Antitumor agents 287. Substituted 4-amino-2H-pyran-2-one (APO) analogs reveal a new scaffold from neo-tanshinlactone with in vitro anticancer activity

作者：Dong Yizhou; Nakagawa Goto Kyoko; Lai Chin Yu; Morris Natschke Susan L; Bastow Kenneth F; Lee Kuo Hsiung^*

来源：Bioorganic & Medicinal Chemistry Letters, 2011, 21(8): 2341-2344.

DOI：10.1016/j.bmcl.2011.02.084

• 4-Amino-2H-pyran-2-one (APO) analogs
• Neo-tanshinlactone
• Cytotoxicity

4-Amino-2H-benzo[h] chromen-2-one (ABO) and 4-amino-7,8,9,10-tetrahydro-2H-benzo[h] 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 ED(50) values of 0.059-0.090 mu M.

• 出版日期2011-4-15
• 单位中国医科大学