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Monoterpenoid 계의 새로운 항암제 합성 및 In vitro 세포독성 평가
이민정(Min Jung Lee),백형근(Hyung Gun Baek),김대근(Dae Keun Kim),이강노(Kang Ro Lee),정규혁(Kyu Hyuk Chung),지옥표(Ok Pyo Zee),정영훈(Young Hoon Jung) 한국응용약물학회 2001 Biomolecules & Therapeutics(구 응용약물학회지) Vol.9 No.3
N/A Many attention has been focused on developing new chemotherapeutic agents for a treatment of cancer from natural products. From Carpesium divaricatum S. et Z. (Compositae), various monoterpenoid compounds were isolated and exhibited mild antitumor activity against human tumor cell lines. `These facts prompted us to explore the structure-activity relationship of these compounds. The synthesis of monoterpenoid compound was accomplished by Fries rearrangement, Grignard reaction, elimination, allylic oxidation, esterification and epoxidation as key steps. The results of in vitro cytotoxicity (A549, SK-OV-3, SK-MEL-2, XF498, HCT15) of the synthesised compounds are as follows: First of all, epoxide moiety is prerequisite for cytotoxic activity in diester compound. Any kind of compounds with olefin or diol moiety instead of epoxide ring exhibited poor or mild cytotoxic activity respectively. Of o-acetoxy and isobutoxy epoxy esters, p-substituted phenylacetate compounds exhibited high cytotoxic activities against SK-MEL-2 and HCT15.