Efficient Synthesis and Biological Evaluation of Topopyrone C Derivatives

被引:1
作者
Aziz, Shahid [1 ,2 ]
Habib-ur-Rehman [1 ]
Ch, Muhammad Aziz [1 ]
Ghani, Kh. Shakeel [3 ]
Yasin, Kh. Ansar [4 ]
Hussain, Hidayat [2 ]
Krohn, Karsten [2 ]
机构
[1] Mirpur Univ Sci & Technol, Dept Chem, Mirpur, AJ & K, Pakistan
[2] Univ Paderborn, Dept Chem, Warburger Str 100, D-33098 Paderborn, Germany
[3] Mohiud Din Islamic Med Coll Mirpur, Mirpur, Ajk, Pakistan
[4] Univ Azad Jammu & Kashmir, Dept Chem, Muzaffarabad 13100, Pakistan
关键词
synthesis; topopyrone C; free radical scavenging effect; TOPOISOMERASE-I INHIBITORS; ANTIOXIDANT ACTIVITY; PREMITHRAMYCINONE-H;
D O I
10.1007/s10600-016-1546-2
中图分类号
R914 [药物化学];
学科分类号
100701 ;
摘要
A concise route to the synthesis of topopyrone C derivatives is reported. The 1,4-dihydroxyanthraquinone was converted to the target compound 2 using five-step sequences, while only three steps were required to access the said compound, starting from the same anthraquinone. A new one-pot alkylation served as the crucial operation for this new synthesis. Two lengthy steps are eliminated, which not only shorten the reaction but improve the yield too. Spectral techniques were used to confirm the structures of the synthesized compounds. The compound exhibited strong scavenging effect on DPPH and NO radicals. The free radical scavenging effect of the compound was found to be comparable to that of reference antioxidants BHA and ascorbic acid. This study is the first evidence for the radical scavenging property of topopyrone C derivatives.
引用
收藏
页码:58 / 61
页数:4
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