Zhang Wei-Ge, Zhao Rui, Ren Jian, Ren Li-Xiang, Lin Jin-Guang, Liu Dai-Lin, Wu Ying-Liang, Yao Xin-Sheng
School of Pharmaceutical Engineering, Shenyang Pharmaceutical University, Shenyang, PR China.
Arch Pharm (Weinheim). 2007 May;340(5):244-50. doi: 10.1002/ardp.200600146.
A total synthetic route for two natural dihydrostilbenes with significant cytotoxicity toward human cancer cell lines, (3-(2-(7-methoxybenzo[d][1,3]dioxol-5-yl)ethyl)phenol 1a and 6-(3-hydroxyphenethyl)benzo[d][1,3]dioxol-4-ol 1b), which were isolated from Bulbophyllum odoratissimum Lindl, was developed via Wittig-Horner reaction. The natural products 1a and 1b were obtained in 28% and 20% overall yield, respectively. Additionally, nine analogues, 1c-1k, of the two natural dihydrostilbenes were synthesized and evaluated for their anti-proliferative activity against human SGC-7901, KB and HT-1080 cell lines by MTT assay. The activities of 1c and 1d were in the same range as those of the natural products 1a and 1b.
从芳香石豆兰（Bulbophyllum odoratissimum Lindl）中分离得到了两种对人癌细胞系具有显著细胞毒性的天然二氢茋类化合物，即3-(2-(7-甲氧基苯并[d][1,3]二氧杂环戊烯-5-基)乙基)苯酚1a和6-(3-羟基苯乙基)苯并[d][1,3]二氧杂环戊烯-4-醇1b，通过维蒂希-霍纳尔反应开发了它们的全合成路线。天然产物1a和1b的总收率分别为28%和20%。此外，合成了这两种天然二氢茋类化合物的九个类似物1c-1k，并通过MTT法评估了它们对人SGC-7901、KB和HT-1080细胞系的抗增殖活性。1c和1d的活性与天然产物1a和1b的活性在同一范围内。
