Figure 1.
Artemisinin structure and activity. A) Structures of artemisinin monomer NSC 369397 (1), artemisinin dimers NSC 724910 (2), NSC 735847 (3), and deoxy-derivative of NSC 735847 (NSC 735847DX) (4). B) Activity of artemisinin monomer and dimers. PC-3 cells were incubated with NSC 369397 (A), NSC 724910 (B) or NSC 735847 (C) for 48 h before viability was determined. C) Activity of monomer and dimers in a panel of tumor cell lines following 48 h of exposure. IC50 was defined as the concentration of drug required to inhibit [14C]-leucine incorporation by 50% relative to control-treated cells. D) The importance of the endoperoxide bridge on dimer activity. HL-60 cells (triangles) or PC-3 cells (circles) were incubated for 24 h with either NSC 735847 or NSC 735847DX before protein synthesis was determined. HL-60 cells, NSC 735847 (D), NSC 735847DX (A); PC-3 cells, NSC 735847 (C), NSC 735847DX (B). [14C]-leucine cell viability assays were performed at least twice with triplicate determinations for each point and the data pooled.