Compounds containing quinoline moiety are well known due to their broad biological activities. A number of them have been widely investigated and clinically used as antifungal or antibacterial agents [1, 2]. Quinoline derivatives have gained strong attention recently due to their activity as perspective HIV integrase inhibitors [3]. Recently, some quinoline-based compounds have been synthesized and reported as potent antitumor agents by our research team [4]. Anti-proliferative activity of the synthesized compounds was tested by the MTS assay against the human colon adenocarcinoma cell lines with normal expression of p53 protein (Hct116 p53+/+) and mutants with disabled TP53 gene (Hct116 p53-/-). The compounds were also tested for their cytotoxicity against mouse melanoma cell line B16-F10 and nontumor cell line NHDF. Anti-proliferative activity of quinoline derivatives was determined. Compound (Figure 1) demonstrated the highest anti-proliferative activity (IC₅₀=1,40µM). The most active compound makes it promising for further development.

Figure 1. Chemical structure 8-hydroxy-N'-(2-hydroxybenzoyl)-2-methylquinoline-7-carbohydrazide.

References:

[1] Musiol R., et al., Bioorganic Medicinal Chemistry, 2006, 14, 3592-3598.

[2] Palit P., et al., European Journal of Medicinal Chemistry, 2009, 44, 845-853.

[3] Zouhiri F., et al., Tetrahedron Letters, 2005, 46, 2201-2205.

[4] Musiol R., et al.,Bioorganic Medicinal Chemistry, 2007, 15, 1280-1288.

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