Synthesis and biological evaluation of taxinine analogues as orally active multidrug resistance reversal agents in cancer

Add time:09/04/2019    Source:sciencedirect.com

Three novel taxinine analogues were prepared and tested for their activity as multidrug resistance (MDR) reversal agents in comparison with verapamil. In vitro testing demonstrated that compounds 8–10 possess MDR-reversal activity in the KB/V cell line. Half-hour after treatment with 5, 10, and 20 μmol/L compound 9, the intracellular rhodamine123 concentration increased 2.3, 2.9, and 3.2-fold, respectively, higher than 1.88-fold of 10 μmol/L verapamil in KB/V cell line. In vivo studies with VCR-resistant KB/V tumor xenografts showed that compound 9 in combination with VCR significantly inhibited tumor growth. Treatment with VCR or 9 alone did not result in growth inhibition. These results reveal that three taxinine analogues are good modifiers of MDR in tumor cells.

We also recommend Trading Suppliers and Manufacturers of Taxinine B (cas 18457-44-8). Pls Click Website Link as below: cas 18457-44-8 suppliers

Prev:Novel Dimeric Taxoids via Highly Regio- and Stereospecific Diels–Alder Cycloadditions of Taxinine B (cas 18457-44-8) and Taxicine I Derivatives
Next:Original articleIn vitro and in vivo anticancer activity of 2-deacetoxytaxinine J and synthesis of novel taxoids and their in vitro anticancer activity☆)