Design, Synthesis, and Mechanistic Study of Novel Ciprofloxacin/Thiazole Chalcone Hybrids as Potential Anticancer Agents.

ABSTRACT: A novel series of thiazole chalcone/ciprofloxacin hybrids were synthesized and screened for their anticancer activity against NCI-60 cancer cell lines, USA. Interestingly, compounds 4b and 4d exhibited potent antiproliferative activities, particularly against leukemia HL-60, RPMI-8226, and colon HCT-116 cells, with IC₅₀ values of 0.3-3.70 µM. Importantly, compounds 4b and 4d exhibited enhanced selectivity for cancer cells relative to doxorubicin with IC₅₀ values of 26.80, 41.20, and 19.80 µM, respectively. Mechanistic investigations revealed that compounds 4b and 4d inhibited topoisomerases (Topo) I/IIβ activity, being fourfold and twofold more effective than untreated controls, respectively. Furthermore, these compounds induc

SUBMITTER: Hashem H 

PROVIDER: S-EPMC12655637 | biostudies-literature | 2025 Nov

REPOSITORIES: biostudies-literature