Review
Chemistry, Medicinal
Kritika Laxmikeshav, Pooja Kumari, Nagula Shankaraiah
Summary: This review provides a comprehensive report on the design strategies of sulfur-bearing cytotoxic agents and their potential in anticancer therapy. The article discusses various sulfur-containing heterocyclic scaffolds and their cytotoxic effects through multiple mechanisms. The assessment of antiproliferative activities allows for a proficient evaluation of the structure-activity relationships of the synthesized molecules.
MEDICINAL RESEARCH REVIEWS
(2022)
Article
Biochemistry & Molecular Biology
Stefano Scoditti, Eslam Dabbish, Emilia Sicilia
Summary: The reactivity of phenanthriplatin and its derivatives was investigated through quantum mechanical and molecular dynamics approaches. Increasing the number of rings in the phenanthridine ligand was found to influence the activity and cytotoxicity of the complexes.
JOURNAL OF INORGANIC BIOCHEMISTRY
(2021)
Article
Chemistry, Physical
Kritika Laxmikeshav, Pooja Sharma, Manisurya Palepu, Pravesh Sharma, Ashutosh Mahale, Joel George, Regur Phanindranath, Manoj P. Dandekar, Onkar Prakash Kulkarni, Narayana Nagesh, Nagula Shankaraiah
Summary: A new series of carboxamide-bearing benzimidazole derivatives have been investigated for their cytotoxicity on selected human tumor cells. Compounds 10g and 10m showed selective cytotoxicity towards SK-Mel-28 skin cancer cells and were safe for human non-cancerous lung epithelial cells.
JOURNAL OF MOLECULAR STRUCTURE
(2023)
Article
Biochemistry & Molecular Biology
Manish Rana, Imran Ansari, Charmy Twala, Sumbul Khan, Anupam Mandal, Rahisuddin Rahisuddin
Summary: In this study, a series of Pyrazoline derivatives were designed and synthesized, and their molecular structures were characterized using various techniques. The compounds showed promising anticancer activity against MCF-7 cancer cells with low toxicity towards HepG2 normal cells. The study also investigated the DNA binding interactions, antioxidant capacity, and ADMET properties of the derivatives.
JOURNAL OF BIOMOLECULAR STRUCTURE & DYNAMICS
(2023)
Article
Biochemistry & Molecular Biology
Yan-Ru Fan, Bo-Jin Wang, Deng-Guo Jia, Xin-Bin Yang, Yu Huang
Summary: A series of tripodal ferrocenyl bis-naphthalimide derivatives were synthesized to study their DNA binding ability and cytotoxicity induced by reactive oxygen species. All compounds exhibited good DNA binding ability, with the structure of n = 3, m = 1 being identified as the best choice based on structure cytotoxicity relationship.
JOURNAL OF INORGANIC BIOCHEMISTRY
(2021)
Article
Chemistry, Multidisciplinary
Danica Sabolova, Simona Sovova, Ladislav Janovec, Eva Timko, David Jager, Jana Tothova
Summary: Four novel 3,6-bis[(alkylamino)ureido]acridines were synthesized and characterized using NMR spectra. In vitro DNA binding studies showed that these compounds bind to DNA through intercalation, as confirmed by absorption, fluorescence, circular dichroism and DNA viscosity measurements. The binding constant (K-b) values ranged from 4.46 to 6.73 x 10(4) M-1.
Article
Chemistry, Multidisciplinary
Mohamed A. A. Radwan, Osamah Al Rugaie, Waleed Al Abdulmonem, Mohammad Y. Alfaifi, Serag Eldin Elbehairi
Summary: The study described the synthesis of a new series of indolylpyrrole derivatives and tested their in vitro cytotoxic activity against prostate cancer cells, ovarian cancer cells, and colorectal cancer cells. Some compounds exhibited potent anticancer activity, laying the groundwork for further exploration of these compounds as antiproliferative agents.
ARABIAN JOURNAL OF CHEMISTRY
(2021)
Article
Biochemistry & Molecular Biology
Dawid Lazewski, Malgorzata Kucinska, Edward Potapskiy, Joanna Kuzminska, Lukasz Popenda, Artur Tezyk, Tomasz Goslinski, Marcin Wierzchowski, Marek Murias
Summary: This study has successfully developed a series of curcumin derivatives through modifications. The results showed that one derivative with PEG chains and a BF2 moiety exhibited higher cytotoxicity against bladder cancer cells and stronger anticancer effects under hypoxic conditions. However, PEGylation did not improve cellular uptake, and the lack of serum proteins limited intracellular uptake. The regulation of cell cycle and stress-related proteins may be involved in the anticancer mechanism. In conclusion, PEGylated curcumin derivatives are more effective anti-bladder cancer drugs than the parent compound, and derivative 5 deserves further investigation to elucidate its anticancer mechanism under hypoxic conditions.
INTERNATIONAL JOURNAL OF MOLECULAR SCIENCES
(2023)
Review
Chemistry, Multidisciplinary
Maria Letizia Di Pietro, Giuseppina La Ganga, Francesco Nastasi, Fausto Puntoriero
Summary: The paragraph discusses the importance of transition metal complexes with dppz-type ligands in studying the structure of DNA helix and their role as DNA light-switches. It also provides a brief overview of the binding mechanism of Ru-dppz complexes with DNA and their effects on structural modifications and biological applications.
APPLIED SCIENCES-BASEL
(2021)
Article
Chemistry, Medicinal
Nazariy Pokhodylo, Nataliya Finiuk, Olha Klyuchivska, Mykola A. Tupychak, Vasyl Matiychuk, Evgeny Goreshnik, Rostyslav Stoika
Summary: The N-(4-thiocyanatophenyl)-1H-1,2,3-triazole-4-carboxamides were synthesized using CDI as amide coupling reagents, and their antiproliferative potency towards different cell lines was evaluated. One compound with promising anticancer activity was selected for further studies as a biocompatible agent.
EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
(2022)
Review
Biochemistry & Molecular Biology
Potlapati Varakumar, Kalirajan Rajagopal, Baliwada Aparna, Kannan Raman, Gowramma Byran, Clara Mariana Goncalves Lima, Salma Rashid, Mohammed H. Nafady, Talha Bin Emran, Slawomir Wybraniec
Summary: This review provides a summary of the recent advancements in the chemistry of acridines as anti-cancer agents, including new structural and biologically active attributes. Acridine derivatives are extensively studied as potential anti-cancer drugs. Despite their high cytotoxic activity, the clinical application of acridines is limited or even excluded due to side effects.
Article
Chemistry, Medicinal
Gleyton Sousa, Maria C. F. de Almeida, Lucas L. Locio, Vanda L. dos Santos, Daniel P. Bezerra, Valdenizia R. Silva, Sinara M. de Almeida, Alice Simon, Thiago da S. Honorio, Lucio M. Cabral, Rosane N. Castro, Ricardo O. de Moura, Arthur E. Kummerle
Summary: In this study, twenty new acridine-thiosemicarbazone derivatives were synthesized and showed strong antiproliferative activities, with DL-08 exhibiting the highest potency. Certain active derivatives were studied for their interactions with DNA and inhibition of topoisomerase II alpha by in silico and in vitro methods. Non-clinical toxicity tests on mice at a dose of 2000 mg/kg showed no serious signs of toxicity for selected compounds.
Article
Biochemistry & Molecular Biology
Lini Huo, Xiaochen Liu, Yogini Jaiswal, Hao Xu, Rui Chen, Rumei Lu, Yaqin Nong, Leonard Williams, Yan Liang, Zhiruo Jia
Summary: We designed and synthesized a series of novel acridine-triazole and acridine-thiadiazole derivatives. These compounds showed high levels of antitumor activity against gastric cancer cells and bladder cancer cells, while exhibiting low toxicity to normal liver cells. Moreover, their pharmacological mechanisms and effects on cell cycle and apoptosis were evaluated. Furthermore, these compounds demonstrated low cytotoxicity to zebrafish but strong inhibition of the formation of zebrafish sub-intestinal veins, suggesting potential clinical applications.
INTERNATIONAL JOURNAL OF MOLECULAR SCIENCES
(2023)
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
Chemistry, Medicinal
Daria Rozycka, Aleksandra Kowalczyk, Marta Denel-Bobrowska, Olga Kuzmycz, Magdalena Gapinska, Pawel Staczek, Agnieszka B. Olejniczak
Summary: Synthesis of carborane-modified acridine analogs showed their DNA-binding ability and potential anticancer activities. Compound 30 demonstrated strong interaction with ct-DNA, while compound 29 changed the conformation of ct-DNA. Compound 30 exhibited cytotoxicity, inhibited cell proliferation, arrested the cell cycle, and induced reactive oxygen species production in the HeLa cancer cell line.
Review
Toxicology
Maria Kozurkova, Danica Sabolova, Pavol Kristian
Summary: Heterocycles, especially acridine and its derivatives, have been studied intensively for their potential therapeutic properties. The multitarget properties of acridine derivatives, particularly in inhibiting topoisomerase enzymes and interfering with DNA function, make them promising candidates for cancer treatment. Additionally, these compounds show antibacterial and antimalarial activities.
JOURNAL OF APPLIED TOXICOLOGY
(2021)
Article
Biochemistry & Molecular Biology
Eva Konkolova, Monika Hudacova, Slavka Hamulakova, Rastislav Jendzelovsky, Jana Vargova, Juraj Sevc, Peter Fedorocko, Maria Kozurkova
Summary: A series of new drugs with tacrine and coumarin pharmacophores were studied for their ability to inhibit human lung carcinoma cell growth and topoisomerase I and II activity. All compounds were found to completely inhibit topoisomerase I activity, with derivatives 1c and 1d displaying the highest activity, likely due to their longer chain length between tacrine and coumarin moieties.
Review
Toxicology
Maria Kozurkova
Summary: The potential of acridines as topoisomerase II inhibitors was first discovered in 1984, leading to the testing of numerous derivatives with various substituents. Recent studies have focused on novel acridine derivatives and their activity against topoisomerase II.
JOURNAL OF APPLIED TOXICOLOGY
(2022)
Article
Biochemistry & Molecular Biology
Elsayed Ali Drweesh, Veronika Kucharova, Vladislav Volarevic, Dragana Miloradovic, Aleksandar D. Ilic, Ivana R. Radojevic, Ivana Rakovic, Romana Smolkova, Maria Vilkova, Danica M. Sabolova, Mohamed Elnagar, Ivan Potocnak
Summary: In this study, four hybrid organic-inorganic compounds were synthesized through organic cation modulation. The compounds were characterized and evaluated for their DNA interaction, antimicrobial activity, and antiproliferative activity. Compound 1 and compound 2 showed selective and high cytotoxicity against human lung and breast cancer cells.
JOURNAL OF INORGANIC BIOCHEMISTRY
(2022)
Article
Chemistry, Medicinal
Maria Vilkova, Radka Michalkova, Martin Kello, Danica Sabolova, Peter Takac, Zuzana Kudlickova, Monika Garberova, Monika Tvrdonova, Tibor Beres, Jan Mojzis
Summary: In this study, two series of novel chalcone derivatives were synthesized and evaluated for their inhibitory activity against human cancer cell lines. Compound 4e exhibited the best cytotoxic activity against breast cancer cells, inducing apoptosis and interacting with DNA. These findings suggest that compound 4e has the potential to be developed as an antitumor agent for breast cancer.
MEDICINAL CHEMISTRY RESEARCH
(2022)
Article
Biochemistry & Molecular Biology
Maria Vilkova, Monika Hudacova, Nikola Palusekova, Rastislav Jendzelovsky, Miroslav Almasi, Tibor Beres, Peter Fedorocko, Maria Kozurkova
Summary: A series of novel acridine derivatives were synthesized and evaluated for their potential as DNA topoisomerase inhibitors and anticancer agents. One of the derivatives (compound 3b) displayed high binding affinity and potential antitumor activity. Other derivatives also showed varying effects on the metabolic activity of cancer cells. Overall, these novel compounds have potential for further development as anticancer agents.
Review
Pharmacology & Pharmacy
Martin Majernik, Rastislav Jendzelovsky, Jana Vargova, Zuzana Jendzelovska, Peter Fedorocko
Summary: Photodynamic therapy (PDT) for cancer has advantages over conventional therapeutic approaches, but multidrug resistance is a major limitation. The use of dynamic nanoplatforms can minimize the effect of multidrug resistance and significantly enhance the therapeutic efficacy of PDT. Additionally, nanoparticles can induce synergistic effects when used in combination treatments and improve the target potential in multidrug resistant and cancer stem cells.
Article
Biochemistry & Molecular Biology
Kristina Krochtova, Annamaria Haleckova, Ladislav Janovec, Michaela Blizniakova, Katarina Kusnirova, Maria Kozurkova
Summary: A series of novel 3,9-disubstituted acridines were synthesized and their biological potential was investigated. The physicochemical properties of the acridines were studied in relation to their biological activity, and it was found that the acridine derivatives inhibited both topoisomerase I and topoisomerase II alpha. The acridines also showed strong binding affinity to DNA and demonstrated cytostatic activity against cancer cell lines.
Article
Chemistry, Inorganic & Nuclear
Michaela Harmosova, Martin Kello, Michal Goga, Ludmila Tkacikova, Maria Vilkova, Danica Sabolova, Simona Sovova, Erika Samolova, Miroslava Litecka, Veronika Kucharova, Juraj Kuchar, Ivan Potocnak
Summary: In this study, five metal complexes were synthesized and characterized by IR spectroscopy, elemental analysis, and single crystal X-ray structure analysis. The stability of these complexes in solution was confirmed by NMR spectroscopy. The prepared complexes showed strong antiproliferative activity against cancer cell lines, especially complex 3. However, they exhibited poor selectivity towards normal cells, except for complex 5, which showed some level of selectivity. Only complex 5 showed antibacterial potential. Additionally, the DNA/BSA binding potential of complexes 1-3 was investigated using UV-vis and fluorescence spectroscopic methods.
Article
Chemistry, Multidisciplinary
Danica Sabolova, Simona Sovova, Ladislav Janovec, Eva Timko, David Jager, Jana Tothova
Summary: Four novel 3,6-bis[(alkylamino)ureido]acridines were synthesized and characterized using NMR spectra. In vitro DNA binding studies showed that these compounds bind to DNA through intercalation, as confirmed by absorption, fluorescence, circular dichroism and DNA viscosity measurements. The binding constant (K-b) values ranged from 4.46 to 6.73 x 10(4) M-1.
Article
Chemistry, Multidisciplinary
Eva Konkolova, Monika Hudacova, Slavka Hamulakova, Katarzyna E. E. Nowak, Maria Kozurkova
Summary: Identifying the binding mode of tacrine-coumarin derivatives with DNA is essential for understanding their pharmacological activity. This study evaluated the binding affinity of seven derivatives to ctDNA using various spectroscopic techniques and determined that they bind through a non-intercalative groove binding mode. Molecular docking results further confirmed the non-intercalative DNA binding mode for two specific derivatives.
Article
Chemistry, Inorganic & Nuclear
Michaela Harmosova, Martin Kello, Michal Goga, Richard Frenak, L'udmila Tkacikova, Maria Vilkova, Danica Sabolova, Simona Sovova, Erika Samol'ova, Ivan Potocnak
Summary: Four new zinc(II) complexes containing 5-chloro-7-nitro-8-hydroxyquinoline molecules were synthesized and characterized. The complexes exhibited different structures and coordination modes, and showed varied antiproliferative and antibacterial activities.
Article
Biochemistry & Molecular Biology
Michaela Rendosova, Robert Gyepes, Simona Sovova, Danica Sabolova, Maria Vilkova, Petra Olejnikova, Martin Kello, Boris Lakatos, Zuzana Vargova
Summary: A series of novel Ga(III)-pyridine carboxylates were successfully synthesized by a simple one-step procedure. The molecular structure, inter and intramolecular interactions, and their influence on spectral and thermal properties were confirmed by various analysis techniques. The complex species speciation, antimicrobial activity, and anticancer activity were investigated, as well as the binding activity between the complexes and bovine serum albumin.
JOURNAL OF BIOLOGICAL INORGANIC CHEMISTRY
(2023)
