Potent, Orally Active Heterocycle-Based ... - ACS Publications

Laura Gherke, R. Bruce Credo, Yu-Hua Hui, Kennan Marsh, Robert Warner, Jang Y. Lee, Nicolette Zielinski-Mozng, David Frost, Saul H. Rosenberg, and...
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4946

J. Med. Chem. 2002, 45, 4946

Additions and Corrections

2002, Volume 45

Le Wang,* Keith W. Woods, Qun Li, Kenneth J. Barr, Richard W. McCroskey, Steven M. Hannick, Laura Gherke, R. Bruce Credo, Yu-Hua Hui, Kennan Marsh, Robert Warner, Jang Y. Lee, Nicolette Zielinski-Mozng, David Frost, Saul H. Rosenberg, and Hing L. Sham: Potent, Orally Active Heterocycle-Based Combretastatin A-4 Analogues: Synthesis, Structure-Activity Relationship, Pharmacokinetics, and In Vivo Antitumor Activity Evaluation. Page 1704. Table 4 and Figure 3 contained some errors. In Table 4, all four “mg” units in the column head should be “µg” and there should be a center dot in the unit “µg‚h/mL” for AUC. In Figure 3, the compound listed in the inset should be 25f. The following are the corrected table and figure. Table 4. Pharmacokinetic Studies in Dog, Monkey, and Mouse on Compounds 24h and 25fa 24h Cmax AUC (PO) (µg/mL) (µg‚h/mL) dog monkey mouse

1.87 0.354 0.25

7.05 0.98 0.82

25f F (%) 44.5 12.5 24.2

Cmax AUC (PO) (µg/mL) (µg‚h/mL) 4.15 9.68 5.52

9.65 43.98 3.82

F (%) 45.8 91.2 89.7

a Two animals used for each dosing group (oral and iv, 5 mg/ kg); the PK parameters reported here were the average of two animals.

Figure 3. Regression trial of 25f against murine M5076 reticulum sarcoma cell line.

JM020332+ 10.1021/jm020332+ Published on Web 09/19/2002