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Antitumor agents 287. Substituted 4-amino-2H-pyran-2-one (APO) analogs reveal a new scaffold from neo-tanshinlactone with in vitro anticancer activity
Authors:Dong Yizhou  Nakagawa-Goto Kyoko  Lai Chin-Yu  Morris-Natschke Susan L  Bastow Kenneth F  Lee Kuo-Hsiung
Institution:a Natural Products Research Laboratories, UNC Eshelman School of Pharmacy, University of North Carolina, Chapel Hill, NC 27599-7568, USA
b Division of Medicinal Chemistry and Natural Products, UNC Eshelman School of Pharmacy, University of North Carolina, Chapel Hill, NC 27599-7568, USA
c Chinese Medicine Research and Development Center, China Medical University and Hospital, Taichung, Taiwan
Abstract:4-Amino-2H-benzoh]chromen-2-one (ABO) and 4-amino-7,8,9,10-tetrahydro-2H-benzoh]chromen-2-one (ATBO) analogs were found to be significant in vitro anticancer agents in our previous research. Our continuing study has now discovered a new simplified (monocyclic rather than tricyclic) class of cytotoxic agents, 4-amino-2H-pyran-2-one (APO) analogs. By incorporating various substituents on the pyranone ring, we have established preliminary structure-activity relationships (SAR). Analogs 19, 20, 23, and 26-30 displayed significant tumor cell growth inhibitory activity in vitro. The most active compound 27 exhibited ED50 values of 0.059-0.090 μM.
Keywords:4-Amino-2H-pyran-2-one (APO) analogs  Neo-tanshinlactone  Cytotoxicity
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