Synthesis of 10β-Substituted Triazolyl Artemisinins and Their Growth Inhibitory Activity against Various Cancer Cells

Antitumor Activity of Artemisinin and Its Derivatives: From a Well-Known Antimalarial Agent to a Potential Anticancer Drug

“…Considerable progress has been made in the design of novel compounds with enhanced potency at the nanomolar range, increased selectivity, and low toxicity in vitro . It has been reported that triazolyl substituted artemisinins-induced significant growth inhibitory effect [ 127 ]. Independent of stereo- or region-chemistry, strong inhibition was influenced by the functional group attached to the triazole ring.…”

“…Independent of stereo- or region-chemistry, strong inhibition was influenced by the functional group attached to the triazole ring. Substituted compounds with a penthyl benzene group showed the highest antiproliferative activity ranging from 0.07 to 0.39 μ M 72 h IC 50 in 6 cancer lines [ 127 ]. Recently, Feng et al synthesized a series of dihydroartemisinin derivatives via an aza-Michael addition reaction with high selectivity index and IC 50 in the nanomolar range against HeLa cells (0.37 μ M) [ 128 ].…”

Synthesis of novel artemisinin–triazole hybrids

“…[7] Recent years, modifications of the parent structure of artemisinin could produce potentially important derivatives, which were found to be more biologically effective than the staring one. [4,5,[8][9][10][11][12][13] . Previous studies already indicated that the incorporation of artemisinin and triazole moeity gave hybrid compounds with improved cytotoxic activity, compared to the individual parent compounds [5,[10][11][12] .…”

“…[4,5,[8][9][10][11][12][13] . Previous studies already indicated that the incorporation of artemisinin and triazole moeity gave hybrid compounds with improved cytotoxic activity, compared to the individual parent compounds [5,[10][11][12] . In continuation of our interest in pharmacophore hybridization,herein we reported the hybridization of artemisinin containing the propan-2-ol unit and triazole.…”

Antimalarial Activity of C-10 Substituted Triazolyl Artemisinin

“…However, when the ratio was changed to 1:3, compound 12 was obtained instead of 9. The stereochemistry of compounds (12a–12h) were different from that of compounds with the C-9 methyl group (9a–9h) [ 21 – 23 ]. By using the above 2 different reaction conditions, 32 novel artemisinin derivatives having a substituted triazole group were obtained.…”