Antitumor agents 278. 4-Amino-2H-benzo[h]chromen-2-one (ABO) analogs as potent in vitro anti-cancer agents |
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Authors: | Yizhou Dong Kyoko Nakagawa-Goto Chin-Yu Lai Susan L Morris-Natschke Kenneth F Bastow Kuo-Hsiung Lee |
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Institution: | 1. Natural Products Research Laboratories, Eshelman School of Pharmacy, University of North Carolina, Chapel Hill, NC 27599-7568, United States;2. Division of Medicinal Chemistry and Natural Products, Eshelman School of Pharmacy, University of North Carolina, Chapel Hill, NC 27599-7568, United States |
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Abstract: | 4-Amino-2H-benzoh]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 0.01–5.8 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 0.01–76 μM. Preliminary SAR results indicated that substitutions on nitrogen are critical to the antitumor potency. |
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