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Discovery of a highly potent, orally active mitosis/angiogenesis inhibitor r1530 for the treatment of solid tumors.

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.

SUBMITTER: Liu JJ

PROVIDER: S-EPMC4027509 | biostudies-literature | 2013 Feb

REPOSITORIES: biostudies-literature

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Discovery of a highly potent, orally active mitosis/angiogenesis inhibitor r1530 for the treatment of solid tumors.

Liu Jin-Jun JJ Higgins Brian B Ju Grace G Kolinsky Kenneth K Luk Kin-Chun KC Packman Kathryn K Pizzolato Giacomo G Ren Yi Y Thakkar Kshitij K Tovar Christian C Zhang Zhuming Z Wovkulich Peter M PM

ACS medicinal chemistry letters 20130115 2

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. ...[more]

PMID: 24900658

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