2. Academic Validation
  3. (6,7-Dimethoxy-2,4-dihydroindeno[1,2-c]pyrazol-3-yl)phenylamines: platelet-derived growth factor receptor tyrosine kinase inhibitors with broad antiproliferative activity against tumor cells

(6,7-Dimethoxy-2,4-dihydroindeno[1,2-c]pyrazol-3-yl)phenylamines: platelet-derived growth factor receptor tyrosine kinase inhibitors with broad antiproliferative activity against tumor cells

  • J Med Chem. 2005 Dec 29;48(26):8163-73. doi: 10.1021/jm050680m.
Chih Y Ho 1,  Donald W Ludovici,  Umar S M Maharoof,  Jay Mei,  Jan L Sechler,  Robert W Tuman,  Eric D Strobel,  Laura Andraka,  Hwa-Kwo Yen,  Gregory Leo,  Jian Li,  Harold Almond,  Hong Lu,  Ann DeVine,  Rose M Tominovich,  Judith Baker,  Stuart Emanuel,  Robert H Gruninger,  Steven A Middleton,  Dana L Johnson,  Robert A Galemmo Jr
Affiliations

Affiliation

  • 1 Johnson & Johnson Pharmaceutical Research and Development, L.L.C., Spring House Research and Early Development Site, Spring House, Pennsylvania 19477, USA.
PMID: 16366598 DOI: 10.1021/jm050680m
Abstract

A series of (6,7-dimethoxy-2,4-dihydroindeno[1,2-c]pyrazol-3-yl)phenylamines has been optimized to preserve both potent kinase inhibition activity against the angiogenesis target, the receptor tyrosine kinase of Platelet-Derived Growth Factor-BB (PDGF-BB), and to improve the broad tumor cell antiproliferative activity of these compounds. This series culminates in the discovery of 17 (JNJ-10198409), a compound with anti-PDGFR-beta kinase activity (IC(50)=0.0042 microM) and potent antiproliferative activity in six of eight human tumor cell lines (IC(50) < 0.033 microM).

Figures
Products
  • Cat. No.
    Product Name
    Description
    Target
    Research Area
  • HY-W011266
    99.57%, PDGFR Inhibitor