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Nostocine A Derivatives as Human DNA Topoisomerase II-alpha Inhibitor

1,2, 2, 1

  1. 1Central Research Laboratory, Institute of Medical Sciences and Sum Hospital, Siksha ‘O’ Anusandhan (Deemed to be University), Bhubaneswar, Odisha, INDIA.
  2. 2Department of Medicinal Chemistry, School of Pharmaceutical Sciences, Siksha ‘O’ Anusandhan (Deemed to be University), Bhubaneswar, Odisha, INDIA.

CORRESPONDENCE

Rabindra Nath Padhy,

Central Research Laboratory, Institute of Medical Sciences and Sum Hospital, Siksha ‘O’ Anusandhan (Deemed to be University), Bhubaneswar, Odisha, INDIA.

rnpadhy54@gmail.com

Received: 16-11-2019; Accepted: 14-04-2020.

Volume 54, Issue 3 · pp. 698-704 · 2020 · DOI: 10.5530/ijper.54.3.120

ABSTRACT

Introduction: Due to heavy morbidity and mortality from cancer, the designing of newer drugable molecules against breast cancer is the call of day. As, Schiff-base sulfonamides have been widely used in tumor treatments.Methods: Nostocine-sulfonamide (NS) Schiff-base molecules were designed with tools of bioinformatics against the target enzyme, human topoisomerase II-alpha (topo IIa) against breast cancer. The designed NS conjugates were assessed by RO5, ADMET and molecular docking.Results: Herein, these analogues, NS-20b (Nostocine A-sulfaphenazole), 12a (Nostocine A-sulfisoxazole) and 16b (Nostocine A-sulfamethazineare) are N-heteroaryl substituted sulfonamide moieties linked with pyrazolo[4,3-e][1,2,4]triazine of Nostocine A.Conclusion: These derivatives would act as potent inhibitors of topo IIa for breast cancer.

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    Sahoo, C. R., Paidesetty, S. K., & Padhy, R. N. (2020). Nostocine A Derivatives as Human DNA Topoisomerase II-alpha Inhibitor. Indian Journal of Pharmaceutical Education and Research, 54(3), 698-704. https://doi.org/10.5530/ijper.54.3.120

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    © 2020 Author(s)

    This is an open access article distributed under the terms of the Creative Commons Attribution 4.0 License, which permits unrestricted use, distribution and reproduction in any medium, provided the original author and source are credited. CC BY 4.0