| Autor: |
Tsepaeva, Olga V., Nemtarev, Andrey V., Abdullin, Timur I., Grigor’eva, Leysan R., Kuznetsova, Elena V., Akhmadishina, Rezeda A., Ziganshina, Liliya E., Cong, Hanh H., Mironov, Vladimir F. |
| Zdroj: |
Journal of Natural Products; 20240101, Issue: Preprints |
| Abstrakt: |
A series of new triphenylphosphonium (TPP) derivatives of the triterpenoid betulin (1, 3-lup-20(29)-ene-3β,28-diol) have been synthesized and evaluated for cytotoxic effects against human breast cancer (MCF-7), prostate adenocarcinoma (PC-3), vinblastine-resistant human breast cancer (MCF-7/Vinb), and human skin fibroblast (HSF) cells. The TPP moiety was applied as a carrier group through the acyl linker at the 28- or 3- and 28-positions of betulin to promote cellular and mitochondrial accumulation of the resultant compounds. A structure–activity relationship study has revealed the essential role of the TPP group in the biological properties of the betulin derivatives produced. The present results showed that a conjugate of betulin with TPP (3) enhanced antiproliferative activity toward vinblastine-resistant MCF-7 cells, with an IC50value as low as 0.045 μM. |
| Databáze: |
Supplemental Index |
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