Literature

Abstract

Previously, 4-tosylanthra[1,2-c][1,2,5]thiadiazole-6,11-dione (1) was identified as a novel non-camptothecin topoisomerase I (Top1) inhibitor by structure-based virtual screening. Herein, a series of 4-substituted derivatives were designed and synthesized. Most of them showed potent Top1 inhibitory activity. Their in vitro antiproliferative activity was also evaluated in A549, HCT-116 and ZR-75-30 human cancer cell lines. Compound 8s showed good antiproliferative activity with IC50 of 0.52μM and 0.42μM against HCT-116 and ZR-75-30 cell line, respectively. Top1 unwinding assay and molecular modeling studies rationalized the mode of action of this new class of inhibitors.

DOI： 10.1016/j.bmcl.2017.03.039

Design, synthesis and evaluation of 4-substituted anthra[2,1-c][1,2,5]thiadiazole-6,11-dione derivatives as novel non-camptothecin topoisomerase I inhibitors

Bioorganic & Medicinal Chemistry Letters 2017.0

Design, synthesis and evaluation of thiohydantoin derivatives as potent topoisomerase I (Top1) inhibitors with anticancer activity

European Journal of Medicinal Chemistry 2015.0

Novel 4-(4-substituted amidobenzyl)furan-2(5H)-one derivatives as topoisomerase I inhibitors

European Journal of Medicinal Chemistry 2017.0

Ring fusion strategy for the synthesis of anthra[2,3-d]oxazole-2-thione-5,10-dione homologues as DNA topoisomerase inhibitors and as antitumor agents

European Journal of Medicinal Chemistry 2014.0

Design, synthesis and antitumor activity of non-camptothecin topoisomerase I inhibitors

Bioorganic & Medicinal Chemistry Letters 2015.0

Discovery of a Novel Series of Quinolone and Naphthyridine Derivatives as Potential Topoisomerase I Inhibitors by Scaffold Modification