738. Aplidine

Description and references

Cyclic depsipeptide analog of the didemnins, q.v., isolated from the marine tunicate, Aplidum albicans. Induces rapid apoptotic death with or without previous cell cycle arrest. Isoln and synthesis: K. Rinehart, A. M. Lithgow-Bertelloni, WO 9104985 (1991 to PharmaMar); G. Jou et al., J. Org. Chem. 62, 354 (1997). Antiproliferative effects on Ehrlich carcinoma: J. L. Urdiales et al., Cancer Lett. 102, 31 (1996); cytotoxic effect on acute lymphoblastic leukemia cells: E. Erba et al., Br. J. Cancer 89, 763 (2003). Mechanism of action study: idem et al., ibid. 86, 1510 (2002). Degradation kinetics in solution: J. C. M. Waterval et al., J. Chromatogr. B 754, 161 (2001). 2D-NMR conformational analysis in solution: F. Cárdenas et al., J. Org. Chem. 68, 9554 (2003). LC/MS/MS determn in plasma: J. Yin et al., Rapid Commun. Mass Spectrom. 17, 1909 (2003). In vitro toxicity on hematopoietic progenitors and stem cells: S. G. Gomez et al., Exp. Hematol. 31, 1104 (2003). Clinical pharmacokinetics and evaluation in advanced malignancies: S. Faivre et al., J. Clin. Oncol. 23, 7871 (2005).

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