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Title: Agents for Hepatocellular Carcinoma: Synthesis and Mode of Action
Authors: CHEN XIAO
Keywords: Benzylideneindolinone,hepatocellular carcinoma, growth inhibition, receptor tyrosine kinases, sirtuins, drug likeness
Issue Date: 22-Jan-2014
Citation: CHEN XIAO (2014-01-22). Agents for Hepatocellular Carcinoma: Synthesis and Mode of Action. ScholarBank@NUS Repository.
Abstract: The benzylideneindolinone scaffold is historically linked to the inhibition of receptor tyrosine kinases (RTKs) and anticancer activity. The aim of this thesis was to test the hypothesis that structural elaboration of the underfunctionalized 47 would provide a means of uncovering drug-like compounds with greater potency and selectivity on HCC. To this end, 115 compounds across 8 series of functionalized benzylideneindolinones were designed, synthesized and evaluated for their effects on the viability of liver cancer cell lines (HuH7, Hep3B, HepG2). Compound 3-12 was one of the more potent and selective compounds affecting the viability of HCC cells. It inhibited the phosphorylation of FGFR4 and HER3 in HuH7 cells at low concentrations. Inhibition of FGFR4 and HER3 may contribute to the growth inhibitory effects of 3-12 on HuH7 cells.Several members of the library inhibited Sirt 2 activity. The most potent inhibitors were the 6-methoxybenzylidene indolinones and N-substituted analogs of 47.
Appears in Collections:Ph.D Theses (Open)

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