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Design, synthesis, cytotoxic evaluation, and QSAR study of some 6H-indolo[2,3-b]quinoxaline derivatives.

N S Hari Narayana Moorthy, C Karthikeyan, Piyush Trivedi

School of Pharmaceutical Sciences, Rajiv Gandhi Technical University, Gandhi Nagar, Bhopal, India.

Journal Article: Journal of Enzyme Inhibition and Medicinal Chemistry (impact factor: 1.5). 03/2010; 25(3):394-405. DOI: 10.3109/14756360903190747

Abstract

In the pathway of anticancer drug development, we designed and synthesized some 6H-indolo[2,3-b]quinoxaline derivatives (which act as DNA intercalators) by structural modification. The structure of the 6H-indolo[2,3-b]quinoxaline derivatives was confirmed by IR, NMR, Mass and elemental analysis. The compounds (IDQ-5, IDQ-10, IDQ-11, IDQ-13, and IDQ-14) exhibited significant in vitro activity against a human leukemia (HL-60) cell line. The QSAR derived for modeling the cytotoxic activity of 6H-indolo[2,3-b]quinoxaline derivatives suggests that candidate structures for increased cytotoxic potency should incorporate cyclic substituents or substituents with primary carbon atoms.

Source: PubMed

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Keywords

6H-indolo[2,3-b]quinoxaline derivatives
 
anticancer drug development
 
candidate structures
 
cyclic substituents
 
cytotoxic activity
 
DNA intercalators
 
human leukemia
 
IDQ-5
 
IR
 
primary carbon atoms
 
QSAR
 
vitro activity