In order to reverse drug resistance and reduce side effects of oxaliplatin (OXA) in colon cancer (CRC) treatment, six platinum(IV) complexes modified with indole-chalcone derivatives were synthesized and evaluated for their antiproliferative activities against various CRC cell lines. Among them, indole-chalcone oxaliplatin(IV)-propanoate (ICplatin-18), which obtained a two-methylene linker and was derived from oxaliplatin(IV), exhibited the most parental anticancer activity compared with either monotherapy or combination against parent and OXA-resistant HCT-116 (HCT-116/OXA) cells, obtained good selectivity to-ward normal cell line (L02 and HUEVC), and significantly inhibited migration of HCT-116 cells. This per-formance may be associated to the dramatic increase in intracellular accumulation and enhancement of DNA damage. Further mechanistic studies indicated that ICplatin-18 significantly inhibited tubulin poly-merization, elevated accumulation of intracellular reactive oxygen molecule, and activated mitochondrial apoptotic.(c) 2022 Published by Elsevier B.V.
基金：
Young and Middle-aged Health and Technology Innovation Leading Talent Project of Henan Province [YXKC2020 0 08]
第一作者单位：[1]Zhengzhou Univ, Dept Digest Dis, Affiliated Hosp 1, Zhengzhou, Peoples R China
共同第一作者：
通讯作者：
推荐引用方式(GB/T 7714)：
Cao Xinguang,Li Rui,Wang Hui,et al.Novel indole-chalcone platinum(IV) complexes as tubulin polymerization inhibitors to overcome oxaliplatin resistance in colorectal cancer *[J].JOURNAL OF MOLECULAR STRUCTURE.2023,1272:doi:10.1016/j.molstruc.2022.134169.
APA：
Cao, Xinguang,Li, Rui,Wang, Hui,Guo, Changqing,Wang, Saiqi...&Zhao, Ruihua.(2023).Novel indole-chalcone platinum(IV) complexes as tubulin polymerization inhibitors to overcome oxaliplatin resistance in colorectal cancer *.JOURNAL OF MOLECULAR STRUCTURE,1272,
MLA：
Cao, Xinguang,et al."Novel indole-chalcone platinum(IV) complexes as tubulin polymerization inhibitors to overcome oxaliplatin resistance in colorectal cancer *".JOURNAL OF MOLECULAR STRUCTURE 1272.(2023)
