6H-Indolo[2,3-b]Quinoxalines: DNA and Protein Interacting Scaffold for Pharmacological Activities

Author(s): N.S. Hari Narayana Moorthy, E. Manivannan, C. Karthikeyan, Piyush Trivedi

Journal Name: Mini-Reviews in Medicinal Chemistry

Volume 13 , Issue 10 , 2013

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6H-Indolo[2,3-b]quinoxaline, a planar fused heterocyclic compound exhibits a wide variety of pharmacological activities. The mechanism of pharmacological action exerted by these compounds is predominantly DNA intercalation. The thermal stability of the intercalated complex (DNA and 6H-indolo[2,3-b]quinoxaline derivatives) is an important parameter for the elucidation of anticancer, antiviral and other activities. This thermal stability of the 6H-indolo[2,3- b]quinoxaline–DNA complex depends on the type of substituents and side chains attached to the 6H-indolo[2,3- b]quinoxaline nucleus and also the orientation of the side chain towards the GC rich minor groove of the DNA. Highly active 6H-indolo[2,3-b]quinoxaline derivatives such as NCA0424, B-220 and 9-OH-B-220 have shown good binding affinity to DNA as evident from high thermal stability of compound-DNA complex. Interestingly, these compounds possessed poor inhibitory activity on topoisomerase II enzyme but have significant MDR modulating activity. This review establishes ‘6H-indolo[2,3-b]quinoxaline’ as a valuable template for design and development of novel molecules with different biological activities.

Keywords: 6H-indolo[2, 3-b]quinoxalines, anticancer, antiviral, P-glycoprotein, DNA intercalation.

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Article Details

Year: 2013
Published on: 30 June, 2013
Page: [1415 - 1420]
Pages: 6
DOI: 10.2174/13895575113139990005
Price: $65

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