📜甲氨蝶呤置于tris-Hcl Buffer体系中,用 水 用作溶剂,化学反应 2.0H,反应生成4-[n-(2,4-二氨基-6-蝶啶甲基)-N-甲氨基]苯甲酸半盐酸盐n水 参考文献:Metabolism Of Folate And Related Compounds In A Trypanosomid Flagellate,Crithidia Fasciculata. Part V. Uptake And Metabolism Of Methotrexate By Crithidia Fasciculata. 标题:Metabolism Of Folate And Related Compounds In A Trypanosomid Flagellate,Crithidia Fasciculata. Part V. Uptake And Metabolism Of Methotrexate By Crithidia Fasciculata. 摘要:在crithidia Fasciculata Atcc 12857中检测甲氨蝶呤的摄取和代谢.当细胞在含有生物蝶呤的培养基中生长时,与甲氨蝶呤一起孵育,细胞在1分钟内完成甲氨蝶呤的摄取,并且每108个细胞的甲氨蝶呤量维持在19之间.和 37 Fmol/min 在整个剩余的生长期.相比之下,叶酸的摄取在至少20分钟内呈线性,并且在生长期间细胞的叶酸摄取率在31至247Fmol/分钟/108个细胞之间变化.甲氨蝶呤和氨基蝶呤抑制叶酸摄取.当 C. Fasciculata 在含有甲氨蝶呤的培养基中培养时,细胞吸收的甲氨蝶呤代谢成多种化合物.使用 Deae-纤维素和 Sephadex G-10 柱色谱从细胞和培养上清液中分离出其中一种代谢物,并根据其在薄层色谱法及其紫外和红外吸收光谱.在 C. Fasciculata 的无细胞提取物中发现了将甲氨蝶呤转化为 Ampte 的酶活性. Doi:10.1271/bbb1961.47.1847
专利号:US-7230101-B1 优先权日:2002-08-28 标 题:Synthesis of methotrexate-containing heterodimeric molecules 发明人:MURTHI KRISHNA K; SMITH CHASE C 权利人:GPC BIOTECH INC 摘要:The present invention relates to novel compositions of methotrexate-containing heterodimeric probe molecules, also known as chemical inducers of dimerization (CID), useful in three-hybrid assays. The invention further relates to synthesis of said compositions and their intermediates. Another aspect of the invention is a method for using the heterodimeric probe molecules described herein in drug screens to identify potential protein targets to a given ligand, optimize protein-ligand interactions, or identify potential ligands for a given protein target. In certain embodiments, the invention contemplates the synthesis of the following methotrexate-containing heterodimeric probe:
专利号:US-9402911-B2 优先权日:2011-12-08 标题:Multifunctional small molecules 发明人:BAKER JR JAMES R; HUANG BAOHUA M; THOMAS THOMMEY P 权利人:UNIV MICHIGAN REGENTS 摘要:The present invention relates to dendrimer synthesis. Specifically, the present invention relates to dendrimer compositions (e.g., scaffolds) capable of copper-free click conjugation for use in the synthesis of functionalized dendrimers, and methods of use of the same.
专利号:US-7799524-B2 优先权日:2002-10-03 标 题:Substrates for O6-alkylguanina-DNA alkyltransferase 发明人:KINDERMANN MAIK; JOHNSSON KAI; BIERI CHRISTOPH 权利人:ECOLE POLYTECHNIQUE FERDEALE D 摘要:The invention relates to compounds of formula 1 n nwherein R 1 -R 2 is a guanine derivative; X is oxygen or sulfur; R 3 is a heteroaromatic, unsaturated heterocyclyl or an alkynyl group with the double or triple bond connected to CH 2 ; R 4 is a linker; and L is a label, a plurality of same or different labels, a bond connecting R 4 to R 1 forming a cyclic substrate, or a further group —R 3 —CH 2 —X—R 1 -R 2 . The invention relates also to methods of manufacture of such novel AGT substrates, to intermediates useful in the synthesis of such AGT substrates, and to a method of transferring a label from such AGT substrates to O 6 -alkylguanine-DNA alkyltransferase (AGT) fusion proteins comprising proteins of interest.
专利号:US-12144874-B2 优先权日:2015-09-09 标题 :Synthesis and composition of photodynamic therapeutic agents for the targeted treatment of cancer 发明人:KULARATNE SUMITH A; GAGARE PRAVIN 权利人:ON TARGET LABORATORIES LLC; ON TARGET LABORATORIES INC 摘要:The present invention describes new compounds that are useful for image-guided surgery and photodynamic therapy. In particular the compounds may be targeted to the nucleus or the mitochondria after compounds were delivered to diseased tissues such as cancer using a ligand that target receptor that express on the diseased tissue and followed by receptor mediated endocytosis and provide effective activity against cancer cells as well as other disorders. Methods and compositions for use of the same are described.
专利号:US-6291673-B1 优先权日:1997-10-17 标题:Folic acid derivatives 发明人:FUCHS PHILIP L; LUO JIN; LANTRIP DOUGLAS A 权利人:PURDUE RESEARCH FOUNDATION 摘要:Novel folic acid derivatives and their use in preparation of γ-esters of folic acid via a pteroyl azide intermediate are described. Folic acid γ-esters are useful intermediates in the synthesis of folic acid conjugates capable of binding folate receptors in vitro and in vivo.
专利号:CN-102617356-B 优先权日:2005-11-03 标 题:Synthesis of N, N-dimethyl-1,3-diaminopropane (DMAPA) method
1: Silva MF, Ribeiro C, Gonçalves VMF, Tiritan ME, Lima Á. Liquid chromatographic methods for the therapeutic drug monitoring of methotrexate as clinical decision support for personalized medicine: A brief review. Biomed Chromatogr. 2018 May;32(5):e4159. doi: 10.1002/bmc.4159. Epub 2018 Jan 12. Review. doi: 10.1021/acs.analchem.7b00916. Epub 2017 May 25. doi: 10.1684/abc.2016.1135. doi: 10.1080/10826076.2016.1243558. Epub 2016 Oct 10. 5: Schofield RC, Ramanathan LV, Murata K, Fleisher M, Pessin MS, Carlow DC. Development of an Assay for Methotrexate and Its Metabolites 7-Hydroxy Methotrexate and DAMPA in Serum by LC-MS/MS. Methods Mol Biol. 2016;1383:213-22. doi: 10.1007/978-1-4939-3252-8_23. doi: 10.1016/j.jchromb.2015.08.025. Epub 2015 Aug 22. 7: Passari AK, Mishra VK, Saikia R, Gupta VK, Singh BP. Isolation, abundance and phylogenetic affiliation of endophytic actinomycetes associated with medicinal plants and screening for their in vitro antimicrobial biosynthetic potential. Front Microbiol. 2015 Apr 7;6:273. doi: 10.3389/fmicb.2015.00273. eCollection 2015.
合成参考文献
参考文献:10.2116/analsci.19p481 摘要:Mei S, Cui Y, Zhang D, Zeng C, Ren X, Yu K, Lin S, Zhao Z. Simultaneous Determination of Urine Methotrexate, 7-Hydroxy Methotrexate, Deoxyaminopteroic Acid, and 7-Hydroxy Deoxyaminopteroic Acid by UHPLC-MS/MS in Patients Receiving High-dose Methotrexate Therapy. Anal Sci. 2020 Dec 10;36(12):1479–83. doi: 10.2116/analsci.19p481.