Journal
EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
Volume 102, Issue -, Pages 540-551Publisher
ELSEVIER FRANCE-EDITIONS SCIENTIFIQUES MEDICALES ELSEVIER
DOI: 10.1016/j.ejmech.2015.08.032
Keywords
Topoisomerase I; Thiohydantoin; Hydantoin; Methylfuro[3,4-c]pyridine-3,4(1H,5H)-dione; Camptothecin; Leishmania bi-subunit topoisomerase I
Categories
Funding
- Wellcome Trust/DBT-India Alliance Intermediate Fellowship [IA/I/13/1/500888]
- IACS startup fund, Department of Science and Technology, Government of India
- Shiv Nadar University
Ask authors/readers for more resources
DNA topoisomerase I is a potential chemotherapeutic target. Here, we designed and synthesized a library comprising of hydantoin and thiohydantoin derivatives and tested them against human and Leishmania Top1. One of the thiohydantoin compounds with substituted thiophenyl as the central moiety (compound 15) exhibited potent inhibition of human Top1) through stabilization of Top1-DNA cleavage complexes and showed selective anticancer activity against human cervical carcinoma (HeLa) and breast carcinoma (MCF-7) cell lines. Molecular modeling studies with HTop1 rationalized the inhibitory mechanism of compound 15. (C) 2015 Elsevier Masson SAS. All rights reserved.
Authors
I am an author on this paper
Click your name to claim this paper and add it to your profile.
Reviews
Recommended
No Data Available
Share Paper
