Synthesis and cytotoxic activity of MOM-ether analogs of isosteviol

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• 作者：Ahmed Malki ; Rumita Laha ; Stephen C. Bergmeier
• 关键词：XOGHKSPSZUMWSW-DLVPKPCGSA-N ; MBEXDVODIOJSHS-OVWDBLRBSA-N ; SHKJSFWJVKXKMC-WTTUNBIBSA-N ; JXBMAQPSDYYPJG-LHAFMROOSA-N ; DGGPEEYHUQAZIT-SIQVWGOZSA-N ; ZCMULAIBYWUMFO-LFJMRGCMSA-N ; IOMQVFBKFJIBDB-SIQVWGOZSA-N ; DMXYKZDFNHUYNQ-WTTUNBIBSA-N ; YADQWCRDIBHUGG-SMMOOYLESA-N ; QICUIWNDRCCPFH-LFJMRGCMSA-N ; UEWBUUFUGYUSHO-SMMOOYLESA-N ; OJGDDOLCFMFPJR-SIQVWGOZSA-N
• 刊名：Bioorganic and Medicinal Chemistry Letters
• 出版年：15 February, 2014
• 年：2014
• 卷：24
• 期：4
• 页码：1184-1187
• 全文大小：707 K

文摘

Lung cancer is one of the most common malignancies worldwide. In this Letter, novel MOM-ether analogs of isosteviol were designed and synthesized to be tested for anticancer activities against H1299 lung cancer cell lines. The effects of these derivatives were studied in H1299 human large cell lung carcinoma cells that are null for p53 and compared to normal counterparts NL-20 normal lung epithelial cells. The initial screening of twelve MOM-ether analogs of isosteviol derivatives on H1299 lung cancer cells by MTT assay revealed that two derivatives (an ester and a carbamate) were the most potent in reducing cell viability. The IC₅₀ values for these derivatives were determined to be 14 and 21 渭M respectively. We compared the cytotoxicity of the best derivatives in H1299 lung cancer cells and NL-20 normal lung epithelial cells. Both derivatives showed lower cytotoxic effects on NL-20 normal lung epithelial cells. Moreover, both derivatives induced apoptosis in H1299 lung cancer cells more than NL-20 normal lung epithelial cells.