Nostocine A Derivatives as Human DNA Topoisomerase II-alpha Inhibitor

Sahoo, Chita Ranjan; Paidesetty, Sudhir Kumar; Padhy, Rabindra Nath

doi:10.5530/ijper.54.3.120

Original ArticleIndian Journal of Pharmaceutical Education and ResearchVol. 54 | Issue 3 | 2020 | pp. 698–704Open access

Nostocine A Derivatives as Human DNA Topoisomerase II-alpha Inhibitor

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²,
¹^*

¹ Central Research Laboratory, Institute of Medical Sciences and Sum Hospital, Siksha ‘O’ Anusandhan (Deemed to be University), Bhubaneswar, Odisha, INDIA.
² Department 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.
Email: rnpadhy54@gmail.com

Published:: Aug 22, 2020
Received:: Nov 16, 2019
Accepted:: Apr 14, 2020
DOI:: 10.5530/ijper.54.3.120

How to cite

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

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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Article metadata

Title	Nostocine A Derivatives as Human DNA Topoisomerase II-alpha Inhibitor
Authors	Chita Ranjan Sahoo; Sudhir Kumar Paidesetty; Rabindra Nath Padhy
Affiliations	Central Research Laboratory, Institute of Medical Sciences and Sum Hospital, Siksha ‘O’ Anusandhan (Deemed to be University), Bhubaneswar, Odisha, INDIA.; Department of Medicinal Chemistry, School of Pharmaceutical Sciences, Siksha ‘O’ Anusandhan (Deemed to be University), Bhubaneswar, Odisha, INDIA.
Corresponding author	rnpadhy54@gmail.com
Journal	Indian Journal of Pharmaceutical Education and Research
Volume / Issue	Vol. 54, Issue 3 (2020)