抗肿瘤药物 278. 4-氨基-2H-苯并[h]色烯-2-酮（ABO）类似物作为有效的体外抗癌剂。
Antitumor agents 278. 4-Amino-2H-benzo[h]chromen-2-one (ABO) analogs as potent in vitro anti-cancer agents.
机构信息
Natural Products Research Laboratories, Eshelman School of Pharmacy, University of North Carolina, Chapel Hill, NC 27599-7568, United States.
出版信息
Bioorg Med Chem Lett. 2010 Jul 15;20(14):4085-7. doi: 10.1016/j.bmcl.2010.05.079. Epub 2010 May 24.
Abstract
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 microM 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 microM. Preliminary SAR results indicated that substitutions on nitrogen are critical to the antitumor potency.
摘要
4-氨基-2H-苯并[h]色烯-2-酮（ABO）类似物被设计、合成并评估其细胞毒性活性。在所有 4-取代的 ABO 类似物中，环己基（12）、N-甲氧基-N-甲基乙酰胺（14）和各种芳基衍生物（15-25 和 27）对所有测试的肿瘤细胞系表现出有希望的细胞生长抑制活性，ED（50）值为 0.01-5.8 μM。4'-甲氧基苯基衍生物（18）和 3'-甲基苯基衍生物（24）对广泛的癌细胞系表现出最有效的抗肿瘤活性，ED（50）值为 0.01-76 μM。初步 SAR 结果表明，氮上的取代对于抗肿瘤活性至关重要。
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