Five novel derivatives of N-(9,10-dihydro-9,10-dioxoanthracenyl)-1H-indole-2-carboxamide were synthesized and their lipid-lowering effects studied in hyperlipidemic rats. Fusion of the anthraquinone derivatives at high temperature with 5-indole-2-carbonyl chloride, followed by recrystallization from chloroform/methanol gave the desired compounds in excellent yields. Compounds 1 to 5 at a non-toxic dose (1 ml of 57 microM solutions) and bezafibrate as positive control were administered to rats that were hyperlipidemic due to treatment with Triton WR-1339. A decrease in the plasma levels of triglyceride (TG) and low-density lipoprotein-cholesterol (LDL-C) and an increase in the plasma level of high-density lipoprotein-cholesterol (HDL-C) were observed with compounds 1, 3, 4, and 5. Compounds 1, 4, and 5 significantly reduced total cholesterol (TC) levels as well. These compounds may provide agents for targeting dyslipidemia and cardiovascular disease.
The N-(benzoylphenyl)-1H-indole-2-carboxamide derivatives 1 -6 were synthesized, and the lipid-lowering effects of two of these novel compounds were studied using hyperlipidemic rats as an experimental model. Treatment of ethyl-1H-indole-2-carboxylate with aminobenzophenones in the presence of sodium ethoxide and DMF, followed by purifi cation using column chromatography, gave the target compounds in good yields. The tested animals were divided into control, hyperlipidemic, compounds 2-, 3-and bezafi brate-treated groups. At a dose of 15 mg/kg body weight, compounds 2, 3 and bezafi brate signifi cantly reduced the elevated plasma triglyceride levels after 7 and 24 h. Furthermore, the high-density lipoprotein-cholesterol levels were remarkably increased in all treated groups after 7 and 24 h compared to the hyperlipidemic control group. However, only compounds 2-and 3-treated groups obviously showed a signifi cant reduction in plasma total cholesterol levels after 24 h. It is therefore reasonable to assume that 2 and 3 may have a promising potential in the treatment of hyperlipidemia and coronary heart diseases.
Topoisomerase II (Top-II) is an essential therapeutic target in cancer treatment owing to its overexpression in a wide variety of cancerous cells, including colorectal and breast cancer. Significant efforts have been made to discover and develop competitive inhibitors of the Top-II enzyme as potential anticancer agents. Herein, molecular modeling was employed to identify a new series of furyl-2-carboxamide derivatives as potential anticancer agents. Compounds 3, 5, and 7 were synthesized and characterized with the aid of several spectroscopic techniques, such as FT-IR, NMR, and mass spectroscopy, as well as elemental analysis. The anticancer activity properties of compounds 3, 5, and 7 were evaluated in vitro using an MTT assay in a human colorectal HCT-116 cell line with different concentration dilutions. The results indicate that the anthraquinone compound 3 is 1.3-1.6 times more potent against human colon cancer HCT-116 cells than the pyridine and benzophenone compounds 7 and 5, respectively, which reveals the importance of the anthraquinone moiety in exerting the inhibitory activity of the compound. Our findings recommend that further optimization of this series would benefit colon cancer treatment.
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