Article
Chemistry, Multidisciplinary
Qiyuan Zhou, Shu Chen, Zoufeng Xu, Gongyuan Liu, Shuyuan Zhang, Zhigang Wang, Man-Kit Tse, Shek-Man Yiu, Guangyu Zhu
Summary: This study reports the synthesis of Pt-IV complexes bearing axial pyridines through ligand exchange reactions. It was discovered that these axial pyridines can be quickly released after reduction, indicating their potential as axial leaving groups. Two multitargeted Pt-IV prodrugs containing bioactive pyridinyl ligands, a PARP inhibitor and an EGFR tyrosine kinase inhibitor, were successfully obtained using this method. These conjugates show great potential for overcoming drug resistance, with the latter inhibiting the growth of Pt-resistant tumor in vivo. This research expands the synthetic methods for Pt-IV prodrugs and increases the range of bioactive axial ligands that can be conjugated to a Pt-IV center.
ANGEWANDTE CHEMIE-INTERNATIONAL EDITION
(2023)
Article
Chemistry, Multidisciplinary
Denise Lovison, Dario Alessi, Lorenzo Allegri, Federica Baldan, Maurizio Ballico, Giuseppe Damante, Marilisa Galasso, Daniele Guardavaccaro, Silvia Ruggieri, Andrea Melchior, Daniele Veclani, Chiara Nardon, Walter Baratta
Summary: The paper describes a chiral ruthenium complex with high cytotoxic activity against various cell lines, particularly showing strong inhibition against the anaplastic thyroid cancer cell line 8505 C.
CHEMISTRY-A EUROPEAN JOURNAL
(2022)
Article
Chemistry, Medicinal
Stefano Zoroddu, Paola Corona, Luca Sanna, Federica Borghi, Valentina Bordoni, Battistina Asproni, Gerard A. Pinna, Luigi Bagella, Gabriele Murineddu
Summary: A library of novel 1,3,4-oxadiazole bioisosteres was synthesized and evaluated for their cytotoxic activity. Several of the new compounds showed potent anticancer activity, surpassing the previously synthesized oxadiazole compound. The nature of the selenadiazole and thiadiazole rings may play a crucial role in the antitumor activity. These compounds exhibited strong cytotoxic effects in tumor cells compared to human primary cells.
EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
(2022)
Article
Pharmacology & Pharmacy
Leide Laura Figueiredo Maciel, Marina Barreto Silva, Rafaela Oliveira Moreira, Ana Paula Cardoso, Christiane Fernandes, Adolfo Horn Jr, Joao Carlos de Aquino Almeida, Milton Masahiko Kanashiro
Summary: This study investigated the antineoplastic activity of two platinum complexes containing alpha- and beta-naphthyl groups. The results showed that one of the platinum complexes exhibited higher cytotoxicity against all cancer cell lines tested and lower cytotoxicity against normal peripheral blood mononuclear cells. Further investigations revealed that this complex induced cell death by apoptosis and was associated with mitochondrial membrane depolarization, elevated levels of reactive oxygen species (ROS), and caspase activation.
Article
Chemistry, Multidisciplinary
Valerio Giuso, Jeannine Yang, Jeremy Forte, Heloise Dossmann, Chantal Daniel, Christophe Gourlaouen, Matteo Mauro, Benoit Bertrand
Summary: A series of binuclear gold complexes have been synthesized and characterized. These complexes exhibit long-lived yellow-green phosphorescence in the solid state with high photoluminescence quantum yields. Two of the complexes show promising antiproliferative activity against lung adenocarcinoma cells.
Article
Chemistry, Multidisciplinary
Esteban Rodriguez-Arce, Eric Gavrilov, Ximena Alvite, Nazia Nayeem, Ignacio E. Leon, Michelle C. Neary, Lucia Otero, Dinorah Gambino, Claudio Olea Azar, Maria Contel
Summary: This work reports the synthesis and stability study of four gold(I) [AuClL] compounds containing chloro and biologically active protonated thiosemicarbazones based on 5-nitrofuryl (L=HSTC). The cytotoxicity of these compounds was evaluated against cancer cell lines, and one compound showed significant antimigratory and anti-angiogenic properties on a renal cancer cell line (Caki-1), along with preferential accumulation in the cell nuclei. Its mode of action seems to involve interaction with DNA and induction of apoptosis.
Article
Pharmacology & Pharmacy
Anife Ahmedova, Rositsa Mihaylova, Silviya Stoykova, Veronika Mihaylova, Nikola Burdzhiev, Viktoria Elincheva, Georgi Momekov, Denitsa Momekova
Summary: Pt(IV) complexes formed by linking pyrene butyric acid with cisplatin exhibit high anticancer potency against leukemia cells and multidrug-resistant derivatives, while showing low toxicity to healthy cells. The larger bis-pyrene complex is found to potentially be trapped in the cytoskeleton, limiting its cytotoxicity to adherent cells.
Article
Chemistry, Multidisciplinary
Alexander Kastner, Hemma Schueffl, Patrick A. Yassemipour, Bernhard K. Keppler, Petra Heffeter, Christian R. Kowol
Summary: Platinum(IV) prodrugs are promising alternatives to platinum(II) anticancer therapeutics. This study investigated the reactivity and synthetic usability of a platinum(IV) complex with hydrolyzable equatorial ligands, and successfully synthesized stable platinum(IV) complexes suitable for long-circulating tumor-targeting strategies. Additionally, platinum(IV) complexes with equatorial maleimides were synthesized, showing prolonged plasma half-life and improved anticancer activity compared to oxaliplatin.
ANGEWANDTE CHEMIE-INTERNATIONAL EDITION
(2023)
Article
Biochemistry & Molecular Biology
Rosario Serrano, Isabel Martinez-Argudo, Miguel Fernandez-Sanchez, Pedro J. Pacheco-Linan, Ivan Bravo, Boiko Cohen, Raul Calero, Maria Jose Ruiz
Summary: Titanium-based therapies have shown promise as a treatment for cancer patients, especially those with cisplatin resistant tumors. A newly synthesized titanium complex demonstrated improved stability in water and strong interaction with human serum albumin, showing potential anti-tumor effects.
JOURNAL OF INORGANIC BIOCHEMISTRY
(2021)
Article
Chemistry, Medicinal
Monika Absolonova, Lucie Melounkova, Jaromir Vinklarek, Jan Honzicek, Libor Dostal, Ondrej Mrozek
Summary: Cytotoxic complexes containing molybdenum are studied as potential alternatives to commercial drugs, with different ligands having a significant impact on cytotoxicity. Functionalization of the Cp ring in Mo complexes can improve cytotoxicity against cancer cells, suggesting a potential strategy for designing highly efficient cytotoxic drugs in the future.
Article
Chemistry, Multidisciplinary
Masafumi Okuno, Keita Yamana, Shogo Kawamura, Kotaro Nishimura, Shodai Hino, Riku Kawasaki, Atsushi Ikeda
Summary: Tetrakis(4-aminophenyl)porphyrin and tetrakis(4-acetamidophenyl)porphyrin were dissolved in water using a polysaccharide (λ-carrageenan) as a water-solubilizing agent. The photodynamic activity of the CGN-2 complex was lower than that of the CGN-1 complex, but the selectivity index (SI) of the CGN-2 complex was higher. In vivo experiments showed that the CGN-2 complex inhibited tumor growth with higher blood retention compared to the CGN-1 complex and Photofrin.
CHEMISTRY-A EUROPEAN JOURNAL
(2023)
Article
Chemistry, Inorganic & Nuclear
Raphael T. Ryan, Dmytro Havrylyuk, Kimberly C. Stevens, L. Henry Moore, Sean Parkin, Jessica S. Blackburn, David K. Heidary, John P. Selegue, Edith C. Glazer
Summary: The beta-diketone scaffold, a commonly used synthetic intermediate, showed promising structure-dependent cytotoxicity in constructing Ru(II) complexes, suggesting the potential for future drug development.
EUROPEAN JOURNAL OF INORGANIC CHEMISTRY
(2021)
Article
Chemistry, Inorganic & Nuclear
Aisling L. Ryan, Joshua Northcote-Smith, Aoife McKeon, Andrew Roe, Paul O'Dowd, Brendan Twamley, Triona Ni Chonghaile, Kogularamanan Suntharalingam, Darren M. Griffith
Summary: The first example of a Pt complex of GANT61, a hedgehog (Hh) pathway inhibitor, is reported. The complex showed potent inhibition activity against breast CSC cells and triple negative breast cancer cells, as well as significant inhibition effect on the CSC-enriched mammosphere model.
DALTON TRANSACTIONS
(2022)
Article
Chemistry, Multidisciplinary
Marzieh Dadkhah Aseman, Parisa Negaresh, Zahra Shojaeifard, Bahram Hemmateenejad, S. Masoud Nabavizadeh
Summary: The biomolecular interactions between two previously reported cycloplatinated complexes and bovine serum albumin (BSA) were investigated. The results showed a strong binding interaction between the complexes and the protein with a static quenching mechanism. The binding was found to be exothermic, involving mainly noncovalent hydrophobic forces and ionic interactions. The complexes induced structural changes in the protein and exhibited cytotoxicity against various cancer cell lines.
NEW JOURNAL OF CHEMISTRY
(2023)
Article
Chemistry, Inorganic & Nuclear
Akifumi Sumida, Hiroaki Imoto, Kensuke Naka
Summary: In this study, an efficient synthetic method for AB2-type arsenic ligands was developed and applied in the Suzuki-Miyaura cross-coupling reaction. The arsenic analogues of Buchwald ligands showed comparable activity to the well-known Buchwald ligand, SPhos, and exhibited higher activity and stability under open-air conditions.
INORGANIC CHEMISTRY
(2022)
Article
Chemistry, Inorganic & Nuclear
Zhuxin Zhang, Chunli Li, Xiaojun Sun, Chuanzhu Gao, Congtao Yu, Qinghua Liu, Linkui Bai, Yunxu Qian, Bo Yang, Peng Dong, Yingjie Zhang
INORGANICA CHIMICA ACTA
(2017)
Review
Chemistry, Applied
Linxiang Cai, Congtao Yu, Linkui Ba, Qinghua Liu, Yunxu Qian, Bo Yang, Chuanzhu Gao
APPLIED ORGANOMETALLIC CHEMISTRY
(2018)
Article
Integrative & Complementary Medicine
Congtao Yu, Lifen Dai, Zhaoxia Ma, Hongbin Zhao, Yong Yuan, Yunfeng Zhang, Pengfei Bao, Yanfang Su, Daiping Ma, Change Liu, Xingfei Wu, Jinxue Liu, Yanjiao Li, Bing Wang, Min Hu
BMC COMPLEMENTARY AND ALTERNATIVE MEDICINE
(2019)
Article
Chemistry, Medicinal
Congtao Yu, Chuanzhu Gao, Linkui Bai, Qinghua Liu, Zhuxin Zhang, Yingjie Zhang, Bo Yang, Chunli Li, Peng Dong, Xiaojun Sun, Yunxu Qian
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
(2017)
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)