Design, Synthesis, and Evaluation of Tetraethylene Glycol Tethered Isatin-Coumarin Hybrids as Novel Anticancer Agents

摘要

Herein, we report the design and synthesis of a new set of tetraethylene glycol tethered isatin-coumarin hybrids 7a-l as anticancer agents. Results revealed that all the synthesized hybrids showed no or weak activities against their in vitro antitumor activities against drug-sensitive HepG2, Hela, A549, DU145, SKOV3, and MCF-7 as well as drug-resistant MCF-7/DOX (doxorubicin-resistant MCF-7) human cancer cell lines. The structure-activity relationship was also discussed, and the enriched structure-activity relationship may pave the way for further rationale design of this kind of hybrids.