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(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

Chih Y Ho, 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, etc.

J Med Chem. 2005 Dec 29;48(26):8163-73.

PMID: 16366598

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).

Chemicals Related in the Paper:

Catalog Number	Product Name	Structure	CAS Number	Price
AP627518405-A	JNJ-10198409		627518-40-5	Price

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