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

作者：Moorthy N S Hari Narayana^*; Manivannan E; Karthikeyan C; Trivedi Piyush

来源：Mini Reviews in Medicinal Chemistry, 2013, 13(10): 1415-1420.

DOI：10.2174/13895575113139990005

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

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 %26apos;6H-indolo[2,3-b]quinoxaline%26apos; as a valuable template for design and development of novel molecules with different biological activities.

• 出版日期2013-8