Due to a great deal of biological activities, quinoline derivatives have drawn attention for synthesis and biological activities in the search for new anticancer drug development. In this work, a variety of substituted (phenyl, nitro, cyano, N-oxide, and methoxy) quinoline derivatives (3-13) were tested in vitro for their biological activity against cancer cell lines, including rat glioblastoma (C6), human cervical cancer cells (HeLa), and human adenocarcinoma (HT29). 6-Bromo-5-nitroquinoline (4), and 6,8-diphenylquinoline (compound 13) showed the greatest antiproliferative activity as compared with the reference drug, 5-fluorouracil (5-FU), while the other compounds showed low antiproliferative activity. 6-Bromo-5-nitroquinoline (4) possesses lower cytotoxic activity than 5-FU in HT29 cell line. Due to its the apoptotic activity 6-Bromo-5-nitroquinoline (4) has the potential to cause cancer cell death.
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http://dx.doi.org/10.1002/jbt.22260 | DOI Listing |
Based on the biologically active heterocycle quinoline, we successfully synthesized a series of quinoline-based dihydrazone derivatives (3a-3d). H NMR, C NMR, ESI-HRMS, IR, element analysis, UV/Vis spectroscopy and fluorescence spectroscopy were performed to comprehensively characterize their chemical structures, spectral properties and stability. Nitrosamine impurities were not detected in 3a-3d, and the systemic toxicological assessment indicated that the toxicity of 3a-3d was lower.
View Article and Find Full Text PDFBioorg Chem
December 2024
Biotechnology Research Center, Pharmaceutical Technology Institute, Mashhad University of Medical Sciences, Mashhad, Iran; Department of Medicinal Chemistry, School of Pharmacy, Mashhad University of Medical Sciences, Mashhad, Iran. Electronic address:
In this study, novel 2-styrylquinoline derivatives possessing a planar aromatic system and a flexible side chain with an amino substituent were designed and synthesized as DNA-intercalating antitumor agents. The cytotoxic activity of the synthesized compounds was evaluated against four cancer cell lines including MCF-7 (breast cancer cells), A549 (lung epithelial cancer cells), HCT116 (colon cancer cells) and normal cell line L929 (mouse fibroblast cell line). The results displayed that the anti-cancer activity of the target quinolines is sensitive to the lipophilic nature of the C-6 and C-7 quinoline substituents.
View Article and Find Full Text PDFDalton Trans
January 2025
Laboratory for Molecular & Functional Design, Department of Engineering, Nara Women's University, Nara 630-8506, Japan.
Rational molecular design afforded fluorescent Cd sensors based on bisquinoline derivatives. Introduction of three methoxy groups at the 5,6,7-positions of the quinoline rings of BQDMEN (,'-bis(2-quinolylmethyl)-,'-dimethylethylenediamine) resulted in the reversal of metal ion selectivity in fluorescence enhancement from zinc to cadmium. Introduction of bulky alkyl groups and an ,-bis(2-quinolylmethyl)amine structure, as well as replacement of one of the two tertiary amine binding sites with an oxygen atom and the use of a 1,2-phenylene backbone significantly improved the Cd specificity.
View Article and Find Full Text PDFOrg Biomol Chem
January 2025
School of Life Sciences and Health Engineering, Jiangnan University, Jiangsu, 214122, China.
Dysfunction in the SHP1 enzyme can cause cancers and many diseases, so it is of great significance to develop novel small molecule SHP1 inhibitors. Through continuous monitoring of metabolic and targeted processes of SHP1 inhibitors in real-time, we can evaluate the effectiveness and toxicity of the inhibitors, further optimize drug design, and explore SHP1 biology. Indoloquinoxaline is an important class of N-containing heterocycle, which has been studied and applied in the pharmacological field and in optoelectronic materials.
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December 2024
Chemistry Department, Faculty of Science, Ain Shams University, Cairo 11566, Egypt. Electronic address:
A new series of benzo[h]quinoline-containing heterocycles was synthesized via reactions of benzo[h]quinolinyl-2(3H)-furanone with some nitrogen bidentate nucleophiles, leading to the formation of pyridazinone, pyrrolinone, benzimidazole, and benzoxazinone derivatives. The synthesized compounds were evaluated for their insecticidal activity against Culex pipiens L. larvae.
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