66726-12-3Relevant articles and documents
Sesquiterpene Lactones Potentiate Olaparib-Induced DNA Damage in p53 Wildtype Cancer Cells
Larrosa, Igor,Osborne, Hugh C.,Schmidt, Christine K.
, (2022/01/22)
Despite notable advances in utilising PARP inhibitor monotherapy, many cancers are not PARP inhibitor-sensitive or develop treatment resistance. In this work, we show that the two structurally-related sesquiterpene lactones, a 2-bromobenzyloxy derivative
Synthesis and biological evaluation of α-santonin derivatives as anti-hepatoma agents
Chen, Hao,Yang, Xiao,Yu, Zongmin,Cheng, Ziying,Yuan, Hu,Zhao, Zeng,Wu, Guozhen,Xie, Ning,Yuan, Xing,Sun, Qingyan,Zhang, Weidong
, p. 90 - 97 (2018/03/06)
A series of α-santonin-derived compounds as potentially anti-hepatoma agents were designed and synthesized in an effort to find novel therapeutic agents. Among them, derivative 5h was more potent than the positive control 5-fluorouracil (5-Fu) on HepG-2, QGY-7703 and SMMC-7721 with IC50 values of 7.51, 3.06 and 4.08 μM, respectively. The structure-activity relationships (SARs) of these derivatives were discussed. In addition, flow cytometry and western blot assay revealed that the derivatives induced hepatoma cells apoptosis by facilitating apoptosis-related proteins expressions. Our findings suggested that these α-santonin-derived analogues hold promise as chemotherapeutic agents for the treatment of human hepatocellular cancer.
Design, synthesis and anticancer activity of Michael-type thiol adducts of α-santonin analogue with exocyclic methylene
Khazir, Jabeena,Riley, Darren L.,Chashoo, Gousia,Mir, Bilal Ahmad,Liles, David,Islam, Md. Ataul,Singh, Shashank K.,Vishwakarma, Ram A.,Pilcher, Lynne A.
, p. 769 - 779 (2015/08/06)
Abstract A series of Michael-type analogues were generated on the C-ring of α-santonin (α-methylene-γ-butyrolactone) upon reaction with various thiols. All the thiol adducts synthesized were evaluated for their anticancer activity against four human cance