Q1 · MEDICINE
Article
Author: Beaulieu, Francis ; Bachand, Carol ; Lee, Frank Y. ; Saulnier, Mark G. ; Kramer, Robert ; Long, Byron H. ; Rose, William C. ; Stadnick, Linda K. ; Solomon, Carola ; Vyas, Dolatrai M. ; Stoffan, Karen M. ; Martel, Alain ; Zimmermann, Kurt ; Fairchild, Craig R. ; Langley, David R. ; Wright, John J. ; Mahler, Mikael ; Eummer, Jeffrey T. ; St. Laurent, Denis R. ; Ruediger, Edward ; Balasubramanian, Balu N. ; Frennesson, David B. ; Wong, Henry ; Naidu, B. Narasimhulu
A series of fluoroglycosylated fluoroindolocarbazoles was examined with respect to their topoisomerase I activity, cytotoxicity, and selectivity. The lead clinical candidate from this series, BMS-250749, displays broad spectrum antitumor activity superior to CPT-11 against some preclinical xenograft models, including curative antitumor activity against Lewis lung carcinoma.