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Research Article

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

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Pages 394-405 | Received 26 Apr 2009, Accepted 17 Jul 2009, Published online: 16 Mar 2010
 

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.

Acknowledgements

The authors are thankful to the Vice Chancellor, RGPV, Bhopal for providing laboratory facilities. Another of the authors (C.K.) would like to thank CSIR, New Delhi for providing a Senior Research Fellowship. The authors are also acknowledge CDRI, Lucknow and CNCI, Kolkata for their help in this work.

Declaration of interest: One of the authors (N.S.H.N.M.) would like to give his sincere thanks to AICTE, New Delhi for a grant from Career Award to Young Teachers.

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