In vitro anti-breast cancer study of hybrid cinnamic acid derivatives bearing 2-thiohydantoin moiety

被引:2
作者
Binjawhar, Dalal Nasser [1 ]
Al-Salmi, Fawziah A. [2 ]
Alghamdi, Maha Ali [3 ]
Abu Ali, Ola A. [4 ]
Fayad, Eman [3 ]
Rizzk, Youstina William [5 ]
Ali, Nourhan M. [6 ]
El-Deen, Ibrahim Mohey [7 ]
Eltamany, Elsayed H. [6 ]
机构
[1] Princess Nourah Bint Abdulrahman Univ, Coll Sci, Dept Chem, POB 84428, Riyadh 11671, Saudi Arabia
[2] Taif Univ, Coll Sci, Biol Dept, POB 11099, Taif 21944, Saudi Arabia
[3] Taif Univ, Coll Sci, Dept Biotechnol, POB 11099, Taif 21944, Saudi Arabia
[4] Taif Univ, Coll Sci, Dept Chem, POB 11099, Taif 21944, Saudi Arabia
[5] Port Said Univ, Fac Sci, Dept Chem, Div Biochem, Port Said, Egypt
[6] Suez Canal Univ, Fac Sci, Dept Chem, Ismailia, Egypt
[7] Port Said Univ, Fac Sci, Dept Chem, Div Organ Chem, Port Said, Egypt
关键词
2-thiohydantoin; anti-breast cancer; caspase-9; cinnamic acid and ester derivatives; Nrf2; topoisomerase II; BIOLOGICAL EVALUATION; THIOHYDANTOIN; INHIBITORS; DESIGN;
D O I
10.1080/17568919.2024.2366694
中图分类号
R914 [药物化学];
学科分类号
100701 ;
摘要
Aim: To synthesize new hybrid cinnamic acids (10a, 10b and 11) and ester derivatives (7, 8 and 9) and investigate their anti-breast cancer activities. Materials & methods: Compounds 7-11 were evaluated (in vitro) for their cytotoxic activities against the MCF-7 cell line. A flow cytometry examination was performed. Protein levels of nuclear factor erythroid 2-related factor 2 (Nrf2), topoisomerase II and caspase-9 were measured by qRT-PCR. Molecular docking studies were conducted. Results: Several components were discovered to be active, mainly component 11, which induced arrest in the cell cycle at phase S, greatly decreased the expression of Nrf2 and topoisomerase II; and upregulated the expression of caspase-9. Conclusion: The newly thiohydantoin-cinnamic acid hybrids can contribute to creating promising candidates for cancer drugs.
引用
收藏
页码:1665 / 1684
页数:20
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