CAS: 237430-03-4; 7,12-Dihydro-9-Nitroindolo[3,2-D][1]Benzazepin-6(5H)-One

该化合物是一种合成化合物,属于被称为环状单体动脉抑制剂的小型分子类别,其特点是它能够有选择地抑制CDK2, 这在细胞循环监管中起着关键的作用.这种抑制可能导致细胞循环停用,使Alsterpaullone成为癌症研究的一个对象,因为它可能有助于控制癌症细胞的扩散.该化合物有一个独特的化学结构,包括双环核,有助于其生物活动. 甲状腺素通常在其潜在的治疗应用方面,特别是在肿瘤学方面研究,因为针对CDKs可成为癌症治疗的战略.此外,这种抑制还被用于各种生物化学学研究,探索细胞循环监管机制以及CDK抑制对细胞过程的影响.与许多化学物质一样,处理Alsterpaulone需要适当的安全措施,因为其生物活动和潜在毒性.

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CAS号16511-38-9 1H-[1]-苯并氮杂卓-2,... | CAS号636-99-7 4-硝基苯肼盐酸盐

合成工艺路线路线简述

    📜在 硫酸,溶剂黄146体系中,化学反应 3.0H,反应生成阿特波龙
    参考文献:Paullones,一系列细胞周期蛋白依赖性激酶抑制剂:合成,Cdk1 /细胞周期蛋白b抑制作用的评估以及体外抗肿瘤活性.
    标题:Paullones,一系列细胞周期蛋白依赖性激酶抑制剂:合成,Cdk1 /细胞周期蛋白b抑制作用的评估以及体外抗肿瘤活性.
    摘要:丹参酮代表一类新的小分子细胞周期蛋白依赖性激酶(cdk)抑制剂.为了研究结构活性关系并开发具有抗肿瘤活性的paullones,先导结构kenpaullone(9-Bromo-7,12-Dihydroindolo [3,2-D] [1] Benzazepin-6(5H)-One,4A )合成.通过1S-[1]苯并ze庚因-2,5(3H,4H)-二酮5的fischer吲哚反应制备在2,3,4,9和11位具有不同取代基的泡龙.通过分别在氢化钠/ Thf或氢氧化钾/丙酮的存在下用烷基卤化物处理肯保隆来实现内酰胺或吲哚氮原子上的选择性取代.Kenpaullone衍生的硫内酰胺18的s-甲基化产生了甲基硫代亚氨酸19,与羟胺反应后得到羟基am20.新的paullones在cdk1 / Cyclin B抑制试验和美国国家癌症研究所(nci)的体外抗肿瘤细胞株筛选程序中均进行了测试.关于cdk1 /细胞
    Doi:10.1021/jm9900570

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    专利信息


    专利号:US-7763292-B2
    优先权日:2004-05-10
    标题 :Cancer cell growth inhibition by black bean (Phaseolus vulgaris L) extracts
    发明人：GUTIERREZ-URIBE JANET A; SERNA-SALDIVAR SERGIO R O; MORENO-CUEVAS JORGE E; HERNANDEZ-BRENES CARMEN; GUAJARDO-TOUCHE ELSA M
    权利人:INST TECHNOLOGICO Y DE ESTUDIO
    摘要:This invention relates to processes or methods for the production of compositions comprising extracts of black beans containing phenolics, such as polyphenols, flavonoids, and tannins, phytosterols, and triterpenoids such as saponins and other natural products with proven antioxidant capacity, colorant capacity, and uses thereof, e.g., as antioxidants, nutritional supplements, as food, cosmetic or pharmaceutical antioxidants or colorants, as antineoplastic or anti-cancer or anti-tumor preparations, e.g., to treat, prevent and/or inhibit cancers or cancer cell growth, such as hormone dependent or hormone independent tumors or cancers or cancer cells. such as mammalian mammary, prostate, colon, hepatic, leukemia cancer or cancer cell growth, as active ingredient(s) in compositions for lowering cholesterol or lowering oxidation of LDL or for inhibiting cholesterol synthesis (or the enzyme therefor), as an active ingredient(s) in compositions, e.g., nutritional supplements.

    专利号:CN-117903053-A
    优先权日:2024-01-15
    标 题 :Synthesis method and application of diaryl azepine compound

    专利号:CN-112500349-B
    优先权日:2021-01-12
    标题 :Synthesis method of benzolactam compound

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    主要参考文献


    1: Cui C, Wang Y, Wang Y, Zhao M, Peng S. Alsterpaullone, a Cyclin-Dependent Kinase Inhibitor, Mediated Toxicity in HeLa Cells through Apoptosis-Inducing Effect. J Anal Methods Chem. 2013;2013:602091. doi: 10.1155/2013/602091. Epub 2013 Mar 12.
    2: Faria CC, Agnihotri S, Mack SC, Golbourn BJ, Diaz RJ, Olsen S, Bryant M, Bebenek M, Wang X, Bertrand KC, Kushida M, Head R, Clark I, Dirks P, Smith CA, Taylor MD, Rutka JT. Identification of alsterpaullone as a novel small molecule inhibitor to target group 3 medulloblastoma. Oncotarget. 2015 Aug 28;6(25):21718-29. doi: 10.18632/oncotarget.4304.
    3: Yin P, Zheng N, Dong J, Xu C, Zhang X, Ding G. Alsterpaullone induces apoptosis of HepG2 cells via a p38 mitogen-activated protein kinase signaling pathway. Oncol Lett. 2019 Jan;17(1):1177-1183. doi: 10.3892/ol.2018.9700. Epub 2018 Nov 14.

    合成参考文献


    参考文献:10.1186/1477-7827-7-144
    摘要:Tang L, Zhang Y, Pan H, Luo Q, Zhu X, Dong M, Leung PC, Sheng J, Huang H. Involvement of cyclin B1 in progesterone-mediated cell growth inhibition, G2/M cell cycle arrest, and apoptosis in human endometrial cell. Reproductive Biology and Endocrinology. 2009 Dec 07;7(1):144. doi: 10.1186/1477-7827-7-144.
    参考文献:10.1371/journal.pone.0020069
    摘要:Krumm SA, Ndungu JM, Yoon J, Dochow M, Sun A, Natchus M, Snyder JP, Plemper RK. Potent Host-Directed Small-Molecule Inhibitors of Myxovirus RNA-Dependent RNA-Polymerases. PLoS ONE. 2011 May 16;6(5):e20069. doi: 10.1371/journal.pone.0020069.
    参考文献:10.1186/1478-811x-9-15
    摘要:Kaufmann L, Marinescu G, Nazarenko I, Thiele W, Oberle C, Sleeman J, Blattner C. LiCl induces TNF-α and FasL production, thereby stimulating apoptosis in cancer cells. Cell Communication and Signaling. 2011 May 24;9(1):15. doi: 10.1186/1478-811x-9-15.
    摘要:Soni DV, Jacobberger JW. Inhibition of cdk1 by alsterpaullone and thioflavopiridol correlates with increased transit time from mid G2 through prophase. Cell Cycle. 2004 Mar;3(3):349–57.
    参考文献:10.1002/mrd.20495
    摘要:Acevedo N, Wang X, Dunn RL, Smith GD. Glycogen synthase kinase‐3 regulation of chromatin segregation and cytokinesis in mouse preimplantation embryos. Molecular Reproduction Devel. 2006 Aug 29;74(2):178–88. doi: 10.1002/mrd.20495.
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