通过四步合成法制备了一种新的杂环生物还原性双烷基化剂2,3-双(氯甲基)苯并[ g ]喹喔啉-5,10-二酮。已显示通过bis-S RN 1机理在电子转移条件下与2-硝基丙烷阴离子发生反应,从而以优异的收率得到三种C-烷基化产物。将此bis-S RN 1反应扩展到各种亚硝酸根或丙二酸根阴离子和以S为中心的阴离子,导致了一类新的潜在活性的苯并[ g ]喹喔啉-5,10-二酮衍生物。
[EN] HETEROCYCLIC NAPHTHOQUINONES DERIVATIVES FOR USE IN THE TREATMENT OF CANCERS INCLUDING CUSHING DISEASE<br/>[FR] DÉRIVÉS DE NAPHTHOQUINONES HÉTÉROCYCLIQUES DESTINÉS À ÊTRE UTILISÉS DANS LE TRAITEMENT DE CANCERS, Y COMPRIS LA MALADIE DE CUSHING
申请人:COMMISSARIAT ENERGIE ATOMIQUE
公开号:WO2018029137A1
公开(公告)日:2018-02-15
The present invention concerns heterocyclic naphthoquinones derivatives for use in the treatment of Cushing disease and other cancers, in particular via the inhibition of Ubiquitin Specific Proteases (USP) 8 and/or 2.
HETEROCYCLIC NAPHTHOQUINONES DERIVATIVES FOR USE IN THE TREATMENT OF CANCERS INCLUDING CUSHING DISEASE
申请人:Commissariat à l'Énergie Atomique
et aux Énergies Alternatives
公开号:EP3497083B1
公开(公告)日:2022-01-19
Heterocyclic Naphthoquinones Derivatives for Use in the Treatment of Cancers Including Cushing Disease
申请人:Commissariat a l'Energie Atomique et aux Energies Alternatives
公开号:US20190169136A1
公开(公告)日:2019-06-06
The present invention concerns heterocyclic naphthoquinones derivatives for use in the treatment of Cushing disease and other cancers, in particular via the inhibition of Ubiquitin Specific Proteases (USP) 8 and/or 2.
Giorgi-Renault; Renault; Baron, European Journal of Medicinal Chemistry, 1985, vol. 20, # 2, p. 144 - 148