Abstract
Herein, a direct strategy to synthesize 3-(2-hydroxybenzoyl)-1-aza-anthraquinones with excellent efficiency, mild conditions, and benign functional group compatibility was reported. A variety of 3-formylchromone compounds were employed as compatible substrates and this protocol gave the 3-(2-hydroxybenzoyl)-1-aza-anthraquinone derivatives in good to excellent yields without inert gas and expensive transition metal catalysts. Some compounds displayed good anti-proliferative activities.
Highlights
Anthraquinone, as a classical pharmacophore, has been applied in drug discovery for many years, [1,2,3] and this scaffold contributes to a great number of important drugs, such as Mitoxantrone [4], Doxorubicin [5], and Daunorubicin [6]
Marcanine A was first isolated from the stem bark of Goniothalamus marcanii in 1999 and was proved to have significant cytotoxicity against human tumor cell lines [10,11]
We have developed a facile, efficient, and mild synthetic strategy to assemble 3-(2-hydroxybenzoyl)1-aza-anthraquinone derivatives from 3-formylchromones and 2-amino-naphthalene-1,4-dione
Summary
Anthraquinone, as a classical pharmacophore, has been applied in drug discovery for many years, [1,2,3] and this scaffold contributes to a great number of important drugs, such as Mitoxantrone [4], Doxorubicin [5], and Daunorubicin [6]. Aza-anthraquinones are crucial analogues of anthraquinones, which have attracted considerable attention for their pronounced biological activities (Figure 1) [7,8,9]. Marcanine A was first isolated from the stem bark of Goniothalamus marcanii in 1999 and was proved to have significant cytotoxicity against human tumor cell lines [10,11]. [8,12] Figure.
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