V3 / ADC VILKOVÁ, Mária [15 %] - MICHALKOVÁ, Radka [15 %] - KELLO, Martin [15 %] - SABOLOVÁ, Danica [10 %] - TAKÁČ, Peter [10 %] - KUDLIČKOVÁ, Zuzana [10 %] - GARBEROVÁ, Monika [2 %] - TVRDOŇOVÁ, Monika [10 %] - BÉRES, Tibor [3 %] - MOJŽIŠ, Ján [10 %]. Discovery of novel acridine-chalcone hybrids with potent DNA binding and antiproliferative activity against MDA-MB-231 and MCF-7 cells. In Medicinal Chemistry Research. ISSN 1054-2523, 2022, vol. 31, no. 8, p. 1323-1338. (2022: 2.6 - IF, 2.3 - IF 5y, 56 - H-index, 0.377 - SJR, Q2 - SJR Best Q, Q3 - JCR Best Q). (2022 - Current Contents). Dostupné na internete: .

Basic data
OCA1. Surname awarded to the assessed person	Takáč
OCA2. Name awarded to the assessed person	Peter
OCA3. Degrees awarded to the assessed person	Assoc. prof. , Pharm.D., PhD
OCA4. Hyperlink to the entry of the person in the Register of university staff	https://www.portalvs.sk/regzam/detail/27235
OCA5. Area of assessment	study programme pharmacy · I. + II. degree
OCA6. Category of the research/artistic/other output	scientific output
OCA7. Year of publication of the research/artistic/other output	2022
OCA8. ID of the record in the Central Registry of Publication Activity (CRPA) or the Central Registry of Artistic Activity (CRAA)	ID: 514052
OCA9. Hyperlink to the record in CRPA or CRAA	https://app.crepc.sk/?fn=detailBiblioForm&sid=5F197B5B0CD8DA9E8B68457241
Characteristics of the output that is not registered in CRPA or CRAA
OCA10. Hyperlink to the record in another publicly accessible register, catalogue of research/ artistic/other outputs
OCA11. Characteristics of the output in the format of the CRPA or the CRAA bibliographic record, if the output is not available in a publicly accessible register or catalogue of outputs	V3 / ADC VILKOVÁ, Mária [15 %] - MICHALKOVÁ, Radka [15 %] - KELLO, Martin [15 %] - SABOLOVÁ, Danica [10 %] - TAKÁČ, Peter [10 %] - KUDLIČKOVÁ, Zuzana [10 %] - GARBEROVÁ, Monika [2 %] - TVRDOŇOVÁ, Monika [10 %] - BÉRES, Tibor [3 %] - MOJŽIŠ, Ján [10 %]. Discovery of novel acridine-chalcone hybrids with potent DNA binding and antiproliferative activity against MDA-MB-231 and MCF-7 cells. In Medicinal Chemistry Research. ISSN 1054-2523, 2022, vol. 31, no. 8, p. 1323-1338. (2022: 2.6 - IF, 2.3 - IF 5y, 56 - H-index, 0.377 - SJR, Q2 - SJR Best Q, Q3 - JCR Best Q). (2022 - Current Contents). Dostupné na internete: .
OCA12. Type of the output (if the output is not registered in CRPA or CRAA)
OCA13. Hyperlink to the webpage where the output is available (full text, other documentation, etc.)
OCA14. Characteristics of the author's contribution
OCA15. Annotation of the output with contextual information concerning the description of creative process and the content of the research/artistic/other activity, etc.
Other data
OCA16. Annotation of the output in English	Two series of novel chalcone derivatives containing acridin-9-yl or acridin-4-yl moieties were synthesized, structurally characterized, and tested for growth inhibitory activity against human cancer cell lines. Among the 12 compounds, (2E)-3-(acridin-4-yl)-1-(3,4,5-trimethoxyphenyl)-prop-2-en-1-one (4e) showed the most potent cytotoxicity against aggressive triple-negative breast cancer cells (MDA-MB-231) and estrogen-responsive MCF-7 cells, with IC50 values of 8.4 and 7.7 μM, respectively. Flow cytometry revealed that 4e induced cell cycle arrest in the G2/M phase and increased the sub-G0/G1 cell population, indicating apoptosis. Further studies demonstrated that 4e triggered mitochondria-mediated apoptosis involving loss of mitochondrial membrane potential, dysregulation of Bax and Bcl-xl proteins, cytochrome c release, caspase-7 activation, and PARP cleavage. Upregulation of tumor suppressor proteins p53 and p21 was also observed. In vitro DNA interaction assays showed that 4e binds calf thymus DNA through a bimodal mode: intercalation and groove binding. Additionally, 4e displayed affinity for bovine serum albumin, suggesting efficient transport in the bloodstream. These findings support 4e as a promising candidate for further development as an antitumor agent against breast cancer.
OCA17. List of maximum 5 most significant citations corresponding to the output	[1]/[1] GÜLTEKIN, Büşra - INCI ÖZBAĞCI, Duygu - AYDIN, İpek , Rahmiye - ARI, Fer- AYDINda - ZORLU, Yunus. New copper(II) complexes containing tryptophan based Schiff bases as promising antiproliferative agents on breast cancer cells. In Journal of Molecular Structure, 2024-04-05, 1301, pp. ISSN 00222860. Dostupné na: https://doi.org/10.1016/j.molstruc.2023.137273., Registrované v: WOS, SCOPUS [1]/[1] WANG, Huan - ZHU, Juanying - ZHANG, Qianru - TANG, Jie - HUANG, Xufeng. Current scenario of chalcone hybrids with antibreast cancer therapeutic applications. In Archiv der Pharmazie, 2024-05-01, 357, 5, pp. ISSN 03656233. Dostupné na: https://doi.org/10.1002/ardp.202300640., Registrované v: WOS, SCOPUS [1]/[1] ÖZBAĞCI, Duygu İnci - GÜLTEKIN, Büşra - AYDIN, İpek - AYDIN, Rahmiye - ARI, Ferda - ZORLU, Yunus. New copper (II) complexes bearing tryptophan-based Schiff bases and 2,2′-bipyridine: Crystal structures, DNA/BSA interactions and antiproliferative activities. In Applied Organometallic Chemistry, 2024-04-01, 38, 4, pp. ISSN 02682605. Dostupné na: https://doi.org/10.1002/aoc.7369., Registrované v: WOS, SCOPUS [1]/[1] JAVADI, Samira - HABIBI, Davood. Comparative study of cerium-manganese ratios in the design of Ce-Mn-binuclear LDH-based Cu complex: a potent nanocatalyst for the green synthesis of spiro[acridine-9,3’-indole]triones. In Scientific Reports, 2024-12-01, 14, 1, pp. Dostupné na: https://doi.org/10.1038/s41598-024-75724-3., Registrované v: WOS, SCOPUS [1]/[1] AHMADI, Shirin - OLAD, Ali - FATHI, Marziyeh - MOLAVI, Ommoleila. An injectable chitosan based dual thermo/pH-responsive fast gelling hydrogel loaded by methotrexate/curcumin as local drug delivery system of breast cancer. In Journal of Drug Delivery Science and Technology, 2025-02-01, 104, pp. ISSN 17732247. Dostupné na: https://doi.org/10.1016/j.jddst.2024.106540., Registrované v: WOS, SCOPUS
OCA18. Characteristics of the output's impact on socio-economic practice	The output brings a significant contribution to socio-economic practice by presenting a new chalcone derivative (4e) with strong anticancer activity against aggressive triple-negative and estrogen-responsive breast cancer. The compound’s ability to induce apoptosis and cell cycle arrest makes it a promising candidate for developing more effective breast cancer treatments. Its potential can lead to improved treatment outcomes, increased patient survival, and reduced burden on healthcare systems. Moreover, its efficient binding to serum proteins suggests good distribution in the body, which is crucial for clinical application. This research supports the development of new, targeted, and more effective anticancer therapies, positively impacting the healthcare sector and economy by lowering treatment costs and improving patients’ quality of life.
OCA19. Characteristics of the output and related activities' impact on the educational process	The output and related activities significantly enrich the educational process in pharmacy, biomedicine, and molecular biology. Students gain exposure to modern methods of drug synthesis and testing, including analysis of the anticancer mechanisms of chalcone derivative 4e. This research fosters the development of critical thinking, experimental skills, and an interdisciplinary approach combining chemistry, biology, and medicine. Involvement in similar projects enhances students’ practical experience and motivation for scientific work. It also prepares them for challenges in cancer research and treatment, contributing to the formation of qualified professionals capable of developing innovative therapies.