Yao, Hong published the artcileDesign, synthesis, and biological evaluation of truncated deguelin derivatives as Hsp90 inhibitors, SDS of cas: 104-01-8, the main research area is truncated deguelin synthesis SAR mol docking breast lung antitumor; deguelin truncated derivative heat shock protein inhibitor antitumor; antitumor truncated deguelin apoptosis inducer cell cycle arrest; cell migration inhibitor truncated deguelin derivative antitumor; Anticancer; Deguelin; Heat shock protein 90; Structure simplification.
A series of novel B- and C-rings truncated deguelin derivatives have been designed and synthesized in the present study as heat shock protein 90 (Hsp90) inhibitors. The synthesized compounds exhibited micromolar antiproliferative potency toward a panel of human cancer cell lines. Their structure-activity relationships (SARs) were investigated in a systematic manner. Compound I was identified to have high Hsp90 binding potency (60 nM) and caused degradation of client proteins through ubiquitin proteasome system. Further biol. studies showed that compound I induced a dose-dependent S and G2-phase cell cycle arrest on human breast cancer MCF-7 cells. Flow cytometry and Western blot analyses confirmed that compound I caused apoptosis of MCF-7 cells. In addition, compound I showed much potent inhibition on the migration and invasion of MCF-7 cells. Taken together, these results suggest that I might be a promising lead compound for further development of Hsp90 inhibitors.
European Journal of Medicinal Chemistry published new progress about Antitumor agents. 104-01-8 belongs to class isoquinoline, name is 4-Methoxyphenylacetic acid, and the molecular formula is C9H10O3, SDS of cas: 104-01-8.
Referemce:
Isoquinoline – Wikipedia,
Isoquinoline | C9H7N – PubChem