Molecular editing of NSC-666719 enabling discovery of benzodithiazinedioxide-guanidines as anticancer agents

Author:

Krishna Rao Vajja1ORCID,Paul Subarno2,Gulkis Mitchell3,Shen Zhihang4ORCID,Nair Haritha5,Singh Amandeep6,Li Chenglong4,Sharma Arun K.6,Çağlayan Melike3,Das Chinmay2,Das Biswajit2,Kundu Chanakya N.2ORCID,Narayan Satya5,Guchhait Sankar K.1ORCID

Affiliation:

1. Department of Medicinal Chemistry, National Institute of Pharmaceutical Education and Research (NIPER), Sector 67, SAS Nagar, Mohali, Punjab 160062, India

2. Cancer Biology Division, School of Biotechnology, Kalinga Institute of Industrial Technology (KIIT), Deemed to be University, Campus-11, Patia, Bhubaneswar-751024, Odisha, India

3. Department of Biochemistry and Molecular Biology, College of Medicine, University of Florida, 1200 Newell Drive, Gainesville, FL 32610, USA

4. Department of Medicinal Chemistry, College of Pharmacy, University of Florida, 1345 Center Drive, Gainesville, FL 32610, USA

5. Department of Anatomy and Cell Biology, College of Medicine, University of Florida, 1200 Newell Drive, Gainesville, FL 32610, USA

6. Department of Pharmacology, Penn State Cancer Institute, CH72, Penn State College of Medicine, 500 University Drive, Hershey, PA 17033, USA

Abstract

In this study, a unique strategy of scaffold-hopping-based molecular editing of a bioactive agent NSC-666719 was investigated, which led to the development of new benzodithiazinedioxide-guanidine based anticancer agents with Polβ inhibition.

Funder

Science and Engineering Research Board

Council of Scientific and Industrial Research, India

Cancer Center, University of Florida Health

Department of Biotechnology, Ministry of Science and Technology, India

Indian Council of Medical Research

Publisher

Royal Society of Chemistry (RSC)

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