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已报道,天然棒麦角素(Clavines)及其衍生物具有抑制L5178y 小鼠淋巴肉瘤细胞生长的活性。本文报道,天然产物Festuclavine(1)及其半合成衍生物(2～10)在体外抗L5178y 小鼠淋巴肉瘤细胞生长活性的结果(图1),以及festuclavine 的构-效关系。(一)C-8甲基对festuclavine 的抑瘤活性至关重要,因具有C-8甲基的agroclavine 亦有抑瘤活性;而C-8羟甲基的elymoclavine、lysergol 和二氢lysergol
It has been reported that natural clavines and their derivatives have the activity of inhibiting the growth of L5178y mouse lymphosarcoma cells. We report here the results of the growth activity of the natural product Festuclavine (1) and its semisynthetic derivatives (2 ~ 10) in anti-L5178y mouse lymphosarcoma cells (Figure 1) and the structure-activity relationship of festuclavine. (A) C-8 methyl is essential for the antitumor activity of festuclavine due to the antitumor activity of agroclavine with C-8 methyl; while the C-8 hydroxymethyl elymoclavine, lysergol and dihydro lysergol