New lithocholic and chenodeoxycholic piperazinylcarboxamides with antiproliferative and pro-apoptotic effects on human cancer cell lines.
作者： Laïla El Kihel , Monique Clément , Marc-Antoine Bazin , Géraldine Descamps , Mohamed Khalid
DOI: 10.1016/J.BMC.2008.07.046
关键词:
摘要: Six new synthetic bile acid derivatives were synthesized and tested in vitro against various human cancer cells (glioblastoma multiforme (GBM), multiple myeloma (KMS-11), and colonic carcinoma (HCT-116) cell lines. The best activity was obtained with compound IIIb on multiple myeloma cells (LD50: 8.5±0.5 μM). This activity was associated with Mcl-1 and PARP-1 cleavage, inhibition of NFκB signaling, and DNA fragmentation, demonstrating an apoptotic cell death signaling pathway.
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