Xu, Yiming published the artcileNew modification strategy of matrine as Hsp90 inhibitors based on its specific L conformation for cancer treatment, Formula: C7H6N2, the main research area is radicicol thermal shift assay anticancer activity mechanism of action; Anticancer activity; L-shaped matrine derivatives; Mechanism of action; Radicicol; Thermal shift assay.
The similarity of spatial structure between radicicol and matrine urged us to perform conformation modification of matrine, followed by L-shaped matrine derivatives, 6, 12, 21a-h and 22a-h were originally designed, synthesized and evaluated for Hsp90N inhibitors as anticancer agents. TSA (Thermal Shift Assay) results indicated that 21e, 22a-c and 22e-g exhibited strong binding force against Hsp90N with|ΔTm| > 3, meanwhile, MTT assay also revealed these compounds displayed potent anticancer activity with IC50 values below 25μM against HepG2, HeLa and MDA-MB-231 cells lines. Then, compound 22g with a high ΔTm = 10.92 was chosen as a representative to perform further mechanism study. It can induce cell apoptosis, arrest the cell cycle at the S phase and decrease the expression level of Hsp90 in Hela cell. These results originally provided targeted modification strategy for matrine derivatives to serve as Hsp90 inhibitors for cancer therapy.
Bioorganic & Medicinal Chemistry published new progress about Antitumor agents. 1885-29-6 belongs to class nitriles-buliding-blocks, name is 2-Aminobenzonitrile(Flakes or Chunks), and the molecular formula is C7H6N2, Formula: C7H6N2.
Referemce:
Nitrile – Wikipedia,
Nitriles – Chemistry LibreTexts