吴茱萸碱置于sodium Hydride,Sodium Hydroxide体系中,用 四氢呋喃,甲醇,水,N,N-Dimethyl-D6-Formamide 作为反应溶剂,化学反应 10.5H,反应生成 吴茱萸碱 参考文献:Quinazolinecarboline Alkaloid Evodiamine As Scaffold For Targeting Topoisomerase I And Sirtuins 标题:Quinazolinecarboline Alkaloid Evodiamine As Scaffold For Targeting Topoisomerase I And Sirtuins 摘要:This Paper Reports The Synthesis Of A Series Of Evodiamine Derivatives. We Assayed The Ability To Inhibit Cell Growth On Three Human Tumour Cell Lines (H460,Mcf-7 And Hepg2) And We Evaluated The Capacity To Interfere With The Catalytic Activity Of Topoisomerase I Both By The Relaxation Assay And The occurrence Of The Cleavable Complex. Moreover,Whose Effect On Sirtuins 1,2 And 3 Was Investigated. Finally,Molecular Docking Analyses Were Performed In An Attempt To Rationalize The Biological Results. (C) 2013 Elsevier Ltd. All Rights Reserved. DOI:10.1016/j.Bmc.2013.09.030
专利号:WO-2022244943-A1 优先权日:2021-05-21 标题 :Method for predicting recurrence of lung cancer, and pharmaceutical composition for recurrence inhibition 发明人:LEE HO-YOUNG 权利人:SEOUL NAT UNIV R&DB FOUNDATION 摘要:The present invention relates to: a method for providing information necessary in predicting the recurrence of lung cancer; a pharmaceutical composition for inhibiting the recurrence of lung cancer; and the like. Since the present inventors have identified that in slow-cycling cancer cells responsible for lung cancer recurrence, RGS2 is significantly increased and ATF4 is reduced, it is expected that by measuring the level of expression or activity of RGS2 and ATF4, the likelihood of lung cancer recurrence can be easily and quickly predicted. In addition, since the present inventors have identified that the growth of slow-cycling cancer cells can be inhibited and the apoptosis thereof can be induced by eliminating the expression of RGS2 or blocking the protein synthesis inhibitory action of RGS2, the present invention is expected to be also variously usable in the drug development of lung cancer recurrence inhibiting therapeutic agents for inhibiting the expression or activity of RGS2.
专利号:WO-2005102340-A1 优先权日:2003-05-30 标题 :Piperazine melanocortin-specific compounds 发明人:SHARMA SHUBH D; SHI YI-QUN; WU ZHIJUN; RAJPUROHIT RAMESH 权利人:PALATIN TECHNOLOGIES INC; SHARMA SHUBH D; SHI YI-QUN; WU ZHIJUN; RAJPUROHIT RAMESH 摘要:Melanocortin receptor-specific piperazine or ketopiperazine compounds having the structure (I); and stereoisomer and pharmaceutically acceptable salts thereof, where X is CH2 or C=O, R1, R2, and R3 are as described in the specification, preferably where R3 is a D-amino acid with at least one substituted or unsubstituted phenyl or naphthyl aromatic ring, and where R3 optionally further includes an amine capping group, a second amino acid residue or a second amino acid residue with an amine capping group, which compounds are agonists, antagonists or mixed agonists and antagonists at one or more melanocortin receptors, and having utility in the treatment of melanocortin receptor-related disorders and conditions. Methods of synthesis of compounds of structure (I), pharmaceutical compositions containing a compound of structure (I) and methods relating to the use thereof are also disclosed.
专利号:CN-113045503-B 优先权日:2020-07-31 标题:Preparation method of 2-trifluoromethyl substituted quinazolinone compound and application of compound in synthesis of drug molecules
专利号:CA-3111403-A1 优先权日:2018-09-17 标 题:Matter of composition, synthesis, formulation and application of fl118 platform positions 7 and 9-derived analogues for treatment of human disease
专利号:CN-114108013-A 优先权日:2021-12-31 标 题:A kind of electrochemical synthesis method of trifluoromethyl substituted polycyclic quinazolinone derivatives
专利号:WO-2020061106-A4 优先权日:2018-09-17 标题:Matter of composition, synthesis, formulation and application of fl118 platform positions 7 and 9-derived analogues for treatment of human disease
1: Xiong YJ, Chen DP, Peng JY, Wang JY, Lv BC, Liu FF, Lin Y. Characteristics of evodiamine-exerted stimulatory effects on rat jejunal contractility. Nat Prod Res. 2015;29(4):388-91. doi: 10.1080/14786419.2014.947485. Epub 2014 Aug 12. doi: 10.1016/j.fitote.2015.07.019. Epub 2015 Aug 6. Review. Chinese. doi: 10.3892/mmr.2014.2705. Epub 2014 Oct 20. doi: 10.1007/s00280-015-2902-9. Epub 2015 Nov 6. Epub 2015 Apr 27. 7: Sachita K, Kim Y, Yu HJ, Cho SD, Lee JS. In Vitro Assessment of the Anticancer Potential of Evodiamine in Human Oral Cancer Cell Lines. Phytother Res. 2015 Aug;29(8):1145-51. doi: 10.1002/ptr.5359. Epub 2015 Apr 22. doi: 10.1016/j.neulet.2014.12.038. Epub 2014 Dec 26. doi: 10.3892/mmr.2014.1924. Epub 2014 Jan 28. Epub 2014 Dec 11. 11: Jiang DF, Li WT, Yang HL, Zhang ZZ, Chen D, Sun C. Long-term effects of evodiamine on expressions of lipogenesis and lipolysis genes in mouse adipose and liver tissues. Genet Mol Res. 2014 Feb 20;13(1):1038-46. doi: 10.4238/2014.February.20.5. Chinese. doi: 10.3390/ijms15023154.
合成参考文献
参考文献:10.4268/cjcmm20110711 摘要:Ma X, Li J, Liu Y. [Determination of evodiamine and rutacarpine in zhuyu hewei zhitong capsules by HPLC]. Zhongguo Zhong Yao Za Zhi. 2011 Apr;36(7):871–3.