Synthesis and evaluation of aroylthiourea derivatives of 4-β-amino-4'-O-demethyl-4-desoxypodophyllotoxin as novel topoisomerase II inhibitors

Cytotoxic effect and molecular docking of 4-ethoxycarbonylmethyl-1-(piperidin-4-ylcarbonyl)-thiosemicarbazide—a novel topoisomerase II inhibitor

“…Many reports in recent years have indicated that inhibitory action towards Topo II coincides with cytotoxic properties for several naturally occurring and synthetic compounds [25–30]. We therefore subjected 1 to a preliminary MTT assay in estrogen receptor-positive (MCF-7) and estrogen receptor-negative (MDA-MB-231) breast cancer cells to identify any possible correlation.…”

Characterization of the anticancer effects of S115, a novel heteroaromatic thiosemicarbazone compound, in vitro and in vivo

“…Several complexes, including thiourea-platinum [18] , -gold [19] , -iron [20] , and -copper [21] , have been synthesized. Thiourea derivatives of classic anticancer drugs such as camptothecin [22] and podophyllum [23] have also been synthesized and tested for the anticancer activities. In recent years, the successful development of target-specific compounds received widespread recognition for their utility in clinical treatment.…”

Click chemistry‐based synthesis and cytotoxic activity evaluation of 4α‐triazole acetate podophyllotoxin derivatives

“…To overcome these disadvantages, extensive derivation efforts have been continuously carried out in many research laboratories all over the world. As it was found that the sugar moiety of etoposide was not essential for topoisomerase II inhibition (Ren, Wu, Xin, Chen, & Hu, ; Zhao et al., ), several potential C4‐non‐sugar substituted derivatives of 4′‐demethyl‐PPT (Kamal, Ashwini Kumar, Suresh, Juvekar, & Zingde, ; Kumar et al., ; Li et al., ; Sun et al., ; Tang et al., ; Zhang, Chen, Zhang, Chen, & Wang, ; Zhang et al., ) such as GL‐331 ( 4 ) (Huang et al., ; Lee, ), NK‐611 (Utsugi et al., ), NPF, and TOP‐53 ( 5 ) were brought into human clinical trials. However, they did not proceed further (Mross et al., ).…”