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Quinoline–imidazole/benzimidazole Derivatives as Dual-/multi-targeting Hybrids Inhibitors with Anticancer and Antimicrobial Activity by Dumitrela Diaconu; Vasilichia Antoci; Violeta Mangalagiu; Dorina Amariucai-Mantu; Ionel I. Mangalagiu is a Biochemistry, Genetics and Molecular Biology article available to read on EtoBox.
What is Quinoline–imidazole/benzimidazole Derivatives as Dual-/multi-targeting Hybrids Inhibitors with Anticancer and Antimicrobial Activity about?
## Abstract Two new classes of hybrid quinoline–imidazole/benzimidazole derivatives (the hybrid QIBS salts and QIBC cycloadducts) were designed and synthesized to evaluate their anticancer and antimicrobial activity. The strategy adopted for synthesis is straight and efficient, in four steps: N-acylation, N-alkylation, quaternization and a Huisgen 3 + 2 cycloaddition. The in vitro single-dose anticancer assay of forty six hybrid quinoline-benzimidazole compounds reveal that one QIBS salt (11h), has an excellent quasi nonselective activity against all type of cancer cell with an excellent PGI in the area of 90–100% and very good lethality. Three others quinoline–imidazole/benzimidazole hybrids (8h, 12h, 12f) has an excellent selective activity against some cancer cell lines: breast cancer MDA-MB-468 and Leukemia HL-60 TB). The five-dose assay screening confirms that compound 11h possesses excellent anti-proliferative activity, with GI~50~ in the range of nano-molar, against some cancer cell lines: Leukemia HL-60 TB, Leukemia K-526, Leukemia RPMI-8226, Breast cancer MDA-MB-468, Lung cancer HOP-92 and Ovarian cancer IGROV1. The antibacterial assay indicates that three hybrid QIBS salt
Who reads Quinoline–imidazole/benzimidazole Derivatives as Dual-/multi-targeting Hybrids Inhibitors with Anticancer and Antimicrobial Activity?
It is typically read by researchers, students, and practitioners in Biochemistry, Genetics and Molecular Biology.
- Author
- Dumitrela Diaconu; Vasilichia Antoci; Violeta Mangalagiu; Dorina Amariucai-Mantu; Ionel I. Mangalagiu
- Publisher
- Springer Science and Business Media LLC
- Published
- 2022
- Language
- EN
- Field
- Biochemistry, Genetics and Molecular Biology (Life Sciences)