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- Title
Preparation of 6/8/11-Amino/Chloro-Oxoisoaporphine and Group-10 Metal Complexes and Evaluation of Their in Vitro and in Vivo Antitumor Activity.
- Authors
Qin, Qi-Pin; Qin, Jiao-Lan; Meng, Ting; Yang, Gui-Ai; Wei, Zu-Zhuang; Liu, Yan-Cheng; Liang, Hong; Chen, Zhen-Feng
- Abstract
A series of group-10 metal complexes 1-14 of oxoisoaporphine derivatives were designed and synthesized. 1-14 were more selectively cytotoxic to Hep-G2 cells comparing with normal liver cells. In vitro cytotoxicity results showed that complexes 1-6, 7, 8, 10 and 11, especially 3, were telomerase inhibitors targeting c-myc, telomeric, and bcl-2 G4s and triggered cell senescence and apoptosis; they also caused telomere/DNA damage and S phase arrest. In addition, 1-6 also caused mitochondrial dysfunction. Notably, 3 with 6-amino substituted ligand La exhibited less side effects than 6 with 8-amino substituted ligand Lb and cisplatin, but similar tumor growth inhibition efficacy in BEL-7402 xenograft model. Complex 3 has the potential to be developed as an effective anticancer agent.
- Publication
Scientific Reports, 2016, p37644
- ISSN
2045-2322
- Publication type
Academic Journal
- DOI
10.1038/srep37644