Design, synthesis and pharmacological evaluation of new PARP1 inhibitors by merging pharmacophores of olaparib and the natural product alantolactone

التفاصيل البيبلوغرافية
العنوان: Design, synthesis and pharmacological evaluation of new PARP1 inhibitors by merging pharmacophores of olaparib and the natural product alantolactone
المؤلفون: Muzaffar Kayumov, Li Jia, Azizbek Pardaev, Shan-Shan Song, Sharafitdin Mirzaakhmedov, Chunyong Ding, Yong-Jun Cheng, Ruihan (Isabella) Zhang, Xubin Bao, Ze-Hong Miao, Jin-Xue He, Ao Zhang
المصدر: European journal of medicinal chemistry. 240
سنة النشر: 2022
مصطلحات موضوعية: Pharmacology, Biological Products, Organic Chemistry, Poly (ADP-Ribose) Polymerase-1, Apoptosis, General Medicine, Poly(ADP-ribose) Polymerase Inhibitors, Piperazines, G2 Phase Cell Cycle Checkpoints, Lactones, Cell Line, Tumor, Drug Discovery, Humans, Phthalazines, Sesquiterpenes, Eudesmane
الوصف: Based on the reported synthetic lethality of the combination of PARP inhibitor olaparib with the natural product alantolactone, we designed several series of new PARP1 inhibitors by structurally merging both compounds into a single hybrid compound. Among them, compounds 20e and 25a displayed not only high biochemical activity (IC
تدمد: 1768-3254
الوصول الحر: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::fdc3702b4946f51f97055476c9fc94a7Test
https://pubmed.ncbi.nlm.nih.gov/35785724Test
حقوق: CLOSED
رقم الانضمام: edsair.doi.dedup.....fdc3702b4946f51f97055476c9fc94a7
قاعدة البيانات: OpenAIRE