📜替莫唑胺置于硫酸,Sodium Nitrite体系中,用 水 用作溶剂,化学反应 16.0H,以68%的收率获得3,4-二氢-3-甲基-4-氧代咪唑并[5,1-D]-1,2,3,5-四嗪-8-甲酰胺酸 参考文献:A Novel Series Of Phenolic Temozolomide (Tmz) Esters With 4 To 5-Fold Increased Potency,Compared To Tmz,Against Glioma Cells Irrespective Of Mgmt Expression 标题:A Novel Series Of Phenolic Temozolomide (Tmz) Esters With 4 To 5-Fold Increased Potency,Compared To Tmz,Against Glioma Cells Irrespective Of Mgmt Expression 摘要:诊断为多形性胶质母细胞瘤(gbm)的患者的标准治疗是替莫唑胺(tmz). Doi:10.1039/d0Ra02686G
专利号:US-7173021-B2 优先权日:2004-09-02 标题:Synthesis of temozolomide esters as potent anticancer pro-drugs for topical and transdermal applications in treatments of cancers 发明人:WANG YONGFENG; CONWAY BARBARA R; SUPPASANSATORN PANASSAYA 权利人:TIANJIN NORTH PHARM SCI TECH C 摘要:This invention relates to the use of temozolomide esters (4-dihydro-3-methyl-4-oxoimidazo[5,1-d]-1,2,3,5-tetrazine-8-carboxylate esters) Formula 1 as potent anticancer pro-drugs for treatment of cancers by topical and transdermal applications, and to a novel process for synthesis of temozolomide esters by a direct esterification of temozolomide acid (3,4-dihydro-3-methyl-4-oxoimidazo[5,1-d]-1,2,3,5-tetrazine-8-carboxylic acid) with a halogeno-aliphatic compound in presence of a base, or with an alcohol in presence of a dehydrate agent
专利号:US-2006047117-A1 优先权日:2004-09-02 标 题 :Synthesis of temozolomide esters as potent anticancer pro-drugs for topical and transdermal applications in treatments of cancers
专利号:CN-115887450-A 优先权日:2022-12-09 标 题:Synthesis of squalene-based temozolomide and preparation and application of self-assembled nanoparticles
专利号:CN-115887450-B 优先权日:2022-12-09 标题:Synthesis of squalene-temozolomide and preparation and application of its self-assembled nanoparticles
1: Ercelik M, Tekin C, Gurbuz M, Tuncbilekli Y, Dogan HY, Mutlu B, Eser P, Tezcan G, Parın FN, Yildirim K, Sarihan M, Akpinar G, Kasap M, Bekar A, Kocaeli H, Taskapilioglu MO, Aksoy SA, Ozpar R, Hakyemez B, Tunca B. A new nano approach to prevent tumor growth in the local treatment of glioblastoma: Temozolomide and rutin-loaded hybrid layered composite nanofiber. Asian J Pharm Sci. 2024 Dec;19(6):100971. doi: 10.1016/j.ajps.2024.100971. Epub 2024 Oct 23. 2: Li S, Zeng F, Zhou Q, Li L, Lo H, Chen J, Fan Z, Huang G, Nie L. NIR-II Photoacoustic Imaging-Guided Chemo-Photothermal Therapy Using PA1094T Combined with Anti-CD47 Antibody: Activating Pyroptosis against Orthotopic Glioblastoma. Adv Healthc Mater. 2024 Nov 30:e2403108. doi: 10.1002/adhm.202403108. Epub ahead of print. 31(11):7308-7318. doi: 10.3390/curroncol31110539.
合成参考文献
参考文献:10.1021/acs.jmedchem.3c01467 摘要:Stiller T, Merk D. Exploring Fatty Acid Mimetics as NR4A Ligands. J. Med. Chem. 2023 Nov 02;66(22):15362–9. doi: 10.1021/acs.jmedchem.3c01467.