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

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

Volume: 13 Issue: 10

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

Affiliation:

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

Abstract: 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.

Cite this article as:

Moorthy Narayana N.S. Hari, Manivannan E., Karthikeyan C. and Trivedi Piyush, 6H-Indolo[2,3-b]Quinoxalines: DNA and Protein Interacting Scaffold for Pharmacological Activities, Mini-Reviews in Medicinal Chemistry 2013; 13 (10) . https://dx.doi.org/10.2174/13895575113139990005