Majumdar, Papiya ; Bathula, Chandramohan ; Basu, Suparna M. ; Das, Subhendu K. ; Agarwal, Rahul ; Hati, Santanu ; Singh, Ashutosh ; Sen, Subhabrata ; Das, Benu Brata (2015) Design, synthesis and evaluation of thiohydantoin derivatives as potent topoisomerase I (Top1) inhibitors with anticancer activity European Journal of Medicinal Chemistry, 102 . pp. 540-551. ISSN 0223-5234
Full text not available from this repository.
Official URL: https://doi.org/10.1016/j.ejmech.2015.08.032
Related URL: http://dx.doi.org/10.1016/j.ejmech.2015.08.032
Abstract
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 (HTop1) 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.
| Item Type: | Article |
|---|---|
| Source: | Copyright of this article belongs to Elsevier Science. |
| ID Code: | 140890 |
| Deposited On: | 03 Dec 2025 12:04 |
| Last Modified: | 03 Dec 2025 12:04 |
Repository Staff Only: item control page
