Article
Chemistry, Inorganic & Nuclear
Laia Rafols, Dana Josa, David Aguila, Leoni A. Barrios, Olivier Roubeau, Jordi Cirera, Vanessa Soto-Cerrato, Ricardo Perez-Tomas, Manuel Martinez, Arnald Grabulosa, Patrick Gamez
Summary: The newly synthesized compounds showed poor cytotoxic activities in cell cultures, but displayed improved activities in aged DMSO solutions. It was found that the compounds underwent transformation reactions in DMSO, ultimately forming cyclometalated species.
INORGANIC CHEMISTRY
(2021)
Article
Chemistry, Multidisciplinary
Xiang Ma, Saurav Bhattacharya, Talha Nisar, Anja B. Mueller, Veit Wagner, Nikolai Kuhnert, Ulrich Kortz
Summary: We present the synthesis and structural characterization of the first Pd-IV-containing polyoxopalladate(ii) complex. This discrete mixed-valent polyoxopalladate(iv/ii) features a central Pd-IV ion surrounded by a six-membered Pd-II-oxo ring capped by six dimethylarsinate groups. The structure was analyzed using various techniques in the solid state, solution, and gas phase.
CHEMICAL COMMUNICATIONS
(2023)
Article
Spectroscopy
Jebiti Haribabu, Othman I. Alajrawy, Kumaramangalam Jeyalakshmi, Chandrasekar Balachandran, Dhanabalan Anantha Krishnan, Nattamai Bhuvanesh, Shin Aoki, Karuppannan Natarajan, Ramasamy Karvembu
Summary: Copper(II) complexes containing N-substituted isatin thiosemicarbazone(s) were synthesized and characterized using analytical and spectroscopic techniques. The bimetallic nature of one of the complexes was confirmed by X-ray crystallography. Molecular docking studies revealed interactions with tyrosinase kinase receptors. The cytotoxic activity of the complexes against leukemia and cervical cancer cell lines was found to be promising with better efficacy than cisplatin.
SPECTROCHIMICA ACTA PART A-MOLECULAR AND BIOMOLECULAR SPECTROSCOPY
(2021)
Article
Biochemistry & Molecular Biology
Aleksandra M. Bondzic, Jelena J. Zakula, Lela B. Koricanac, Otilija D. Keta, Goran Janjic, Ivana S. Dordevic, Snezana U. Rajkovic
Summary: The stability, lipophilicity, in vitro cytotoxicity, and influence on acetylcholinesterase of five dinuclear platinum(II) complexes were evaluated. Some of the complexes showed promising anticancer activity and selectivity, with minimal effects on normal cells. Docking studies provided insights into the binding modes with acetylcholinesterase.
CHEMICO-BIOLOGICAL INTERACTIONS
(2022)
Article
Chemistry, Inorganic & Nuclear
Rafael Lopez-Sanchez, J. Roberto Pioquinto-Mendoza, Lucero Gonzalez-Sebastian, Ruben A. Toscano, Marcos Flores-Alamo, Maria Teresa Ramirez-Apan, Adrian L. Orjuela, Jorge Ali-Torres, David Morales-Morales
Summary: This study describes the synthesis of a series of Pd(II) (Pd-1-3) complexes with salen or salphen ligands. The complexes were characterized using standard spectroscopic techniques. The crystal structure analysis of complex Pd-3 revealed a distorted square planar environment for the palladium center. In addition, the in vitro cytotoxic activity of the palladium complexes Pd-1-3 against five human cancer cell lines was evaluated, and Pd-2 showed the best inhibitory activity against human prostatic adenocarcinoma (PC-3) with an IC50 of 3.8 +/- 0.4 µM. Docking calculations were also performed to support these results.
INORGANICA CHIMICA ACTA
(2023)
Article
Chemistry, Inorganic & Nuclear
Nikolai F. Romashev, Pavel A. Abramov, Ivan Bakaev, Iakov S. Fomenko, Denis G. Samsonenko, Alexander S. Novikov, Kelvin K. H. Tong, Dohyun Ahn, Pavel Dorovatovskii, Yan Zubavichus, Aleksey A. Ryadun, Olga A. Patutina, Maxim N. Sokolov, Maria Babak, Artem L. Gushchin
Summary: A series of Pt and Pd complexes with dpp-Bian and different ligands were synthesized and characterized. The Pt(dpp-Bian) complexes showed high anticancer activity at low concentrations and exhibited selectivity towards cancer cells. These complexes induced the generation of reactive oxygen species in cancer cells and were able to intercalate into DNA.
INORGANIC CHEMISTRY
(2022)
Review
Biochemistry & Molecular Biology
Robert Czarnomysy, Dominika Radomska, Olga Klaudia Szewczyk, Piotr Roszczenko, Krzysztof Bielawski
Summary: New, safer, and more effective agents are needed for cancer treatment. Cytostatics with transition metals are attracting renewed interest from scientists, who are exploring combination therapy and molecular modifications to enhance effectiveness and selectivity. Recent drug findings with palladium and platinum atoms are being organized.
INTERNATIONAL JOURNAL OF MOLECULAR SCIENCES
(2021)
Article
Chemistry, Inorganic & Nuclear
Rossella Caligiuri, Giuseppe Di Maio, Nicolas Godbert, Francesca Scarpelli, Angela Candreva, Isabella Rimoldi, Giorgio Facchetti, Maria Giovanna Lupo, Emilia Sicilia, Gloria Mazzone, Fortuna Ponte, Isabella Romeo, Massimo La Deda, Alessandra Crispini, Renata De Rose, Iolinda Aiello
Summary: A series of novel cationic curcumin-based Pt(II) complexes with neutral ligands and triflate anions have been synthesized and characterized. The antioxidant activity of these complexes was measured using DPPH and computational strategies were used to determine their mechanism of action. In addition, the growth inhibitory activity of the complexes against bacteria was tested using the disk diffusion technique.
DALTON TRANSACTIONS
(2022)
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
Chemistry, Inorganic & Nuclear
Obinna C. Okpareke, William Henderson, Senem Akkoc, Burak Coban
Summary: A series of alkyl-bridged bisthiourea ligands and their group 10 metal complexes have been synthesized, showing different coordination states and isomeric structures. The ESI mass spectral analysis and NMR characterization revealed complex multiplets and the formation of various isomers in the products. X-ray crystallographic studies confirmed the coordination of NPh group and the formation of M-S-C-N rings involving chelating thiourea monoanions in some derivatives.
INORGANICA CHIMICA ACTA
(2022)
Review
Chemistry, Inorganic & Nuclear
Gabrieli L. Parrilha, Raquel G. dos Santos, Heloisa Beraldo
Summary: Metallic radionuclides have diverse applications as diagnostic and therapeutic agents. This study reports the behavior of different radiometal complexes with mono(thiosemicarbazones) and bis(thiosemicarbazones) as potential radiopharmaceuticals. The application of bis(thiosemicarbazonato)copper(II) complexes as diagnostic radiopharmaceuticals has been successful, while other radioisotopes such as Ga-67/68, (111/114)mIn, and Tc-99m have also been used to obtain mono- and bis(thiosemicarbazone) complexes for potential diagnosis and therapy.
COORDINATION CHEMISTRY REVIEWS
(2022)
Review
Chemistry, Inorganic & Nuclear
Federica De Castro, Erik De Luca, Michele Benedetti, Francesco Paolo Fanizzi
Summary: The emergence of new epidemic viruses has raised new questions about viral infection treatment. There are high expectations for answers and fast solutions from scientists. The potential of platinum compounds in viral diseases is an unexplored field that warrants further research.
COORDINATION CHEMISTRY REVIEWS
(2022)
Article
Biochemistry & Molecular Biology
Zahra Shabaninejad, Maryam Nikkhah, S. Masoud Nabavizadeh
Summary: The DNA binding capacity and cytotoxic effects of two cycloplatinated complexes (C1 and C2) were evaluated. Both complexes exhibited high DNA binding affinity and were able to quench the fluorescence of ethidium bromide. They also induced DNA viscosity increase, confirming their intercalative interactions with DNA. C2 showed the highest cytotoxicity, particularly on a cisplatin resistant-cell line, and induced apoptosis comparable or higher than cisplatin in all cell lines.
JOURNAL OF INORGANIC BIOCHEMISTRY
(2023)
Article
Crystallography
Luis Alonso, Rodrigo Buron, Elena Lopez-Torres, Maria Antonia Mendiola
Summary: The new ligand HMeATSM derived from 2-3-butanedione with 4-methyl-3-thiosemicarbazide and 2,4-dimethyl-3-thiosemicarbazide has been synthesized and its reactivity with nickel(II) and zinc(II) nitrates has been explored. The structures of the resulting complexes were thoroughly characterized and it was found that nickel(II) prefers a square-planar environment while zinc(II) prefers a distorted square-base pyramid or trigonal bipyramid arrangement.
Article
Chemistry, Multidisciplinary
M. S. Denisov, O. N. Gagarskikh
Summary: This study investigated the structures and cytotoxic activities of four new palladium complexes obtained from the reactions of palladium(II) chloride with catecholamine salts and pyridine-2-carbaldehyde. The structure of the complexes was confirmed using NMR spectroscopy and X-ray diffraction analysis. The cytotoxic activity of the complexes on prostate cancer cells (PC3) and human epithelial kidney cells (HEK-293) was evaluated.
RUSSIAN JOURNAL OF GENERAL CHEMISTRY
(2021)
Article
Chemistry, Organic
Yusuf Sicak, Emine E. Oruc-Emre, Mehmet Ozturk, Aysegul Karakucuk-Iyidogan, Said Nadeem
JOURNAL OF HETEROCYCLIC CHEMISTRY
(2020)
Article
Chemistry, Physical
Bedriye Seda Kursun A. Aktar, Yusuf Sicak, Tugba Taskin Tok, Emine Elcin Oruc-Emre, Ayse Sahin Yaglioglu, Aysegul Karakucuk C. Iyidogan, Mehmet Ozturk, Ibrahim Demirtas
JOURNAL OF MOLECULAR STRUCTURE
(2020)
Article
Biochemistry & Molecular Biology
E. Bozkurt, Y. Sicak, E. E. Oruc-Emre, A. Karakucuk Iyidogan, M. Ozturk
RUSSIAN JOURNAL OF BIOORGANIC CHEMISTRY
(2020)
Article
Chemistry, Multidisciplinary
Demet Tasdemir Kahraman, Aysegul Karakucuk-Iyidogan, Yasemin Saygideger, Emine Elcin Oruc-Emre, Tugba Taskin-Tok, Eyup Basaran, Sedat Ilhan, Burcu Saygideger Demir, Aykut Uren, Hasan Bayram
Summary: This study synthesized multiple chiral compounds and identified potential target compounds for treating lung cancer, with compound 6a showing promise as a HIF-1 beta inhibitor candidate. The cytotoxic activity and apoptotic effects of these compounds, as well as their HIF-1 beta inhibitory properties, were evaluated, emphasizing the importance of selective HIF inhibitors in lung cancer treatment.
NEW JOURNAL OF CHEMISTRY
(2022)
Article
Chemistry, Physical
Eyup Basaran, Zeynep Demircioglu, Gonca Ozdemir Tari, Umit Ceylan, Aysegul Karakucuk-Iyidogan, Emine Elcin Oruc-Emre, Muhittin Aygun
Summary: In this study, an enantiomerically pure triazole derivative was successfully synthesized, characterized by spectroscopic techniques and X-ray diffraction, and analyzed for various computational properties and chemical activity descriptors. The stability of the molecule, arising from hyperconjugative interactions and charge delocalization, was examined through natural bond orbital analysis, and nonlinear optical properties were explored.
JOURNAL OF MOLECULAR STRUCTURE
(2022)
Article
Chemistry, Physical
Ahmet Oral Sarioglu, Demet Tasdemir Kahraman, Aysegul Kose, Mehmet Sonmez
Summary: Three new homoleptic six-coordinate Sm(III) complexes with different substituent groups have been synthesized and characterized for their structure. The photoluminescence properties and cytotoxic activities of these complexes have been investigated, and one of the complexes shows potential as a chemotherapeutic drug.
JOURNAL OF MOLECULAR STRUCTURE
(2022)
Article
Chemistry, Medicinal
Bedriye Seda Kursun Aktar, Yusuf Sicak, Gizem Tatar, Emine Elcin Oruc-Emre
Summary: In this study, a series of new sulfonyl hydrazones were synthesized and evaluated for their antioxidant and enzyme inhibitory activities. Molecular docking analysis was performed to understand the inhibitory mechanism at the molecular level. Compound 8 showed the most active AChE activity, while compounds 3, 4, 5, 6, 7, and 8 exhibited better BChE and tyrosinase inhibitory activities compared to the standard drug galantamine.
PHARMACEUTICAL CHEMISTRY JOURNAL
(2022)
Article
Pharmacology & Pharmacy
Halil Ibrahim Toy, Abdullah Burak Yildiz, Demet Tasdemir Kahraman, Sedat Ilhan, Oner Dikensoy, Hasan Bayram
Summary: Capsaicin can suppress ciliary activity and cytokine release from bronchial epithelial cells, while inducing permeability and cellular toxicity. These effects can be partially prevented by formoterol and roflumilast.
FRONTIERS IN PHARMACOLOGY
(2022)
Article
Biochemistry & Molecular Biology
Yusuf Sicak, Huseyin Kekecmuhammed, Aysegul Karakucuk-Iyidogan, Tugba Taskin-Tok, Emine Elcin Oruc-Emre, Mehmet Ozturk
Summary: In this study, a series of chalcones were designed and synthesized, and their chemical structures were elucidated. The chalcones exhibited promising activities against various enzymes and antioxidant activity. The structure-activity relationship analysis and molecular modeling studies provided important information for the drug design and properties.
JOURNAL OF MOLECULAR RECOGNITION
(2023)
Article
Chemistry, Multidisciplinary
Yusuf Sicak, Bedriye Seda Kursun Aktar, Gizem Tatar Yilmaz, Fatma Aydogmus Ozturk, Mehmet Ozturk, Tugba Taskin Tok, Emine Elcin Oruc Emre
Summary: This study aimed to synthesize novel morpholine- and thiazolidine-based compounds and evaluate their inhibition activities against antioxidant, acetylcholinesterase (AChE), butyrylcholinesterase (BChE), tyrosinase, and urease enzymes. The synthesized compounds showed significant inhibition activities, and molecular docking and molecular dynamics simulations provided further evidence.
Article
Chemistry, Multidisciplinary
Bedriye Seda Kursun Aktar, Yusuf Sicak, Gizem Tatar, Emine Elcin Oruc-Emre
Summary: Hydrazone compounds, including anticholinesterase, tyrosinase, and urease, were synthesized and their antioxidant and enzyme inhibition activities were evaluated. Several compounds exhibited high activity, especially in terms of antioxidant and anticholinesterase activities. Molecular docking analysis provided insights into the inhibition mechanism. These findings suggest the potential of these compounds for guiding clinical studies on new drugs for Alzheimer's disease.
TURKISH JOURNAL OF CHEMISTRY
(2022)
Article
Pharmacology & Pharmacy
Sevda Turk, Sevgi Karakus, Arooma Maryam, Emine Elcin Oruc-Emre
JOURNAL OF RESEARCH IN PHARMACY
(2020)
Article
Biochemistry & Molecular Biology
Cigdem Karaca, Nuray Bostancieri, Ali Ovayolu, Demet Tasdemir Kahraman
MOLECULAR BIOLOGY REPORTS
(2020)
Article
Genetics & Heredity
Esra Bozgeyik, Demet Tasdemir-Kahraman, Kaifee Arman, Ibrahim Bozgeyik, Aysegul Karakucuk-Iyidogan, Ecir Ali Cakmak
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)
