Chemistry is traditionally divided into organic and inorganic chemistry. category: benzoxazole, The former is the study of compounds containing at least one carbon-hydrogen bonds.In a patent£¬Which mentioned a new discovery about 22876-22-8
Discover the leading compound of 4beta-S-(5-fluorobenzoxazole)-4-deoxy-4?-demethylepipodophyllotoxin with millimolar-potency toxicity by modifying the molecule structure of 4?-demethylepipodophyllotoxin
4?-Demethylepipodophyllotoxin (DMEP) derivatives are broad-spectrum and potent antitumor leading compound. Because of their unacceptable toxicity, DMEP derivatives often failed in the development of new drug. Until now, there was no report on the millimolar-potency toxicity of DMEP derivatives by modifying the molecule structure of DMEP. For the first time, this work discovered leading compounds with millimolar-potency toxicity by modifying the molecule structure of DMEP. The IC50 value of 4beta-S-(5-fluorobenzoxazole-2-)-4-deoxy-4?-demethylepipodophyllotoxin (Compound 2) was around 323.4?2000.9 muM on human healthy cells (i.e., HL-7702, H8, MRC-5 and HMEC), which was significantly reduced by 171?1999 times than podophyllotoxin (1.0?2.6 muM) and 9?80 times than etoposide (21.5?75.4 muM). Compared with the treatment of etoposide, DNA repair proteins HMGB1 and PARK7 were specifically activated and the expression of anti-apoptotic proteins were up-regulated in HL-7702 cells after the treatment of Compound 2. These indicated the toxicity of Compound 2 was synergistically reduced by DNA repair and anti-apoptosis pathway.
If you are interested in 22876-22-8, you can contact me at any time and look forward to more communication. category: benzoxazole
Reference£º
Benzoxazole – Wikipedia,
Benzoxazole | C7H5NO – PubChem