Discovery of a Highly Potent, Orally Active mitosis/angiogenesis Inhibitor r1530 for the Treatment of Solid Tumors

Jin-Jun Liu, Brian Higgins, Grace Ju, Kenneth Kolinsky, Kin-Chun Luk, Kathryn Packman, Giacomo Pizzolato, Yi Ren, Kshitij Thakkar, Christian Tovar, Zhuming Zhang, Peter M Wovkulich

ACS Med Chem Lett. 2013 Jan 15;4(2):259-63.

PMID: 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.

Chemicals Related in the Paper:

Catalog Number	Product Name	Structure	CAS Number	Price
AP882531875	R1530		882531-87-5	Price