Picolyl amides of betulinic acid as antitumor agents causing tumor cell apoptosis.
作者： Uladzimir Bildziukevich , Lucie Rárová , David Šaman , Zdeněk Wimmer
DOI: 10.1016/J.EJMECH.2017.12.096
关键词:
摘要: Abstract A series of picolyl amides betulinic acid (3a–3c and 6a–6c) was prepared subjected to the cytotoxicity screening tests. Structure-activity relationships studies resulted in finding differences biological activity dependence on o-, m- p-substitution pyridine ring target amides, when data 3a–3c 6a–6c were obtained compared. The 3b 3a displayed (given IC50 values) G-361 (0.5 ± 0.1 μM 2.4 ± 0.0 μM, respectively), MCF7 (1.4 ± 0.1 μM 2.2 ± 0.2 μM, HeLa (2.4 ± 0.4 μM 2.3 ± 0.5 μM, respectively) CEM (6.5 ± 1.5 μM 6.9 ± 0.4 μM, tumor cell lines, showed weak effect normal human fibroblasts (BJ). Selectivity against all tested cancer cells determined compared with therapeutic index (TI) between 7 100 for compounds 3b. (TI = 100) calculated malignant melanoma line (G-361) versus other (3c revealed lower effects than lines.
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