Geirsson Jon K F, Jonsson Stefan, Valgeirsson Jon
Science Institute, University of Iceland, Dunhaga 3, IS-107 Reykjavik, Iceland.
Bioorg Med Chem. 2004 Nov 1;12(21):5563-9. doi: 10.1016/j.bmc.2004.08.006.
Various novel bicyclo[3.3.1.]nonenol derivatives were synthesized in an efficient one-pot procedure in a remarkably stereoselective reaction. The title compounds show significant antitumor activity against human cancer cell lines. A variety of cinnamic acid derivatives were linked to the title compounds as side chains in order to enhance the antitumor activity. These compounds were subjected to the in vitro antitumor screening, and the results are discussed. It seems important with respect to antitumor activity to locate an aromatic ring at the C-7 position of the bicyclo[3.3.1]nonane framework.
通过高效的一锅法在显著的立体选择性反应中合成了各种新型双环[3.3.1]壬烯醇衍生物。标题化合物对人类癌细胞系显示出显著的抗肿瘤活性。为了增强抗肿瘤活性，将多种肉桂酸衍生物作为侧链连接到标题化合物上。对这些化合物进行了体外抗肿瘤筛选，并对结果进行了讨论。对于抗肿瘤活性而言，在双环[3.3.1]壬烷骨架的C-7位上定位一个芳环似乎很重要。
