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Design and synthesis of cyclic urea compounds: a pharmacological study for retinoidal activity
Masaaki Kurihara1, Abu Shara Shamsur Rouf, Hisao Kansui
1Division of Organic Chemistry, National Institute of Health Sciences, Kamiyoga, Setagaya-ku, Tokyo 158-8501, Japan. masaaki@nihs.go.jp
Abstract:
Retinoids are natural and synthetic analogues of all-trans retinoic acid (ATRA). Cancer and other serious hyperproliferative diseases are attractive therapeutic targets for retinoids. We report here the design and synthesis of novel cyclic urea compounds with retinoidal activity. YR105 exhibited potent differentiation-inducing ability toward human promyelocytic leukemia HL-60 cells at the concentration of 10(-9)M: its potency was almost equal to that of the native ligand, all-trans retinoic acid.
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