我們之前合成出一系列含有3,4-取代-1-芳香基-3-己烯-1,5-雙炔基團之新烯雙炔化合物,作為拓譜酶的抑制劑。而且我們利用不同之芳香連接基團來聯結此具有”彈頭”作用的烯雙炔系統與具”導引” 作用的的雌性素,藉以形成能直接攻擊與性激素有關之腫瘤細胞的新型標靶抗癌藥物,利用此類藥物治療,猶如擊靶一般,效果顯著,同時因有選擇性機制,故往往對正常細胞副作用輕微。另外,我們將上述抗癌化合物進行一系列的生物性評估,其包括:化合物細胞毒性的篩選,其對癌細胞生長週期的影響,其與雌性素接受器結合狀況的測試與鑑定。以期開發出具有低副作用,強效且對於生長狀況與性激素相關的各式腫瘤有高度特異性的新型抗癌藥物。
We had synthesized a series of novel enediynes , which contained 3,4-disubstituted-1-aryl-3-hexen-1,5-diynes subdomains act as topoisomerase inhibitors. Compounds combining these enediyne system with estrogen through using various aryl linkers were generated to pass through the bioelavation course, which includes cytotxic screen, cell cycle assay, identification of estrogen receptor binding . We want to obtain novel antitumor agents with lower toxicities (or side effect), greater potency and specific target-directed function towards those cancer cell lines with estrogen receptors.