Angiogenesis inhibitors identified by cell-based high-throughput screening: Synthesis, structure-activity relationships and biological evaluation of 3-[(E)-styryl]benzamides that specifically inhibit endothelial cell proliferation
Proliferation of endothelial cells is critical for angiogenesis. We report orally available, in vivo active antiangiogenic agents which specifically inhibit endothelial cell proliferation. After identifying human umbilical vein endothelial cell (HUVEC) pr
The P1 N-isopropyl motif bearing hydroxyethylene dipeptide isostere analogues of aliskiren are in vitro potent inhibitors of the human aspartyl protease renin
Novel nonpeptide small molecule renin inhibitors bearing an N-isopropyl P1 motif were designed based on initial lead structures 1 and aliskiren (2). (P3-P1)-Benzamide derivatives such as 9a and 34, as well as the corresponding P1 basic tertiary amine derivatives 10 and 35 were found to display low nanomolar inhibition against human renin in vitro.
Yamaguchi, Yasuchika,Menear, Keith,Cohen, Nissim-Claude,Mah, Robert,Cumin, Frédéric,Schnell, Christian,Wood, Jeanette M.,Maibaum, Jürgen
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p. 4863 - 4867
(2010/05/18)
BENZAMIDE DERIVATIVE
To provide compounds which have high angiogenesis inhibiting activity, and are useful as agents for effective treatment and prevention of diseases involving pathologic angiogenesis, for example, cancer and cancer metastasis, methods for producing the comp
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Page/Page column 40-41
(2010/11/23)
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