Quality Control of Isobenzofuran-1(3H)-one. In 2020 FUTURE MED CHEM published article about PARP INHIBITORS; DNA-REPAIR; OPPORTUNITIES; DISCOVERY; THERAPY; UPDATE in [Xin, Minhang; Sun, Jiajia] Xi An Jiao Tong Univ, Hlth Sci Ctr, Sch Pharm, Dept Med Chem, 76 Yanta West Rd, Xian 710061, Peoples R China; [Huang, Wei] Cent China Normal Univ, Coll Chem, Int Joint Res Ctr Intelligent Biosensor Technol &, Key Lab Pesticide & Chem Biol,Minist Educ, Wuhan 430079, Peoples R China; [Tang, Feng; Liu, Zhaoyu; Jin, Qiu; Wang, Jia] Jiangsu Simcere Pharmaceut Co Ltd, 699-18 Xuan Wu Dist, Nanjing 210042, Peoples R China in 2020, Cited 22. The Name is Isobenzofuran-1(3H)-one. Through research, I have a further understanding and discovery of 87-41-2.
Aim:The development of effective PARP-1 inhibitors has received great enthusiasm in medicinal chemistry communities.Results:A new series of novel phthalazinone derivatives were designed and synthesized. Among these,B1andB16displayed more potent PARP-1 inhibitory activities than olaparib.B16gave an IC(50)value of 7.8 nM against PARP-1, and a PF(50)value of 3.4 in the sensitizing effect assay. Thein vivopharmacokinetic properties evaluation showedB16displayed insufficient oral exposure, and it was also not stable in rat blood.Conclusion:The results indicated that our design phthalazinone derivatives were potent PARP-1 inhibitors, and compoundB16was a valuable lead compound with siginificantin vitroefficacy, deseaving further optimization so as to develop anticancer drug candidate.
Quality Control of Isobenzofuran-1(3H)-one. Welcome to talk about 87-41-2, If you have any questions, you can contact Xin, MH; Sun, JJ; Huang, W; Tang, F; Liu, ZY; Jin, Q; Wang, J or send Email.
Reference:
Benzofuran – Wikipedia,
,Benzofuran | C8H6O – PubChem