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
Atousa Goudarzi, Mitra Ghassemzadeh, Maryam Saeidifar, Kioumars Aghapoor, Farshid Mohsenzadeh, Bernhard Neumueller
Summary: The synthesis of a new Pd(II) complex and its characterization were reported. The complex exhibited potent anticancer activity against MCF-7 breast cancer cells, and showed good antimicrobial activity against both Gram-positive and Gram-negative bacteria.
NEW JOURNAL OF CHEMISTRY
(2022)
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
Biochemistry & Molecular Biology
Ju Zang, Bin Zhang, Yuanjiang Wang, Xinyi Wang, Shaohua Gou
Summary: This study reported a series of novel platinum(II) complexes derived from conjugation of several NSAIDs derivatives with two antitumor platinum(II) agents, and evaluated their antitumor effects on multiple cancer cell lines. The compounds showed stronger antitumor activity compared to the parent platinum agents, with some even overcoming cisplatin resistance. One of the compounds, IA-1, exhibited the best cytotoxicity and surpassed cisplatin in terms of antitumor activity. Further research revealed that IA-1 induced significant DNA damage, ROS generation, and apoptosis in A2780 cells. IA-1 also inhibited metastasis and invasion of A2780 cells by suppressing the COX-2/JAK2/STAT3 axis. Overall, this study demonstrated that NSAIDs can enhance the activity of platinum(II) agents by inhibiting inflammation in cancer cells.
BIOORGANIC CHEMISTRY
(2022)
Article
Biochemistry & Molecular Biology
Ivana Vasic, Snezana Rajkovic, Aleksandar Arsenijevic, Marija Milovanovic, Nebojsa Arsenijevic, Jelena Milovanovic, Marija D. Zivkovic
Summary: Nine dinuclear platinum(II) complexes were evaluated for their antitumour potential against mouse colon carcinoma CT26 cells, with Pt1, Pt2, and Pt7 showing significant in vitro cytotoxic activity. Pt5 and Pt6 exhibited the highest antiproliferative effect, while Pt1 and Pt7 demonstrated significant in vivo antitumour effects and reduced metastases without causing significant toxicity. These complexes show promise as potential chemotherapeutic agents.
JOURNAL OF INORGANIC BIOCHEMISTRY
(2021)
Article
Chemistry, Inorganic & Nuclear
Yu-Feng Wang, Ji-Xia Tang, Zai-Yong Mo, Juan Li, Fu-Pei Liang, Hua-Hong Zou
Summary: In this study, three new cobalt(II) complexes were designed and synthesized, showing strong anti-cancer activity and better inhibitory effects compared to the commonly used drug cisplatin. CoCl and Col could induce cell apoptosis by regulating the expression of autophagy-related proteins.
DALTON TRANSACTIONS
(2022)
Article
Biochemistry & Molecular Biology
Andjela A. Franich, Milena M. Jurisevic, Nevena M. Gajovic, Nebojsa N. Arsenijevic, Ivan P. Jovanovic, Bojan S. Stojanovic, Jakob Kljun, Snezana Rajkovic, Marija D. Zivkovic, Milica Dimitrijevic Stojanovic, Slobodanka Lj Mitrovic
Summary: In this study, four novel Pt(II) complexes were synthesized and investigated for their anticancer activity. The Pt3 complex showed potent cytotoxic activity against breast and colorectal cancer cells, with stronger selectivity and lower toxicity compared to other complexes tested.
JOURNAL OF INORGANIC BIOCHEMISTRY
(2022)
Article
Chemistry, Inorganic & Nuclear
Andrea Pettenuzzo, Keti Vezzu, Maria Luisa Di Paolo, Eirini Fotopoulou, Luciano Marchio, Lisa Dalla Via, Luca Ronconi
Summary: The study developed and characterized four organometallic gold(III)-dithiocarbamato glycoconjugates as potential anticancer agents, showing antiproliferative effects against ovarian carcinoma cells in low micromolar range. Mechanistic studies revealed their capability to act as topoisomerase inhibitors and disrupt mitochondrial membrane integrity, leading to cell death through the generation of ROS and promotion of oxidative stress.
DALTON TRANSACTIONS
(2021)
Article
Biochemistry & Molecular Biology
Cassia de Q. O. Cavalcante, Tales H. A. da Mota, Diego M. de Oliveira, Erica C. M. Nascimento, Joao B. L. Martins, Fabio Pittella-Silva, Claudia C. Gatto
Summary: In this study, two dithiocarbazate ligands derived from 1,1,1-trifluoro-2,4-pentanedione and their four Ni(II) complexes were synthesized and characterized. The crystal structure analysis revealed the cyclization reaction of the ligands and the formation of pyrazoline derivative. The coordination geometry of the complexes was found to be square planar, with dithiocarbazates coordinating through the ONS donor system. Hirshfeld surface analysis and mass spectrometry data provided insights into the molecular packing and fragmentation behavior of the compounds. Molecular docking simulations and cytotoxicity assays demonstrated the promising biological activity of the synthesized metal complexes.
FRONTIERS IN MOLECULAR BIOSCIENCES
(2023)
Article
Chemistry, Inorganic & Nuclear
Ya-Ting Chen, Shao-Nan Zhang, Zhen-Feng Wang, Qing-Min Wei, Shu-Hua Zhang
Summary: In this study, 13 transition metal complexes were synthesized and characterized. Two novel complexes exhibited strong cytotoxic activities against A549/DDP cancer cells, inducing apoptosis and autophagy via the mitochondria! dysfunction pathway. These complexes also showed pronounced and selective activity against A549/DDP xenografts in vivo.
DALTON TRANSACTIONS
(2022)
Article
Chemistry, Multidisciplinary
Yeye Ai, Zherui Zhang, Yuexuan Fei, Ruirong Ye, Angela Sin-Yee Law, Zong-Wan Mao, Junqiu Liu, Yongguang Li, Vivian Wing-Wah Yam
Summary: This study prepared mitochondria-targeted platinum(II) complexes, which efficiently entered cancer cells and selectively accumulated in mitochondria, leading to significant enhancement in phosphorescence. These complexes demonstrated distinct antitumor efficacy in inhibiting tumor growth and inducing tumor cell apoptosis in vivo.
SCIENCE CHINA-CHEMISTRY
(2023)
Article
Chemistry, Multidisciplinary
Yeye Ai, Zherui Zhang, Yuexuan Fei, Ruirong Ye, Angela Sin-Yee Law, Zong-Wan Mao, Junqiu Liu, Yongguang Li, Vivian Wing-Wah Yam
Summary: Mitochondria-targeted platinum(II) complexes were prepared by introducing a triazole group and methylation, which enhanced their fluorescence and cellular uptake capacity. In vivo experiments demonstrated that these complexes exhibited significant anti-tumor effects in inhibiting breast cancer tumor growth with negligible systemic cytotoxicity.
SCIENCE CHINA-CHEMISTRY
(2023)
Review
Chemistry, Inorganic & Nuclear
Magdalena Malecka, Anna Skoczynska, David M. Goodman, Christian G. Hartinger, Elzbieta Budzisz
Summary: This review highlights the progress in the development of ruthenium(II)/(III) complexes with flavone derivatives as potential therapeutic agents, focusing on their antimicrobial, antitumor activity, and enzyme inhibition. The design concept for the Ru complexes as multitargeted compounds consisting of a bioactive ligand and a ruthenium center is also emphasized.
COORDINATION CHEMISTRY REVIEWS
(2021)
Article
Biochemistry & Molecular Biology
Arezoo Saadati, Mahnaz Aryaeifar, Olivier Blacque, Rui Cabral, Luis R. R. Raposo, Alexandra R. R. Fernandes, Hadi Amiri Rudbari, Jose V. Cuevas-Vicario
Summary: This study investigated the effect of structure, halogen substitution, metal ions, and ligand flexibility on the antiproliferative activity of Cu(II) and Pt(II) complexes. The results showed that these complexes exhibited different structures depending on the ligand used and the presence of a base during preparation. All complexes demonstrated a reduction in cancer cell viability, but only complexes with iodo-substituted ligands showed low cytotoxicity in normal cells. Further analysis revealed that the I-2-H2L2-Cu complex induced cell death through apoptosis and autophagy mechanisms in the A2780 cell line.
BIOORGANIC CHEMISTRY
(2022)
Article
Chemistry, Multidisciplinary
Jebiti Haribabu, Nithya Balakrishnan, Srividya Swaminathan, Dorothy Priyanka Dorairaj, Mohammad Azam, Mohamed Kasim Mohamed Subarkhan, Yu-Lun Chang, Sodio C. N. Hsu, Pavel Starha, Ramasamy Karvembu
Summary: Three Pd(II) complexes containing tridentate chromone-based thiosemicarbazones were synthesized via in situ Michael addition reaction. The complexes exhibited potent anticancer activity against HeLa cancer cells, with IC50 values of 2.87 and 4.01 μM for complexes 2 and 3, respectively. Furthermore, the active Pd(II) complexes showed minimal damage to normal tissues in mice compared to cisplatin.
NEW JOURNAL OF CHEMISTRY
(2023)
Article
Chemistry, Multidisciplinary
Georgios Charitos, Dimitrios T. Trafalis, Panayiotis Dalezis, Constantinos Potamitis, Vasiliki Sarli, Panagiotis Zoumpoulakis, Charalambos Camoutsis
ARABIAN JOURNAL OF CHEMISTRY
(2019)
Article
Chemistry, Medicinal
T. Chatzisideri, S. Thysiadis, S. Katsamakas, P. Dalezis, I. Sigala, T. Lazarides, E. Nikolakaki, D. Trafalis, O. A. Gederaas, M. Lindgren, V. Sarli
EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
(2017)
Article
Chemistry, Medicinal
Savvas Thysiadis, Sotirios Katsamakas, Panagiotis Dalezis, Theodora Chatzisieri, Dimitrios Trafalis, Vasiliki Sarli
FUTURE MEDICINAL CHEMISTRY
(2017)
Article
Oncology
Panagiotis Dalezis, Eleni Geromichalou, Aikaterini Polonifi, Sofia Sagredou, Nikolaos Nikoleousakos, Michael Nikolaou, Vasiliki Sarli, Mihalis I. Panayiotidis, Dimitrios T. Trafalis
Article
Biotechnology & Applied Microbiology
Sofia Sagredou, Panagiotis Dalezis, Nikolaos Nikoleousakos, Michail Nikolaou, Maria Voura, Konstantinos Almpanakis, Mihalis Panayiotidis, Vasiliki Sarli, Dimitrios T. Trafalis
ONCOTARGETS AND THERAPY
(2020)
Article
Biochemistry & Molecular Biology
Despoina Anastasiadou, Elena Geromichalou, Eleni Tsavea, George Psomas, Antonios G. Hatzidimitriou, Stavros Kalogiannis, George Geromichalos, Dimitrios Trafalis, Panagiotis Dalezis, Paraskevas Aslanidis
JOURNAL OF INORGANIC BIOCHEMISTRY
(2020)
Article
Chemistry, Medicinal
Theodora Chatzisideri, Panagiotis Dalezis, George Leonidis, Spyridon Bousis, Dimitrios Trafalis, Francesca Bianchini, Vasiliki Sarli
Summary: This study developed c(RGDyK)-CUCU conjugates for selective delivery of CUCUs to integrin-overexpressing cancer cells, showing activity against these cancer cells. The conjugates were approximately three times more active than free CUCU-D in MCF-7 cells.
FUTURE MEDICINAL CHEMISTRY
(2021)
Article
Pharmacology & Pharmacy
Dimitrios T. Trafalis, Sofia Sagredou, Panayiotis Dalezis, Maria Voura, Stella Fountoulaki, Nikolaos Nikoleousakos, Konstantinos Almpanakis, Maria V. Deligiorgi, Vasiliki Sarli
Summary: The fusion of 1,2,4-triazole and 1,3,4-thiadiazole rings resulted in compounds with potential anticancer properties, particularly KA25 and KA39 which exhibited inhibition of Akt phosphorylation. These compounds showed promise as cancer therapeutic agents due to their low acute toxicity and effective anticancer activity in vitro and in vivo.
Article
Pharmacology & Pharmacy
Sofia Sagredou, Panagiotis Dalezis, Eirini Papadopoulou, Maria Voura, Maria V. Deligiorgi, Michail Nikolaou, Mihalis I. Panayiotidis, George Nasioulas, Vasiliki Sarli, Dimitrios T. Trafalis
Summary: MSI, TMB, and PD-L1 are established as immunotherapy predictive biomarkers, with the compound KA39 showing potent anticancer activity through PD-L1 upregulation and MSI increase, particularly affecting MMR-deficient cells.
Article
Biochemistry & Molecular Biology
Nikolaos Nikoleousakos, Panagiotis Dalezis, Aikaterini Polonifi, Elena G. Geromichalou, Sofia Sagredou, Constantinos E. Alifieris, Maria Deligiorgi, Vasiliki Sarli, Dimitrios T. Trafalis
Summary: Three newly synthesized B-lactam hybrid homo-aza-steroidal alkylators were evaluated for their PARP1/2 inhibition activity and DNA damaging effect against human ovarian carcinoma cells, with ASA-A and ASA-B showing the most significant anticancer activity.
Article
Chemistry, Multidisciplinary
George Leonidis, Panagiotis Dalezis, Dimitrios Trafalis, Dimitris Beis, Panagiota Giardoglou, Anastasia Koukiali, Ioanna Sigala, Eleni Nikolakaki, Vasiliki Sarli
Summary: The study successfully synthesized SRPIN803 and c(RGDyK)-SRPIN803 hybrid compounds, with one hybrid showing the highest activity and cytotoxicity against cancer cells, as well as antiangiogenic activity in zebrafish embryos. The hybrid compounds were found to be less potent than SRPIN803, but still showed interesting activities, demonstrating the potential of this approach for developing a new class of antiangiogenic compounds.
Article
Biochemistry & Molecular Biology
Elena G. Geromichalou, Dimitrios T. Trafalis, Panagiotis Dalezis, Georgios Malis, George Psomas, George D. Geromichalos
Summary: This study investigated the interactions between non-steroidal anti-inflammatory drugs and copper complexes, as well as their potential as antiviral agents against SARS-CoV-2. Cytotoxic activity on human cell lines was also evaluated.
JOURNAL OF INORGANIC BIOCHEMISTRY
(2022)
Article
Chemistry, Inorganic & Nuclear
Despoina Varna, Elena Geromichalou, Antonios G. Hatzidimitriou, Rigini Papi, George Psomas, Panagiotis Dalezis, Paraskevas Aslanidis, Theodora Choli-Papadopoulou, Dimitrios T. Trafalis, Panagiotis A. Angaridis
Summary: In recent years, there has been increasing interest in studying Ag(I) coordination compounds as effective antibacterial and anticancer agents. This study synthesized a series of Ag(I) complexes with phosphines and heterocyclic thioamide ligands, and evaluated their antibacterial and anticancer properties. The results showed that some of these complexes exhibited potent activity against bacteria and cancer cells, with certain selectivity towards normal cells.
DALTON TRANSACTIONS
(2022)
Article
Pharmacology & Pharmacy
Kosmas E. Verigos, Sofia Sagredou, Kyriakos Orfanakos, Panayiotis Dalezis, Dimitrios T. Trafalis
Article
Chemistry, Medicinal
Dimitrios Trafalis, Panagiotis Dalezis, Elena Geromichalou, Sofia Sagredou, Eleni Sflakidou, Maria Voura, Margarita Grammatikopoulou, Catherine Gabriel, Vasiliki Sarli
FUTURE MEDICINAL CHEMISTRY
(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)