Article
Chemistry, Inorganic & Nuclear
Jin Wang, Yu-Ting Wang, Jiang-Nan Chang, Ming-Xue Li
Summary: The article describes the synthesis and characterization of two nickel complexes of 2-acetylpyrazine thiosemicarbazone, and studies their antibacterial activities. It was found that one of the complexes showed effective antimicrobial activity against tested bacteria, and that complex 2 exhibited inhibitory activity against human hepatocellular carcinoma HepG2 cells. Additionally, toxicity study showed that complex 2 had the highest tumor cell selectivity.
INORGANIC CHEMISTRY COMMUNICATIONS
(2021)
Article
Chemistry, Inorganic & Nuclear
Jin Wang, Zhi-Meng Zhang, Ming-Xue Li
Summary: The synthesis of four metal complexes and their antimicrobial and cytotoxic activities were investigated in this study. The results showed that the antibacterial activity of cadmium (II) and antimony (III) complexes was enhanced compared to their ligands, with Cd2 and Sb2 demonstrating effective antibacterial activity and Cd2 showing the most effective antiproliferative activity against HepG2 cells.
INORGANICA CHIMICA ACTA
(2022)
Article
Multidisciplinary Sciences
Eda Yuhana Ariffin, Emma Izzati Zakariah, Farah Ruslin, Muhammad Kassim, Bohari M. Yamin, Lee Yook Heng, Siti Aishah Hasbullah
Summary: This study found that the HexaFc complex can be used as an electroactive indicator for porcine DNA biosensors, exhibiting strong recognition ability and stability for the detection and measurement of porcine DNA.
SCIENTIFIC REPORTS
(2021)
Article
Chemistry, Inorganic & Nuclear
E. S. Cakmakci, E. Subasi, E. Ozturk, A. Sahiner, B. Sen Yuksel
Summary: Metal(II) complexes including Co(II), Ni(II), Pd(II) and Zn(II) were synthesized and characterized. These complexes were obtained by reacting metal(II) chlorides with the ligand. The structures and properties of these complexes were determined by various characterization techniques including elemental analysis, FT-IR, 1H NMR, and single crystal X-ray diffraction.
INORGANICA CHIMICA ACTA
(2023)
Article
Biochemistry & Molecular Biology
Avinash Kotian, Vinayak Kamat, Krishna Naik, Dhoolesh G. Kokare, Karthik Kumara, Krishnappagowda Lokanath Neratur, Vijay Kumbar, Kishore Bhat, Vidyanand K. Revankar
Summary: This paper investigates the p-halo N4-phenyl substituted thiosemicarbazones derived from 8-hydroxyquinoline, their crystal structures, spectral characterization, and in vitro cytotoxic studies of Co(III), Ni(II) and Cu(II) complexes. The complexes show enhanced antiproliferative activity against MCF-7 breast cancer cell lines, especially the Co(III) complexes displaying a roughly two fold increase in activity compared to the standard drug, Paclitaxel. Additionally, fluorescence microscopy images suggest an apoptotic mode of cell death.
BIOORGANIC CHEMISTRY
(2021)
Article
Polymer Science
Roman Nickisch, Peter Conen, Michael A. R. Meier
Summary: This study presents an easy access to thermoplastic polythiosemicarbazones (polyTSCs) through condensation reaction, resulting in a variety of polymers and copolymers that were thoroughly characterized. The polymerization proceeds at room temperature with broad moiety tolerance, and the synthesized polymers exhibit good thermal stability.
Article
Chemistry, Inorganic & Nuclear
Ali A. A. Al-Riyahee, Peter N. Horton, Simon J. Coles, Angelo J. Amoroso, Simon J. A. Pope
Summary: The synthesis of two thiosemicarbazone derivatised ligands (L1 and L2) was achieved by reacting 1-(2-pyridinyl)ethanone hydrazone with benzoyl or pivaloyl isothiocyanate. Mononuclear complexes of nickel (II), copper (II), and zinc (II) with these ligands were synthesized and characterized using various techniques. The solid-state molecular structures of eight examples were successfully determined by single crystal X-ray diffraction.
Article
Chemistry, Multidisciplinary
Lauren M. McRae, Rebecca C. Radomsky, Jacob T. Pawlik, Daniel L. Dru, Jack D. Sundberg, Matthew G. Lanetti, Carrie L. Donley, Kelly L. White, Scott C. Warren
Summary: Electrides are exotic materials where electrons occupy defined lattice sites instead of within atoms. The effect of cation electronegativity on the properties of electrides remains unclear. In this study, we examine trivalent metal carbides with varying electronegativity and successfully synthesize Sc2C, which is identified as a two-dimensional electride. By computational exploration, we find that higher electronegativity of the cation results in increased hybridization between metal and electride orbitals, leading to the formation of a band gap in these materials. Sc2C is the first 2D electride semiconductor, and a design rule proposing cation electronegativity as a driving force for changes in its band structure is proposed.
JOURNAL OF THE AMERICAN CHEMICAL SOCIETY
(2022)
Article
Chemistry, Inorganic & Nuclear
Azadeh Mirzaahmadi, Seyed Abolfazl Hosseini-Yazdi, Majid Mahdavi, Michal Dusek, Valcav. Eigner, Morgane Poupon
Summary: New water-soluble Zn(II) and Ni(II) complexes, synthesized and characterized in this study, exhibit good solubility and stability in aqueous media. These complexes show potential anticancer activity in cell experiments.
Article
Biochemistry & Molecular Biology
Monica Martinez-Estevez, Soledad Garcia-Fontan, Saray Argibay-Otero, Inmaculada Prieto, Ezequiel M. Vazquez-Lopez
Summary: In this study, the reaction between [Ru2Cl2(mu-Cl)(2)(eta(6)-p-cymene)(2)] and two thiosemicarbazones was investigated. The resulting cationic complexes were isolated and characterized. The study revealed the presence of two isomers in the triflate salts and only one isomer in the chloride. X-ray crystallography confirmed this finding. The coordination of the thiosemicarbazone ligand to the ruthenium center was also demonstrated.
Article
Chemistry, Inorganic & Nuclear
Kentaro Aoki, Kazuya Otsubo, Yukihiro Yoshida, Yojiro Kimura, Kunihisa Sugimoto, Hiroshi Kitagawa
Summary: A dimerized Ni-II trinuclear complex bridged by a Cl anion to form a string structure has been reported. This complex aligns in one dimension in the solid state, leading to intra- and interdimer antiferromagnetic interactions.
INORGANIC CHEMISTRY
(2021)
Article
Chemistry, Inorganic & Nuclear
Chinmoy Biswas, Arnab Chatterjee, Vinu Vijayan, Chandra Shekhar Purohit, Manikantan Syamala Kiran, Rajarshi Ghosh
Summary: This article reports the synthesis and structural characterization of a dinuclear silver(I) complex 1, which exhibits selective anticancer activity against liver cancer cells. The anticancer activity of 1 is achieved through induction of mitochondrial death via Reactive Oxygen Species (ROS).
INORGANIC CHEMISTRY COMMUNICATIONS
(2022)
Article
Chemistry, Inorganic & Nuclear
Takayuki Itabashi, Kazuya Arashiba, Shogo Kuriyama, Yoshiaki Nishibayashi
Summary: The molybdenum-nitride complex is functionalized by reacting with various carbon-centered electrophiles, resulting in the formation of new imide and acylimide complexes through carbon-nitrogen bond formation. The PNP ligand acts as a non-innocent ligand in reactions with phenylisocyanate and diphenylketene, leading to the formation of ureate and acylimide complexes. The nitrogen molecule is converted into an organic amide mediated by the molybdenum-nitride complex during the hydrolysis of the molybdenum-acylimide complex.
DALTON TRANSACTIONS
(2022)
Article
Chemistry, Physical
Forough Jahanbazi, Yuanbing Mao
Summary: Researchers have discovered a new phenomenon of excitation-wavelength-dependent anti-thermal quenching (anti-TQ) luminescence in the Eu3+-doped Sc2Mo3O12 phosphor. This luminescence shows intensified energy transfer from the host to the dopant and increased intensity at elevated temperatures, particularly when excited at 277 nm. The mechanism behind this anti-TQ luminescence is attributed to the negative thermal expansion property of the Sc2Mo3O12 host. The findings provide inspiration for the development of thermally enhanced phosphors with intensified energy transfer for various applications.
CHEMISTRY OF MATERIALS
(2022)
Article
Chemistry, Inorganic & Nuclear
Vigneswari Sankara Narayanan, Archana Rajendran, Srikrishna Mudradi, Soven Dhawa, Sreeja Rajendran, Kondapa Naidu Bobba, Jeya Rajendran, Prasanna Ramani
Summary: In this study, bidentate Schiff-base ligands with nitrogen and sulphur donor sites were successfully synthesized and used to synthesize Co (II), Cu (II), and Zn (II) complexes. The synthesized complexes exhibited high spin and distorted octahedral geometry, strong binding affinity to CT-DNA, good antioxidant properties, and anticancer activity.
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)