Figure 9.
(a) Late-stage preparation and anticancer activity of C-7 analogs of lycoricidine (3). Cell viability was assessed after 72 h using the Alamar Blue assay, n ≥ 3, SEM for each measurement is in the Supporting Information. Doxorubicin (Dox) was used as a reference. (b) Preparation and activity of 7-aminopancratistatin 52. (c) Role of C-7 amine substituent on solubility. High throughput equilibrium solubility using miniaturized shake flask approach was used. Error is SEM, n ≥ 3. (d) Evaluation of metabolic stability of narciclasine (3) and its deuterated isotopologs (4-d5 and 4-d2). Stability was assessed in mouse liver microsomes. Compounds were incubated with microsomes for 3 h, and the percentage remaining was quantified relative to t0 using an internal standard. Error is SEM, n ≥ 2.