Antiproliferative activity of (R)-4'-methylklavuzon on hepatocellular carcinoma cells and EpCAM/CD133 cancer stem cells via SIRT1 and Exportin-1 (CRM1) inhibition.

Cytotoxic effects of (R)-4'-methylklavuzon were investigated on hepatocellular carcinoma cells (HuH-7 and HepG2) and HuH-7 EpCAM/CD133 cancer stem cells. IC of (R)-4'-methylklavuzon was found as 1.25 μM for HuH-7 parental cells while it was found as 2.

CRM1 inhibitory and antiproliferative activities of novel 4'-alkyl substituted klavuzon derivatives.

Klavuzons are 6-(naphthalen-1-yl) substituted 5,6-dihydro-2H-pyran-2-one derivatives showing promising antiproliferative activities in variety of cancer cell lines. In this work, racemic syntheses of nine novel 4'-alkyl substituted klavuzon derivatives were completed in eight steps and anticancer properties of these compounds were evaluated. It is found that size of the substituent has dramatic effect over the potency and selectivity of the cytotoxic activity in cancerous and healthy pancreatic cell lines.