CAS: 763114-25-6; 2-Fluoro-5-((3-Oxoisobenzofuran-1(3H)-Ylidene)Methyl)Benzonitrile

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CAS号61260-15-9 (3-氧代-1,3-二氢异苯并... | CAS号218301-22-5 2-氟-5-甲酰基苯腈 | CAS号17858-15-0 DIETHYL PHTHALI... | CAS号119-67-5 邻羧基苯甲醛 | CAS号77771-02-9 3-溴-4-氟苯甲醛 | CAS号763114-26-7 5-[(3,4-二氢-4-氧代... | CAS号763111-49-5 KU-0058948 | CAS号763114-04-1 奥拉帕尼杂质

3-羟基异苯并呋喃-1(3H)-酮置于sodium Methylate,三乙胺体系中,用 四氢呋喃,甲醇 作为反应溶剂,化学反应 1.17H,反应生成 2-氟-5-[(3-氧代-1(3H)-异苯并呋喃亚基)甲基]苯腈
参考文献:鉴定聚(adp-核糖)聚合酶-1(parp-1)的探针质量降解剂.
标题:鉴定聚(adp-核糖)聚合酶-1(parp-1)的探针质量降解剂.
摘要:聚(adp-核糖)聚合酶-1(parp-1)是碱基切除修复途径中的关键dna修复酶,已被作为有吸引力的癌症治疗靶标进行研究.事实证明,对parp-1的干预对携带brca1 / 2突变的癌细胞更为敏感.市场上已经有几种parp-1抑制剂可用于治疗乳腺癌,卵巢癌和前列腺癌.很有可能,基于parp-1的降解,新开发的针对嵌合体的蛋白水解(protac)可能会提供更潜在的策略.在这里,我们报告基于parp-1抑制剂olaparib和crbn(大脑)配体来那度胺的组合,针对靶向chimaera(protac)的蛋白水解的设计,合成和评估.在sw620电池中,我们的探针级降解剂化合物2有效诱导parp-1降解,从而导致抗增殖,细胞凋亡,细胞周期停滞和癌细胞迁移抑制.因此,我们的发现为parp-1敲除提供了一种新的化学探针.
DOI:10.1080/14756366.2020.1804382

专利信息

专利号:US-10874667-B2
优先权日:2016-10-14
标题 :Pharmaceutical salt of antitumor heterocyclic imidazole compound
发明人：FAN XING; LI WENHUA; QIN JIHONG
权利人:SHANGHAI HUILUN LIFE SCIENCE & TECH CO LTD; SHANGHAI HUILIN LIFE SCINECE & TECH CO LTD
摘要:The present invention relates to the field of pharmaceutical synthesis, and in particular to an antitumor heterocyclic imidazole compound (I), namely: a pharmaceutical salt of 4-(3-(4-(1H-imidazo[4,5-b]pyridine-5-yl)piperazine-1-carbonyl)-4-fluorobenzyl)phthalazine-1(dihydro)-ketone, a preparation method therefor, a pharmaceutical composition thereof and a use thereof in the preparation of antitumor drugs. The pharmaceutical salt of the compound (I) in the present invention may be used in the preparation of a medicament for the treatment or prevention of conditions which can be improved by inhibiting PARP activity.