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Evaluation of cholinesterase inhibitory activity and cytotoxicity of synthetic derivatives of di- and triterpene metabolites from Pinus silvestris and Dipterocarpus alatus resins
Medicinal Chemistry Research ( IF 2.6 ) Pub Date : 2020-05-31 , DOI: 10.1007/s00044-020-02566-9
Irina E. Smirnova , Oxana B. Kazakova , Anne Loesche , Sophie Hoenke , Rene Csuk

A series of hydroxy-, oximino-, lactame, arylidene, N-methylpiperazinyl amide, isoxazole, pyrimidine derivatives of dipterocarpol, quinopimaric, and dammarenolic acids were synthesized and evaluated for cholinesterase inhibitory activity and cytotoxicity. All of the compounds were weak inhibitors for the enzyme acetylcholinesterase while being no inhibitor for butyrylcholinesterase. Dihydroquinopimaric acid was cytotoxic especially for A375 and A2780 tumor cells while being significantly less cytotoxic for nonmalignant fibroblasts (NIH 3T3).


中文翻译:

樟子松和双翅类树脂对二萜和三萜代谢产物合成胆碱酯酶的抑制活性和细胞毒性的评价

合成了一系列的羟基,肟基,内酰胺,亚芳基,N-甲基哌嗪酰胺,异恶唑,二萜类嘧啶的嘧啶衍生物,喹啉酸和dammarenolic酸,并评估了其对胆碱酯酶的抑制活性和细胞毒性。所有化合物都是乙酰胆碱酯酶的弱抑制剂,而没有丁酰胆碱酯酶的抑制剂。二氢喹喔啉酸对A375和A2780肿瘤细胞具有细胞毒性,而对非恶性成纤维细胞(NIH 3T3)的细胞毒性则要小得多。
更新日期:2020-05-31
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