Moxifloxacin-isatin hybrids tethered by 1,2,3-triazole and their anticancer activities.

Moxifloxacin-isatin hybrids tethered by 1,2,3-triazole and their anticancer activities.
Curr Top Med Chem. 2020 Jan 28;:
Authors: Yang M, Liu H, Zhang Y, Wang X, Xu Z
Abstract
Fourteen moxifloxacin-isatin hybrids 5, 6 and 13 tethered via 1,2,3-triazole were designed, and synthesized in this paper. The in vitro activities of the synthesized hybrids against a panel of cancer cell lines including HepG2 liver cancer cells, MCF-7, doxorubicin-resistant MCF-7 (MCF-7/DOX) breast cancer cells, DU-145 and multidrug-resistant DU-145 (MDR DU-145) prostate cancer cells were evaluated. The results indicated that most of them were active against the five cancer cells, whereas the parent moxifloxacin was devoid of activity. In particular, the hybrid 5b (IC50: 31.3-76.8μM) with the anticancer activity higher than Vorinostat (IC50: 96.7->100μM) also showed potential tubulin polymerization inhibitory activity. The structure-activity relationship was summarized for further rational design of more efficient anticancer candidates.
PMID: 31994464 [PubMed - as supplied by publisher]

Source: Current Topics in Medicinal Chemistry - January 27, 2020 Category: Chemistry Authors: Yang M, Liu H, Zhang Y, Wang X, Xu Z Tags: Curr Top Med Chem Source Type: research