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IJPER · Lens · Nostocine A Derivatives as Human DNA Topoisomerase II-alpha Inhibitor

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Article · Volume 54, Issue 3 · pp. 698–704

Nostocine A Derivatives as Human DNA Topoisomerase II-alpha Inhibitor

Chita Ranjan Sahoo1,2, Sudhir Kumar Paidesetty2, Rabindra Nath Padhy1

  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.

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.

Keywords: Pyrazolotriazine; Nostocine A; Cyanobacterium; Nostoc spongiforium; Breast; cancer; Docking

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