Article
Biochemistry & Molecular Biology
Aleksandra Drzewiecka-Antonik, Marta Struga, Agnieszka Glogowska, Ewa Augustynowicz-Kopec, Katarzyna Dobrzynska, Alicja Chrzanowska, Anna Wolska, Pawel Rejmak, Marcin T. Klepka, Malgorzata Wrzosek, Anna Bielenica
Summary: Copper complexes with 1,3-disubstituted thiourea derivatives were synthesized and their structures and properties were investigated. The complexes exhibited antimicrobial, antituberculosis, and antitumor activities.
INTERNATIONAL JOURNAL OF MOLECULAR SCIENCES
(2022)
Article
Biochemistry & Molecular Biology
Karolina Stryjska, Izabela Korona-Glowniak, Lilianna Checinska, Joachim Kusz, Justyn Ochocki
Summary: The synthesis of two novel silver(I) complexes of miconazole with new counter ions was conducted, showing significant antimicrobial activity against Gram-positive bacteria and yeasts, surpassing silver sulfadiazine and silver salts. The complex containing the nitrate counter ion exhibited the highest antimicrobial activity, while all silver(I) complexes of miconazole demonstrated better inhibition of yeast growth compared to silver sulfadiazine, silver salts, and miconazole. Additionally, the synthesized complexes showed good or moderate activity against Gram-negative bacteria when compared to the free ligand.
INTERNATIONAL JOURNAL OF MOLECULAR SCIENCES
(2021)
Article
Chemistry, Inorganic & Nuclear
Jian-Gong Huang, Jiamin Jin, Qin-Zhen Yuan, Xue-Xiao Yang, Deng-Ke Cao, Chungen Liu
Summary: Upon irradiation with 415 nm light, the complex [Ir(pbt)(2)(dppn)]Cl(1) exhibits high photo-oxidation activity (87% conversion yield for 1 and 15% for the free ligand dppn) and light-controlled luminescence. Two complexes, [Ir(pbt)(2)(dppn)]Cl (1) and [Ir(pt)(2)(dppn)]Cl (2), have been synthesized to investigate the influence of cyclometalating ligands on the photo-oxidation activity and explore their photo-oxidation-induced luminescence.
INORGANIC CHEMISTRY
(2023)
Article
Chemistry, Inorganic & Nuclear
Mrittika Roy, Wen Fu, Lilia M. Baldauf, James C. Fettinger, R. David Britt, Alan L. Balch
Summary: The oxidation of thianthrene and 10-phenylphenothiazine into cation radicals or coordination complexes has been studied using redox-active Lewis acids. Different redox reactions and crystalline formations were observed depending on the Lewis acid used and the solvent system employed.
INORGANIC CHEMISTRY
(2023)
Article
Chemistry, Physical
Cassidy E. Jackson, Thacien Ngendahimana, Chun-Yi Lin, Gareth R. Eaton, Sandra S. Eaton, Joseph M. Zadrozny
Summary: This study investigates the impact of different counterions on the spin relaxation of V(IV) complexes and finds that the methyl groups in the counterions play a dominant role in dictating the spin relaxation. The experimental results show that the methyl groups in the counterions are bound to the complex unit via hydrogen bonding. Additionally, the study reveals that the shot repetition time in spin echo measurements has a significant impact on the shape of the decay curve and the measured relaxation times. Furthermore, the spin-lattice relaxation times are independent of cations and remain the same in different systems.
JOURNAL OF PHYSICAL CHEMISTRY C
(2022)
Article
Materials Science, Textiles
Sahil Goyal, Marius Dotter, Elise Diestelhorst, Jan Lukas Storck, Andrea Ehrmann, Boris Mahltig
Summary: This paper reports on a sustainable extraction method for keratin from wool fiber materials and investigates its applications in polymer film preparation and preparation of nano-composite materials. The study shows that the combination of extracted keratin with different biopolymers can generate materials with antibacterial properties.
JOURNAL OF ENGINEERED FIBERS AND FABRICS
(2022)
Article
Materials Science, Multidisciplinary
F. Y. Rajhi, I. S. Yahia, H. Y. Zahran, Mona Kilany
Summary: This study investigated the effects of vanadium addition on nano-sized hydroxyapatite (HAp) synthesized by sol-gel/hydrothermal technique and microwave device. The results showed that vanadium-doped HAp nanostructures exhibit multifunctionality as microbial inhibitory agents and gamma radiation shielding materials.
MATERIALS TODAY COMMUNICATIONS
(2021)
Article
Biochemistry & Molecular Biology
Karyne Rangel, Fellipe O. Cabral, Guilherme C. Lechuga, Joao P. R. S. Carvalho, Maria H. S. Villas-Boas, Victor Midlej, Salvatore G. De-Simone
Summary: This study evaluated the bactericidal effect of high levels of ozone gas on reference and ESKAPE bacteria. The results showed that exposure to high concentrations of ozone inhibited the growth of all bacterial strains tested, significantly reducing colony counts. Cell viability of MRSA and XDR was considerably reduced, and SEM showed damage to bacteria after ozone treatment.
Article
Pharmacology & Pharmacy
Bency Thankappan, Jeyarajan Sivakumar, Sridhar Asokan, Mahendran Ramasamy, Mamatha M. Pillai, R. Selvakumar, Jayaraman Angayarkanni
Summary: The study demonstrated significant antimicrobial activity of a newly designed peptide against Pseudomonas, with no toxicity to human red blood cells and anti-survivability effects on cancer cells.
EUROPEAN JOURNAL OF PHARMACEUTICAL SCIENCES
(2021)
Article
Chemistry, Multidisciplinary
Tonya Vitova, Radmila Faizova, Jorge Amaro-Estrada, Laurent Maron, Tim Pruessmann, Thomas Neill, Aaron Beck, Bianca Schacherl, Farzaneh Fadaei Tirani, Marinella Mazzanti
Summary: The stabilization of uranyl(V) by Fe(II) in natural systems is still a subject of debate. We demonstrate that the covalency of the U(V)-oaxial bond decreases when bound to Fe(II), leading to redirection of electron density and increased covalency of the U(V)-equatorial bonds. This increased covalent interaction between U(V) and equatorial ligands due to iron binding contributes to the higher stability of uranyl(V).
Article
Spectroscopy
Jehan Y. Al-Humaidi, Foziah A. Al-Saif, Dalal N. Binjawhar, Hanan A. Bakhsh, Moamen S. Refat
Summary: Te(IV), Se(IV), V(III), Nb(V) and Ta(V) complexes of indole-3-acetic acid (IAAH) ligand were synthesized and characterized by various spectroscopic techniques, showing different geometries and coordination numbers. The presence of other coordinated molecules in the composition of IAA complexes were supported by thermogravimetry analysis, IR and micro analytical measurements.
SPECTROSCOPY AND SPECTRAL ANALYSIS
(2021)
Article
Chemistry, Multidisciplinary
Min Zhang, Min-Yu Wang, Yue-Ming Yu, Su-Su Meng, Cui-Wei Yan, Zhi-Yong Wu, Yan-Tuan Li
Summary: In this study, a cocrystal complex of p-coumaric acid (TPA) and the antifungal drug bifonazole (BFZ) called BFZ-TPA was successfully synthesized. The cocrystal improved the solubility and permeability of BFZ, enhancing its antifungal efficacy. This work not only filled the research gap in BFZ cocrystals, but also demonstrated a new application pathway for phenolic acid nutrition in antifungal cocrystal drugs.
Article
Engineering, Chemical
Manal A. El Sayed, Nahla T. Elazab, Malek Gassoumi, Magdy A. M. Ibrahim
Summary: This research presents a successful method for synthesizing nanocrystalline silver coatings using electrodeposition from an environmentally friendly electrolyte. The obtained silver coatings from this cyanide-free electrolyte exhibit bright and adherent nanocrystalline structures, and show excellent antibacterial properties against both gram-positive and gram-negative bacteria.
JOURNAL OF THE TAIWAN INSTITUTE OF CHEMICAL ENGINEERS
(2022)
Article
Biochemistry & Molecular Biology
Rabina Pradhan, Laxmi Tiwari, Vincent M. Groner, Caleb Leach, Kyle Lusk, Nathan S. Harrison, Kenneth A. Cornell, Kristopher Waynant
Summary: Redox-active azothioformamides (ATFs) containing NNCS 1,3-heterodiene motif were synthesized and tested. The ATF compounds showed little antimicrobial activity alone, but exhibited cytotoxicity against lung carcinoma cells and leukemia cells. When coordinated with copper(I) and silver(I), the ATFs showed antimicrobial activity and cytotoxicity against fungi and cancer cells.
JOURNAL OF INORGANIC BIOCHEMISTRY
(2023)
Review
Chemistry, Multidisciplinary
Xin Yang, Yan Liu, Ruike Guo, Jiafu Xiao
Summary: This article reviews the application of Ir coupled transition metal compound catalysts in driving electrochemical water splitting and discusses the significant role of Ir in promoting electrocatalytic performance, with an emphasis on correlating the structure-function relationships. The challenges and future directions for the fabrication of more advanced Ir coupled electrocatalysts are also presented.
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)