sosa, Antonela Canneva, Nicolas G. Saggion, Graciela Rojas, Andrea Kaplan, R. Martin Negri, Norma B. D'Accorso
Summary: Superhydrophobic/oleophilic membranes based on covalent silanization of silica nanoparticles on metallic meshes were obtained to achieve highly efficient separation of oil/water mixtures. The membranes were prepared in a scalable two-step process and characterized using various techniques. The modified nanoparticles provided chemical resistance to hard water while maintaining strong hydrophobicity, enabling the separation of oil-water mixtures.
SEPARATION AND PURIFICATION TECHNOLOGY
(2022)
Article
Biochemistry & Molecular Biology
C. A. Rodriguez-Ramirez, Alain Dufresne, Norma D'Accorso, Nancy Lis Garcia
Summary: A chemical modification method was developed to modify the surface of cellulose nanofibrils (CNFs) from an ordinary bamboo. The modified CNFs were used as nano-fillers to improve the properties of films based on polylactic acid (PLA). The study showed that the addition of 5% modified CNFs resulted in improved thermal, mechanical, and surface properties of the films.
INTERNATIONAL JOURNAL OF BIOLOGICAL MACROMOLECULES
(2022)
Article
Polymer Science
Roxana E. Coppola, Hernan E. Lozano, Mario Contin, Antonela Canneva, Fabricio N. Molinari, Graciela C. Abuin, Norma B. D'Accorso
Summary: Thin films of poly(2,5-benzimidazole) (ABPBI) were prepared and studied for their sorption properties with aqueous CuSO4 solutions. Spectroscopic analysis revealed a strong interaction between Cu(II) and the nitrogen groups of ABPBI. The best conditions for Cu(II) uptake were found to be pH = 5 and a soaking time of 60 min, with the sorption isotherm fitting well to the Langmuir equation and a maximum sorption capacity of 1.5 mmol g(-1). Elution studies using hydrochloric acid solution resulted in the complete removal of bonded Cu(II). The surface morphology of the membranes remained unchanged after sorption and elution experiments. ABPBI shows potential as an alternative polymer for the development of materials for heavy metal removal.
POLYMER INTERNATIONAL
(2022)
Article
Engineering, Chemical
Leila M. Saleh M. Medina, Antonela Canneva, Fabricio N. Molinari, Norma D'Accorso, R. Martin Negri
Summary: The objective of this study is to develop absorbent materials based on PDMS for efficient absorption of organic solvents. The materials showed high absorption capacities for various solvents and exhibited demulsification properties and absorption of oleophilic compounds. The reusability of the materials makes them suitable for water remediation applications.
POLYMER ENGINEERING AND SCIENCE
(2023)
Article
Chemistry, Multidisciplinary
M. Veronica Rivas, Daniel Musikant, Rocio Diaz Pena, Daniela Alvarez, Luciana Pelazzo, Ezequiel Rossi, Karina D. Martinez, Maria I. Errea, Oscar E. Perez, Oscar Varela, Adriana A. Kolender
Summary: Polymeric nanoparticles synthesized from D-galactose were used to efficiently encapsulate cilostazol and showed enhanced anti-inflammatory activity, holding great promise for improving its therapeutic administration.
Article
Microbiology
Gonzalo N. Cagnola, J. Nicolas Cabrera, R. Martin Negri, Norma B. D'Accorso, Leonardo Lizarraga, M. Julia Pettinari
Summary: Different strategies including the addition of multi-walled carbon nanotubes (MWCNT) and exposure to bromine vapors in the presence and absence of UV irradiation were tested to reduce biofilm formation of Cobetia marina and Marinobacter hydrocarbonoclasticus on PDMS coated aluminum and cellulose acetate surfaces. The surface modifications led to significant reductions in biofilm formation, with the highest reduction of 30% observed with exposure to Br-2(g). A quantitative theoretical model based on the effective roughness parameter, Ra-eff, was introduced to correlate biofouling reduction with surface properties. The model accounted for morphological changes and the inclusion of bacteria into large surface wells observed with AFM.
CURRENT MICROBIOLOGY
(2023)
Article
Chemistry, Applied
E. Rossi, A. G. Salvayd, M. I. Erreab, M. L. Foresti
Summary: In this study, sorbitol was used as a capping agent in the drying of bacterial nano-cellulose (BNC) to prevent irreversible hydrogen bonding between adjacent cellulose nanofibrils. The effects of different sorbitol:BNC mass ratios, drying strategies, and redispersion methods on the water redispersibility of dried BNC were investigated. The results showed that sorbitol significantly limited irreversible hydrogen bonding and allowed for redispersed BNC suspensions with characteristics similar to those of never-dried ones.
FOOD HYDROCOLLOIDS
(2023)
Review
Chemistry, Multidisciplinary
Veronica E. Manzano, Norma B. D'Accorso
Summary: Basic science plays a crucial role in driving new developments across various industries, and the increasing interaction between academic science and industry has drawn significant attention in recent years. This article highlights the development and transfer of rational materials from basic science to the productive sector, including hydrophobic coatings for aerospace applications, hydrogels for the oil and gas industry, and polymers for the removal of heavy metals. The inspiration drawn from nature, such as superhydrophobicity and superhydrophilicity, has also paved the way for the creation of membranes for separating hydrocarbons and water in subterranean water treatment for the oil and gas industry. The article emphasizes the importance of basic science as the foundation for generating new technology and materials, presenting interesting examples of laboratory research that have successfully addressed industry challenges.
Article
Engineering, Environmental
Ezequiel Rossi, Jhon Alejandro Avila Ramirez, Maria Ines Errea
JOURNAL OF ENVIRONMENTAL CHEMICAL ENGINEERING
(2020)
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)
