Article
Biochemistry & Molecular Biology
Bartosz Skora, Anna Lewinska, Anna Kryshchyshyn-Dylevych, Danylo Kaminskyy, Roman Lesyk, Konrad A. Szychowski
Summary: This study evaluated the cytotoxic, cytostatic, and antibacterial effects of certain 4-thiazolidinone-based derivatives on various cell lines. The results showed that Les-5935, Les-6009, and Les-6166 exhibited anticancer properties, particularly in human lung cancer cells. However, the anticancer effects of these compounds were limited to specific concentrations in certain cell lines.
Review
Chemistry, Applied
Dimitris Matiadis
Summary: 2-Pyrazolines are important five-membered heterocycles with two adjacent nitrogen atoms. They have various functional groups and unique biological properties, and are used as building blocks. In recent years, there has been significant progress in the synthesis of 2-pyrazolines, with the development of novel strategies and improvements of existing protocols. This review summarizes the synthetic methodologies from 2012 to 2022, discussing the challenges, capabilities, scopes, and limitations of the reactions, as well as substitution patterns and mechanisms where applicable.
ADVANCED SYNTHESIS & CATALYSIS
(2023)
Article
Chemistry, Multidisciplinary
Mrugesh Patel, Nilesh Pandey, Jignesh Timaniya, Paranjay Parikh, Alex Chauhan, Neeraj Jain, Kaushal Patel
Summary: A series of novel pyrazoline scaffolds were synthesized from coumarin-carbazole chalcones, and their cytotoxicity and molecular docking properties were investigated. Compounds 4a and 7b showed the highest activity, with the potential to arrest cell cycle progression and induce apoptosis.
Review
Biochemistry & Molecular Biology
Piotr Roszczenko, Serhii Holota, Olga Klaudia Szewczyk, Rostyslav Dudchak, Krzysztof Bielawski, Anna Bielawska, Roman Lesyk
Summary: Oncological diseases have become epidemic, especially in industrialized countries. Researchers in medicinal chemistry have conducted complex studies to develop novel effective anticancer drugs. This review summarizes the data on new 4-thiazolidinone-bearing hybrid molecules with potential anticancer activity and highlights the application of molecular hybridization methodologies and strategies in the design of small molecules as anticancer agents.
INTERNATIONAL JOURNAL OF MOLECULAR SCIENCES
(2022)
Article
Biochemistry & Molecular Biology
Harsha Icharam Narkhede, Avinash Shridhar Dhake, Ajaykumar Rikhabchand Surana
Summary: The novel TSC-DTCs hybrids show promising pharmacological applications with higher activity than their precursor compounds. Some of these hybrids exhibit excellent antioxidant and anticancer properties.
BIOORGANIC CHEMISTRY
(2022)
Review
Chemistry, Inorganic & Nuclear
Renata Paprocka, Malgorzata Wiese-Szadkowska, Sabina Janciauskiene, Tomasz Kosmalski, Marcelina Kulik, Anna Helmin-Basa
Summary: This review examines important research findings on the activity and toxicity of metal-based cancer drug candidates from 2018 to 2020. New multi-action platinum(IV) prodrugs and other metal complexes are designed to overcome cisplatin-resistant cancer cells. The review also discusses the use of new metal complexes for photodynamic therapy and the conjugation of complexes with conventional drugs, showcasing their new mechanisms of action.
COORDINATION CHEMISTRY REVIEWS
(2022)
Article
Chemistry, Multidisciplinary
Michele Anselmi, Adina Borbely, Eduard Figueras, Carmela Michalek, Isabell Kemker, Luca Gentilucci, Norbert Sewald
Summary: The study utilized a hydrophilic beta-glucuronidase-cleavable linker to connect an anticancer drug with a target protein, demonstrating the potential of hydrophilic sugar linkers in reducing cytotoxicity and providing guidance for the development of therapies containing hydrophobic anticancer drugs.
CHEMISTRY-A EUROPEAN JOURNAL
(2021)
Article
Chemistry, Organic
Dina A. Bakhotmah, Tarik E. Ali, Mohammed A. Assiri, Ibrahim S. Yahia
Summary: An unexpected efficient catalytic reaction was utilized to synthesize a series of potentially bioactive compounds with novel molecular structures. These compounds are based on a malononitrile skeleton fused with pyrazole, pyridine, chromone, pyrimidine, and pyrano[2,3-c]pyrazole systems. Elemental analysis and spectral techniques were used to confirm the structures of the products, and their cytotoxic activities were evaluated. Compounds 4 and 11 exhibited the highest cytotoxicity against various cancer cell lines.
POLYCYCLIC AROMATIC COMPOUNDS
(2022)
Article
Chemistry, Medicinal
Md Jahangir Alam, Ozair Alam, Ahmad Perwez, Moshahid Alam Rizvi, Mohd Javed Naim, Vegi Naidu, Mohd Imran, Mohammed M. Ghoneim, Sultan Alshehri, Faiyaz Shakeel
Summary: In this study, a series of compounds were designed, synthesized, and evaluated for their anti-cancer activity and cytotoxicity. Compound 5o showed excellent cytotoxicity and most of the compounds exhibited drug-like properties.
Review
Plant Sciences
Jose Jailson Lima Bezerra, Anderson Angel Vieira Pinheiro
Summary: Cyperus rotundus is widely used in traditional medicine in Asian countries and has shown potential anticancer effects against various tumor cell lines, with its chemical compounds playing a key role.
SOUTH AFRICAN JOURNAL OF BOTANY
(2022)
Article
Pharmacology & Pharmacy
Alicja Chrzanowska, Dagmara Kurpios-Piec, Barbara Zyzynska-Granica, Ewelina Kiernozek-Kalinska, Wen Xin Lay, Andrzej K. Ciechanowicz, Marta Struga
Summary: The positive trend in cancer treatment management is to explore the antineoplastic potential of widely used and safe drugs with different clinical purposes. Moxifloxacin, a fourth-generation fluoroquinolone with broad-spectrum antibacterial activity, has shown promising cytotoxic potential as moxifloxacin conjugates with fatty acids. These conjugates exhibited stronger cytotoxic activity than free moxifloxacin, especially with oleic and stearic acid, without toxicity to normal cells. The conjugates activated caspases 3/7 and induced late apoptosis in cancer cells, and also showed potential anti-inflammatory effects.
EUROPEAN JOURNAL OF PHARMACOLOGY
(2023)
Article
Biochemistry & Molecular Biology
Malgorzata Fabijanska, Maria M. Kasprzak, Justyn Ochocki
Summary: The study found that ruthenium compounds can partially or completely overcome the resistance to platinum drugs by activating apoptosis pathways and inducing loss of mitochondrial membrane potential, while platinum compounds have cytostatic effects requiring longer exposure time. Additionally, cisplatin-resistant cells have higher glutathione levels compared to sensitive cells, indicating mechanisms to evade apoptosis caused by DNA damage.
INTERNATIONAL JOURNAL OF MOLECULAR SCIENCES
(2021)
Review
Chemistry, Medicinal
Naiara Cassia Gancedo, Raquel Isolani, Natalia Castelhano de Oliveira, Celso Vataru Nakamura, Daniela Cristina de Medeiros Araujo, Andreia Cristina Conegero Sanches, Fernanda Stumpf Tonin, Fernando Fernandez-Llimos, Danielly Chierrito, Joao Carlos Palazzo de Mello
Summary: This study aimed to synthesize the anticancer and anti-proliferative potential of Limonium species through a systematic review. The results indicate that Limonium species have the potential to be a source of new potential cytotoxic and anticancer agents. However, further research and improved experimental designs are needed to better understand the mechanism of action of these compounds.
Article
Chemistry, Multidisciplinary
S. Kainth, V. Sharma, M. Bhagat, S. Basu
Summary: The study utilized microwave technology to synthesize carbon dots with high quantum yield and fluorescence, combined with other materials to prepare fluorescent hybrid nano-powders, successfully applied for detecting sweat latent fingermarks on non-porous surfaces. The research also revealed that these fluorescent hybrid nano-powders have low cytotoxicity and biocompatibility, while demonstrating inhibitory effects on breast cancer cells.
MATERIALS TODAY CHEMISTRY
(2022)
Article
Chemistry, Multidisciplinary
Justus Reitz, Patrick W. Antoni, Julian J. Holstein, Max M. Hansmann
Summary: Recently, stable diazoalkenes have gained attention in organic chemistry as a new substance class. A general synthetic approach using a Regitz-type diazo transfer with azides is established, which allows for the synthesis of pyridine diazoalkenes. This approach is applicable to weakly polarized olefins as well. The properties of these pyridine-derived diazoalkenes are distinct from previously reported classes.
ANGEWANDTE CHEMIE-INTERNATIONAL EDITION
(2023)
Article
Chemistry, Medicinal
Dimitris Matiadis, Dimitrios Tsironis, Valentina Stefanou, Spyridon Boussias, Angeliki Panagiotopoulou, Vickie McKee, Olga Igglessi-Markopoulou, John Markopoulos
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
(2020)
Article
Chemistry, Medicinal
Dimitris Matiadis, Tatiana Saporiti, Elena Aguilera, Xavier Robert, Christophe Guillon, Nallely Cabrera, Ruy Perez-Montfort, Marina Sagnou, Guzman Alvarez
Summary: In this study, a small library of functionalized compounds derived from curcuminoids were synthesized and evaluated for their trypanosomicidal activities. Compounds 4a and 4e showed significant activity against epimastigotes of Trypanosoma cruzi, while compound 6b effectively inhibited T. cruzi triosephosphate isomerase, demonstrating their potential as a new family of T. cruzi inhibitors with up to 16-fold higher potency compared to their curcuminoid precursors.
FUTURE MEDICINAL CHEMISTRY
(2021)
Article
Biochemistry & Molecular Biology
Dimitris Matiadis, Panagiota G. Liggri, Eftichia Kritsi, Niki Tzioumaki, Panagiotis Zoumpoulakis, Dimitrios P. Papachristos, George Balatsos, Marina Sagnou, Antonios Michaelakis
Summary: The study showed that curcuminoids and monocarbonyl curcumin derivatives have high larvicidal activity against Cx. pipiens and Ae. albopictus, with compounds like curcumin, demethoxycurcumin, curcumin-BF2 complex, and a monocarbonyl tetramethoxy curcumin derivative exhibiting the highest activity against both mosquito species.
INTERNATIONAL JOURNAL OF MOLECULAR SCIENCES
(2021)
Article
Chemistry, Physical
Dimitris Matiadis, Katarzyna E. Nowak, Eleni Alexandratou, Antonios Hatzidimitriou, Marina Sagnou, Raffaello Papadakis
Summary: In this work, two fluorescent 2-pyrazoline derivatives with remarkable (fluoro) solvatochromic behavior were successfully synthesized and fully characterized. The effects of solvent polarity on the absorption and fluorescence spectra of the derivatives were quantified and rationalized using LSERs. Differences in the solvatochromic behavior among the derivatives were revealed based on their structural diversity.
JOURNAL OF MOLECULAR LIQUIDS
(2021)
Article
Biochemistry & Molecular Biology
Dimitris Matiadis, See-Ting Ng, Eric H-L Chen, Georgia Nigianni, Veroniki P. Vidali, Aleksander Canko, Rita P-Y Chen, Marina Sagnou
Summary: Ten hydroxylated monocarbonyl curcumin derivatives were designed, synthesized, and evaluated for their NEP upregulating potential, with compound 4 showing the highest activity. Derivatives bearing a cyclohexanone group exhibited higher activity enhancement compared to their acetone counterparts.
Article
Chemistry, Medicinal
Dimitris Matiadis, Valentina Stefanou, Dimitrios Tsironis, Angeliki Panagiotopoulou, Olga Igglessi-Markopoulou, John Markopoulos
Summary: The synthesis and biological evaluation of 5-arylidene-N-acetyl-tetramic acids cadmium(II) complexes were reported. The complexes showed promising antimicrobial activities against MRSA and C. neoformans, indicating the potential for further development as novel antibacterial and antifungal agents.
ARCHIV DER PHARMAZIE
(2021)
Editorial Material
Chemistry, Organic
Dimitris Matiadis, Eleftherios Halevas
Article
Neurosciences
Barbara Mavroidi, Archontia Kaminari, Dimitris Matiadis, Dimitra Hadjipavlou-Litina, Maria Pelecanou, Athina Tzinia, Marina Sagnou
Summary: Alzheimer's disease involves the formation of Aβ oligomers, oxidative stress, inflammation and increased acetylcholinesterase activity. Synthetic isatin thiosemicarbazones have shown potential in preventing Aβ aggregation, protecting cells, and inhibiting Akt and GSK-3β phosphorylation.
Article
Chemistry, Inorganic & Nuclear
Valentina Stefanou, Dimitris Matiadis, Dimitrios Tsironis, Olga Igglessi-Markopoulou, Vickie Mckee, John Markopoulos
Summary: This study investigates the structure and assembly of four supramolecular coordination complexes, demonstrating the construction of metallosupramolecular architectures through self-assembly techniques. The findings provide valuable experimental data for the field of supramolecular chemistry.
JOURNAL OF COORDINATION CHEMISTRY
(2022)
Article
Chemistry, Physical
Dimitris Matiadis, Christina Fountzoula, Maria Trapali, Petros Karkalousos, Marina Sagnou
Summary: The study investigated the sensing properties of a monocarbonyl analogue of curcumin for cyanide recognition, demonstrating excellent selectivity and a convenient detection method.
JOURNAL OF MOLECULAR STRUCTURE
(2022)
Article
Biochemistry & Molecular Biology
Tatiana Saporiti, Mauricio Cabrera, Josefina Bentancur, Maria Elisa Ferrari, Nallely Cabrera, Ruy Perez-Montfort, Francisco J. Aguirre-Crespo, Jorge Gil, Ulises Cuore, Dimitris Matiadis, Marina Sagnou, Guzman Alvarez
Summary: Rhipicephalus microplus, the common cattle tick, is a major ectoparasite in livestock causing significant economic and health losses. There is an urgent need to find alternatives for controlling resistant ticks since all currently available acaricides have reported resistance. This study discovered compounds derived from natural sources and synthetic organic molecules that showed potential as acaricidal agents against resistant ticks, with minimal toxicity to mammalian cells.
Article
Biochemistry & Molecular Biology
Panagiota Pantiora, Veronika Furlan, Dimitris Matiadis, Barbara Mavroidi, Fereniki Perperopoulou, Anastassios C. Papageorgiou, Marina Sagnou, Urban Bren, Maria Pelecanou, Nikolaos E. Labrou
Summary: This study investigated the inhibitory effects of two curcuminoids and eleven monocarbonyl curcumin analogues against human glutathione transferase P1-1 (hGSTP1-1). The results showed that Demethoxycurcumin (Curcumin II) and three monocarbonyl curcumin analogues exhibited the highest inhibitory activity, with IC50 values ranging between 5.45 and 37.72 μM. The most potent inhibitors functioned as non-competitive/mixed-type inhibitors. Structural analysis revealed that the strongest hGSTP1-1 inhibitor, DM96, formed hydrophobic interactions and hydrogen bonds with specific residues, contributing to its superior inhibitory activity. The study highlights the potential of DM96 as a strong hGSTP1-1 inhibitor and its relevance for cancer chemosensitization.
Article
Chemistry, Organic
Eleftherios Halevas, Antonios Hatzidimitriou, Barbara Mavroidi, Marina Sagnou, Maria Pelecanou, Dimitris Matiadis
Summary: A novel Cu(II) complex based on Schiff base was successfully synthesized, with its crystal structure reflecting a one-dimensional polymeric compound.
Article
Biochemistry & Molecular Biology
Dimitris Matiadis, Maria Karagiaouri, Barbara Mavroidi, Katarzyna E. Nowak, Georgios Katsipis, Maria Pelecanou, Anastasia Pantazaki, Marina Sagnou
Summary: The study demonstrated the efficient synthesis of a novel pyrazoline-pyridine silver complex with potent antibacterial and antifungal activities, particularly against Gram-negative bacteria, as well as reduction of biofilm formation by MRSA and Pseudomonas aeruginosa. The complex showed strong DNA binding, suggesting a mechanism related to its antibacterial activity.
Article
Chemistry, Organic
Dimitris Matiadis, Barbara Mavroidi, Angeliki Panagiotopoulou, Constantinos Methenitis, Maria Pelecanou, Marina Sagnou