- Design, synthesis, and cytotoxicity of indolizinoquinoxaline-5,12-dione derivatives, novel DNA topoisomerase IB inhibitors
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A series of new indolizinoquinoxaline-5,12-dione derivatives were designed and synthesized via a heterocyclization reaction of 6,7-dichloroquinoxaline-5,8- dione with active methylene reagents and pyridine derivatives. The synthesized compounds exhibited significant activity to inhibit the growth of four human tumour cell lines, including lung adenocarcinoma cell, large-cell lung carcinoma cell, breast carcinoma cell, and ardriamycin-resistant breast carcinoma cell at micromolar range. These compounds were also investigated for their inhibition to DNA topoisomerase IB activity. The results indicated that the indolizinoquinoxaline-5,12-dione structure might be a potential pharmacophore in anti-cancer drug design.
- Shen, De-Qing,Wu, Ning,Li, Yan-Ping,Wu, Zu-Ping,Zhang, Hong-Bin,Huang, Zhi-Shu,Gu, Lian-Quan,An, Lin-Kun
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- A New Synthetic Route to 6,7-Dichloro-5,8-quinoxalinedione and Synthesis of Its Derivatives
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6,7-Dichloro-5,8-quinoxalinedione (2), an analogue of Dichlone, was prepared from 4-aminophenol (3) in 27percent overall yield in 8 steps via chloroxidation of the sulfuric acid salt of 8-amino-5-quinoxalinol (9) as a key step.And two derivatives, 6-chloro-5-hydroxypyrazinophenazine (10) and pyridoimidazoquinoxaline-6,11-dione (11), were prepared by reaction of 2 with 1,2-phenylenediamine and 2-aminopyridine in 79percent and 46percent yields, respectively.
- Han, Gyoonhee,Shin, Kye Jung,Kim, Dong Chan,Yoo, Kyung Ho,Kim, Dong Jin,Park, Sang Woo
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p. 2495 - 2502
(2007/10/03)
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