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A series of 1,2,3-triazole tethered dihydroartemisinin-isatin hybrids 8a-c and 9a-k were designed and synthesized. Their antiproliferative activity against A549, doxorubicin-resistant A549 (A549/DOX) as well as cisplatin-resistant A549 (A549/DDP) lung cancer cell lines was also investigated in this study. All hybrids (half maximal inhibitory concentration/IC 50 : 7.54–73.8  μ M) were more potent than the parent drug dihydroartemisinin (IC 50 : 69.4–88.0  μ M) and also non-cytotoxic towards mouse embryonic fibroblast cells NIH/3T3 (IC 50 : &amp;gt;100  μ M). The structure-activity relationships illustrated that the substituents on C-3 and C-5 position of isatin moiety influenced the activity significantly. Imine at C-3 position decreased the activity, whereas fluoro at C-5 position enhanced the activity. In particular, hybrids 8a,c (IC 50 : 7.54–12.1  μ M) and 9i (IC 50 : 9.10–15.9  μ M) were comparable to cisplatin (IC 50 : 7.54–15.9  μ M  vs  9.38–19.7  μ M) against A549 and A549/DOX, but 4.6–7.6 folds more potent than that of cisplatin (IC 50 : 8.77–14.3  μ M  vs  66.9  μ M) against A549/DDP cells. Moreover, hybrids 8a,c exhibited excellent stability (liver microsomes: 68–83%) in mouse/human microsomes and good pharmacokinetic properties, demonstrating their potential as a novel anti-lung cancer chemotherapeutic candidates.

Design, Synthesis and Anti-Lung Cancer Evaluation of 1, 2, 3-Triazole Tethered Dihydroartemisinin-Isatin Hybrids