新型3-乙酰桦木醇和桦木酮三唑类化合物作为抗癌剂
Novel triazoles of 3-acetylbetulin and betulone as anticancer agents.
作者信息
Bębenek Ewa, Kadela-Tomanek Monika, Chrobak Elwira, Latocha Małgorzata, Boryczka Stanisław
机构信息
1Department of Organic Chemistry, School of Pharmacy with the Division of Laboratory Medicine in Sosnowiec, Medical University of Silesia in Katowice, 4 Jagiellońska Str., 41-200 Sosnowiec, Poland.
2Department of Cell Biology, School of Pharmacy with the Division of Laboratory Medicine in Sosnowiec, Medical University of Silesia in Katowice, 8 Jedności Str., 41-200 Sosnowiec, Poland.
出版信息
Med Chem Res. 2018;27(9):2051-2061. doi: 10.1007/s00044-018-2213-x. Epub 2018 Jul 17.
The CuAAC reaction of azides and acetylenic triterpenes was used for synthesis of new triazoles of 3-acetylbetulin and betulone. The triazole derivatives were evaluated for their anticancer activity in vitro against amelanotic melanoma C-32, ductal carcinoma T47D and glioblastoma SNB-19 cell lines. 28-[1-(3'-Deoxythymidine-5'-yl)-1-1,2,3-triazol-4-yl]carbonylbetulone exhibited a significant IC value (0.17 µM) against the human glioblastoma SNB-19 cell line, an almost 5-fold higher potency while compared with reference cisplatin.
叠氮化物与炔基三萜的铜催化叠氮化物-炔烃环加成反应（CuAAC反应）被用于合成新的3-乙酰桦木醇和桦木酮三唑类化合物。对这些三唑衍生物针对无黑色素黑素瘤C-32、导管癌T47D和成胶质细胞瘤SNB-19细胞系的体外抗癌活性进行了评估。28-[1-(3'-脱氧胸苷-5'-基)-1,2,3-三唑-4-基]羰基桦木酮对人成胶质细胞瘤SNB-19细胞系表现出显著的半数抑制浓度（IC）值（0.17 µM），与参比顺铂相比，其效力高出近5倍。
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