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

Antitumor agents 278. 4-Amino-2H-benzo[h]chromen-2-one (ABO) analogs as potent in vitro anti-cancer agents.
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DOI:
10.1016/j.bmcl.2010.05.079
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发表时间:
2010-07-15
影响因子:
2.7
通讯作者:
Lee, Kuo-Hsiung
Lee, Kuo-Hsiung
中科院分区:
医学4区
文献类型:
--
作者:
Dong, Yizhou;Nakagawa-Goto, Kyoko;Lai, Chin-Yu;Morris-Natschke, Susan L.;Bastow, Kenneth F.;Lee, Kuo-Hsiung

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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 ED50 values of 0.01-2.1 μM 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 ED50 values of 0.01-0.17 μM. Preliminary SAR results indicated that substitutions on nitrogen are critical to the antitumor potency.
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