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Discovery of a highly potent, orally active mitosis/angiogenesis inhibitor r1530 for the treatment of solid tumors.
Liu, Jin-Jun; Higgins, Brian; Ju, Grace; Kolinsky, Kenneth; Luk, Kin-Chun; Packman, Kathryn; Pizzolato, Giacomo; Ren, Yi; Thakkar, Kshitij; Tovar, Christian; Zhang, Zhuming; Wovkulich, Peter M.
  • Liu JJ; Discovery Chemistry, Discovery Oncology, and Chemical Synthesis, Hoffmann-La Roche Inc. , 340 Kingsland Street, Nutley, New Jersey 07110, United States.
  • Higgins B; Discovery Chemistry, Discovery Oncology, and Chemical Synthesis, Hoffmann-La Roche Inc. , 340 Kingsland Street, Nutley, New Jersey 07110, United States.
  • Ju G; Discovery Chemistry, Discovery Oncology, and Chemical Synthesis, Hoffmann-La Roche Inc. , 340 Kingsland Street, Nutley, New Jersey 07110, United States.
  • Kolinsky K; Discovery Chemistry, Discovery Oncology, and Chemical Synthesis, Hoffmann-La Roche Inc. , 340 Kingsland Street, Nutley, New Jersey 07110, United States.
  • Luk KC; Discovery Chemistry, Discovery Oncology, and Chemical Synthesis, Hoffmann-La Roche Inc. , 340 Kingsland Street, Nutley, New Jersey 07110, United States.
  • Packman K; Discovery Chemistry, Discovery Oncology, and Chemical Synthesis, Hoffmann-La Roche Inc. , 340 Kingsland Street, Nutley, New Jersey 07110, United States.
  • Pizzolato G; Discovery Chemistry, Discovery Oncology, and Chemical Synthesis, Hoffmann-La Roche Inc. , 340 Kingsland Street, Nutley, New Jersey 07110, United States.
  • Ren Y; Discovery Chemistry, Discovery Oncology, and Chemical Synthesis, Hoffmann-La Roche Inc. , 340 Kingsland Street, Nutley, New Jersey 07110, United States.
  • Thakkar K; Discovery Chemistry, Discovery Oncology, and Chemical Synthesis, Hoffmann-La Roche Inc. , 340 Kingsland Street, Nutley, New Jersey 07110, United States.
  • Tovar C; Discovery Chemistry, Discovery Oncology, and Chemical Synthesis, Hoffmann-La Roche Inc. , 340 Kingsland Street, Nutley, New Jersey 07110, United States.
  • Zhang Z; Discovery Chemistry, Discovery Oncology, and Chemical Synthesis, Hoffmann-La Roche Inc. , 340 Kingsland Street, Nutley, New Jersey 07110, United States.
  • Wovkulich PM; Discovery Chemistry, Discovery Oncology, and Chemical Synthesis, Hoffmann-La Roche Inc. , 340 Kingsland Street, Nutley, New Jersey 07110, United States.
ACS Med Chem Lett ; 4(2): 259-63, 2013 Feb 14.
Article en En | MEDLINE | ID: mdl-24900658
ABSTRACT
A new series of 7,8-disubstituted pyrazolobenzodiazepines based on the lead compound 1 have been synthesized and evaluated for their effects on mitosis and angiogenesis. Described herein is the design, synthesis, SAR, and antitumor activity of these compounds leading to the identification of R1530, which was selected for clinical evaluation.
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Texto completo: 1 Banco de datos: MEDLINE Idioma: En Año: 2013 Tipo del documento: Article
Texto completo
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PubMed Links
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Texto completo: 1 Banco de datos: MEDLINE Idioma: En Año: 2013 Tipo del documento: Article