Antitumor agents 278. 4-Amino-2H-benzo[h]chromen-2-one (ABO) analogs as potent in vitro anti-cancer agents

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, 2010, 20(14): 4085-4087.

DOI：10.1016/j.bmcl.2010.05.079

• 4-Amino-2H-benzo[h]chromen-2-one analogs (ABO)
• Cytotoxic activity
• Structure-activity relationships

4-Amino-2H-benzo[h]chromen-2-one (ABO) analogs were designed, synthesized, and evaluated for cytotoxic activity. Among all 4-substituted ABO analogs, cyclohexyl (12), N-methoxy-N-methylacetamide (14), and various aromatic derivatives (15-25 and 27) exhibited promising cell growth inhibitory activity with ED(50) values of 0.01-5.8 mu M against all tested tumor cell lines. The 4'-methoxyphenyl derivative (18) and 3'-methylphenyl derivative (24) showed the most potent antitumor activity against a broad range of cancer cell lines with ED(50) values of 0.01-76 mu M. Preliminary SAR results indicated that substitutions on nitrogen are critical to the antitumor potency.

• 出版日期2010-7-15