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Published on:August 2020
Indian Journal of Pharmaceutical Education and Research, 2020; 54(3):698-704
Original Article | doi:10.5530/ijper.54.3.120

Nostocine A Derivatives as Human DNA Topoisomerase II-alpha Inhibitor


Authors and affiliation (s):

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

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

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.

Key words: Pyrazolotriazine, Nostocine A, Cyanobacterium, Nostoc spongiforium, Breast cancer, Docking.

 




 

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The Official Journal of Association of Pharmaceutical Teachers of India (APTI)
(Registered under Registration of Societies Act XXI of 1860 No. 122 of 1966-1967, Lucknow)

Indian Journal of Pharmaceutical Education and Research (IJPER) [ISSN-0019-5464] is the official journal of Association of Pharmaceutical Teachers of India (APTI) and is being published since 1967.

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