Recommanded Product: Isobenzofuran-1(3H)-one. Recently I am researching about PARP INHIBITORS; DNA-REPAIR; OPPORTUNITIES; DISCOVERY; THERAPY; UPDATE, Saw an article supported by the . Published in FUTURE SCI LTD in LONDON ,Authors: Xin, MH; Sun, JJ; Huang, W; Tang, F; Liu, ZY; Jin, Q; Wang, J. The CAS is 87-41-2. Through research, I have a further understanding and discovery of Isobenzofuran-1(3H)-one
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.
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Reference:
Benzofuran – Wikipedia,
,Benzofuran | C8H6O – PubChem