Synthesis of bile acid derivatives and in vitro cytotoxic activity with pro-apoptotic process on multiple myeloma (KMS-11), glioblastoma multiforme (GBM), and colonic carcinoma (HCT-116) human cell lines

Estrogen receptor β potentiates the antiproliferative effect of raloxifene and affects the cell migration and invasion in HCT-116 colon cancer cells

“…Many reports have used HCT-116 cell line for scientiWc research, as HCT-116 cells are more representative (Deng et al 2007;Lee et al 2011;Brossard et al 2010). Wang et al (2006) revealed that curcumin inhibits neurotensinmediated interleukin-8 production and migration of HCT-116 human colon cancer cells, and the same phenomenon was also noted in the colon cancer cells HT-29.…”

Enzymatic synthesis of bile acid derivatives and biological evaluation against Trypanosoma cruzi

“…They are of great interest by acting as powerful biological detergents that help in dissolving and absorption of fats, fatty acids and lipid soluble vitamins 2 and because they exhibit various pharmacological activities, such as potent and selective farnesoid X receptor (FXR) antagonism, 3 antimicrobial 4 and anticancer activities. 5 Moreover, all bile acids and their conjugates form bile salts which, as amphiphilic compounds, are widely used in drug formulations as absorption promoters 6 and as excipients that can influence gastrointestinal solubility, absorption and chemical or enzymatic stability of drugs, 7 enhance transdermal penetration, 8 etc. The application of enzymes and whole cells of microorganisms in the synthesis of pharmaceuticals derivatives has received considerable attention in recent years.…”

Opioid Tripeptides Hybridized with trans‐1‐Cinnamylpiperazine as Proliferation Inhibitors of Pancreatic Cancer Cells in Two‐ and Three‐Dimensional in vitro Models

“…The lipophilic fragment of the peptidomimetics ( trans ‐1‐cinnamylpiperazine) may affect the binding affinity for MOR and increase the penetration abilities of the synthesized compounds. It was shown that this moiety is already used for the synthesis of bile acid derivatives, where the resulting compounds have pro‐apoptotic activity for various human cancer cells (GBM, KMS‐11, and HCT‐116) . It has been reported that the lipophilicity of anticancer compounds is correlated with increased biological activity and cytotoxicity .…”

“…It was shown that this moiety is already used for the synthesis of bile acid derivatives, where the resulting compounds have pro-apoptotic activity for various human cancerc ells (GBM, KMS-11, and HCT-116). [28] It has been reported that the lipophilicity of anticancer compounds is correlated with increased biological activity and cytotoxicity. [29,30] This molecular property is therefore an important factor in the drug design process, due to the formationo fa dditional binding sites in the ligand-receptor complex.…”