alexa Synthesis of friedelan triterpenoid analogs with DNA topoisomerase IIα inhibitory activity and their molecular docking studies.


Biochemistry & Analytical Biochemistry

Author(s): Mandal A, Ghosh S, Bothra AK, Nanda AK, Ghosh P

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Abstract Five highly oxygenated friedelan derivatives (3a, 3b, 4, 5a and 5b) were synthesized. The structures of these compounds were established on the basis of spectral (IR, 1D and 2D NMR, MS etc.) and chemical data. The molecules, including the parent compounds were screened for three-dimensional (3D) molecular docking on the crystal structure of topoisomerase IIα (1 bgw for topoisomerase IIα, PDB). Compounds 3a and 5a showed a dose dependent inhibition of catalytic activity of human topoisomerase IIα. Copyright © 2012 Elsevier Masson SAS. All rights reserved. This article was published in Eur J Med Chem and referenced in Biochemistry & Analytical Biochemistry

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