No abstract

No abstract

No abstract

Terpenes U 0200Synthesis of 10-Substituted Triazolyl Artemisinins Possessing Anticancer Activity via Huisgen 1,3-Dipolar Cycloaddition. -The cyclic hemiacetal functionality at the C-10 position of dihydroartemisinin (I) is regarded as a sugar-anomeric center being able to form a carbon-nitrogen glycoside bond. A separable mixture of diastereomeric azidoartemisinins is obtained by reacting (I) with sodium azide. The cycloaddition reaction of (II) is successfully carried out in a co-solvent system, but in the case of (III) and (IV) it is not as effective as expected. The triazolylartemisinins (VI) exhibit strong growth-inhibition activity against various cancer cell lines, even at sub-micromolar concentrations; especially (VIb) and (VIc) display a highly strong cytotoxicity. -(CHO, S.; OH, S.; UM, Y.; JUNG, J.-H.; HAM, J.; SHIN*, W.-S.; LEE, S.; Bioorg.