CAS: 73792-06-0; Ethyl 4-Amino-2-Fluorobenzoate

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CAS号363-32-6 2-氟-4-硝基苯甲酸乙酯 | CAS号403-24-7 2-氟-4-硝基苯甲酸 | CAS号1427-07-2 2-氟-4-硝基甲苯 | CAS号403-23-6 2-氟-4-硝基苯甲酰氯 | CAS号64-17-5 乙醇 | CAS号915087-26-2 4-[(1-氰基环丁基)氨基]...

2-氟-4-硝基苯甲酸乙酯置于palladium 10% On Activated Carbon,环己烯体系中,用 乙醇 作为反应溶剂,化学反应生成 4-氨基-2-氟苯甲酸乙酯
参考文献:新型姜黄素衍生物作为p-糖蛋白抑制剂:多药耐药细胞对阿霉素的分子建模,合成和敏化.
标题:新型姜黄素衍生物作为p-糖蛋白抑制剂:多药耐药细胞对阿霉素的分子建模,合成和敏化.
摘要:数十年来,人们一直在研究mdr1 / P-糖蛋白(pgp)/ Abcb1多药转运体作为抗肿瘤治疗的药物靶点.已知天然产物姜黄素为能够阻断pgp介导的外排和使多药耐药(mdr)细胞对pgp转运的药物阿霉素(dox)敏感的化合物提供了有效的支架.我们进行了分子动力学模拟,并将姜黄素衍生物对接到pgp模型中.基于这些计算,提出了一系列具有预测的代谢稳定性和/或改善的结合亲和力的吡唑并姜黄素衍生物,用于合成和评估针对dox选择的k562 / 4亚型(k562人慢性粒细胞性白血病细胞系的衍生物)的mdr逆转能力.化合物16和19都是带有np-苯基羧酸酰胺取代基的二甲基姜黄素吡唑衍生物,是通过细胞内dox积累确定的最有效的pgp阻滞剂.此外,在无毒的亚微摩尔浓度16和19可使k562 / 4细胞对dox显着敏感.这些结果与16和19的非常好水溶性一起,表明姜黄素的新型吡唑并衍生物是开发临床适用的pgp拮抗剂的有前途的支架.
DOI:10.1016/j.Ejmech.2020.112331

专利信息

专利号:US-6090810-A
优先权日:1995-09-01
标题:Synthesis and use of retinoid compounds having negative hormone and/or antagonist activities
发明人：KLEIN ELLIOTT S; JOHNSON ALAN T; STANDEVEN ANDREW M; BEARD RICHARD L; GILLETT SAMUEL J; DUONG TIEN T; NAGPAL SUNIL; VULIGONDA VIDYASAGAR; TENG MIN; CHANDRARATNA ROSHANTHA A
权利人:ALLERGAN SALES INC
摘要:Aryl-substituted and aryl and (3-oxo-1-propenly)-substituted benzopyran, benzothiopyran, 1,2-dihydroquinoline, and 5,6-dihydronaphthalene derivatives have retinoid negative hormone and/or antagonist-like biological activities. The invented RAR antagonists can be administered to mammals, including humans, for the purpose of preventing or diminishing action of RAR agonists on the bound receptor sites. Specifically, the RAR agonists are administered or coadministered with retinoid drugs to prevent or ameliorate toxicity or side effects caused by retinoids or vitamin A or vitamin A precursors. The retinoid negative hormones can be used to potentiate the activities of other retinoids and nuclear receptor agonists. For example, the retinoid negative hormone called AGN 193109 effectively increased the effectiveness of other retinoids and steroid hormones in in vitro transactivation assays. Additionally, transactivation assays can be used to identify compounds having negative hormone activity. These assays are based on the ability of negative hormones to down-regulate the activity of chimeric retinoid receptors engineered to possess a constitutive transcription activator domain.

专利号:US-5877207-A
优先权日:1996-03-11
标 题:Synthesis and use of retinoid compounds having negative hormone and/or antagonist activities
发明人：KLEIN ELLIOTT S; JOHNSON ALAN T; STANDEVEN ANDREW M; BEARD RICHARD L; GILLETT SAMUEL J; DUONG TIEN T; NAGPAL SUNIL; VULIGONDA VIDYASAGAR; TENG MIN; CHANDRARATNA ROSHANTHA A
权利人:ALLERGAN SALES INC
摘要:Aryl-substituted and aryl and (3-oxo-1-propenly)-substituted benzopyran, benzothiopyran, 1,2-dihydroquinoline, and 5,6-dihydronaphthalene derivatives have retinoid negative hormone and/or antagonist-like biological activities. The invented RAR antagonists can be administered to mammals, including humans, for the purpose of preventing or diminishing action of RAR agonists on the bound receptor sites. Specifically, the RAR agonists are administered or coadministered with retinoid drugs to prevent or ameliorate toxicity or side effects caused by retinoids or vitamin A or vitamin A precursors. The retinoid negative hormones can be used to potentiate the activities of other retinoids and nuclear receptor agonists. For example, the retinoid negative hormone called AGN 193109 effectively increased the effectiveness of other retinoids and steroid hormones in in vitro transactivation assays. Additionally, transactivation assays can be used to identify compounds having negative hormone activity. These assays are based on the ability of negative hormones to down-regulate the activity of chimeric retinoid receptors engineered to possess a constitutive transcription activator domain.

专利号:US-2003219832-A1
优先权日:1996-03-11
标 题 :Synthesis and use of retinoid compounds having negative hormone and/or antagonist activities
发明人：KLEIN ELLIOTT S; STANDEVEN ANDREW M; NAGPAL SUNIL; CHANDRARATNA ROSHANTHA A
摘要:Aryl-substituted and aryl and (3-oxo-1-propenly)-substituted benzopyran, benzothiopyran, 1,2-dihydroquinoline, and 5,6-dihydronaphthalene derivatives have retinoid negative hormone and/or antagonist-like biological activities. The invented RAR antagonists can be administered to mammals, including humans, for the purpose of preventing or diminishing action of RAR agonists on the bound receptor sites. Specifically, the RAR agonists are administered or coadministered with retinoid drugs to prevent or ameliorate toxicity or side effects caused by retinoids or vitamin A or vitamin A precursors. The retinoid negative hormones can be used to potentiate the activities of other retinoids and nuclear receptor agonists. For example, the retinoid negative hormone called AGN 193109 effectively increased the effectiveness of other retinoids and steroid hormones in in vitro transactivation assays. Additionally, transactivation assays can be used to identify compounds having negative hormone activity. These assays are based on the ability of negative hormones to down-regulate the activity of chimeric retinoid receptors engineered to possess a constitutive transcription activator domain.

专利号:US-6469028-B1
优先权日:1995-09-01
标题:Synthesis and use of retinoid compounds having negative hormone and/or anatgonist activities
发明人：KLEIN ELLIOTT S; JOHNSON ALAN T; STANDEVEN ANDREW M; BEARD RICHARD L; GILLETT SAMUEL J; DUONG TIEN T; NAGPAL SUNIL; VULIGONDA VIDYASAGAR; TENG MIN; CHANDRARATNA ROSHANTHA A
权利人:ALLERGAN INC
摘要:Aryl-substituted and aryl and (3-oxo-1-propenly)-substituted benzopyran, benzothiopyran, 1,2-dihydroquinoline, and 5,6-dihydronaphthalene derivatives have retinoid negative hormone and/or antagonist-like biological activities. The invented RAR antagonists can be administered to mammals, including humans, for the purpose of preventing or diminishing action of RAR agonists on the bound receptor sites. Specifically, the RAR agonists are administered or coadministered with retinoid drugs to prevent or ameliorate toxicity or side effects caused by retinoids or vitamin A or vitamin A precursors. The retinoid negative hormones can be used to potentiate the activities of other retinoids and nuclear receptor agonists. For example, the retinoid negative hormone called AGN 193109 effectively increased the effectiveness of other retinoids and steroid hormones in in vitro transactivation assays. Additionally, transactivation assays can be used to identify compounds having negative hormone activity. These assays are based on the ability of negative hormones to down-regulate the activity of chimeric retinoid receptors engineered to possess a constitutive transcription activator domain.

专利号:US-5958954-A
优先权日:1995-09-01
标题 :Synthesis and use of retinoid compounds having negative hormone and/or antagonist activities
发明人：KLEIN ELLIOTT S; JOHNSON ALAN T; STANDEVEN ANDREW M; BEARD RICHARD L; GILLETT SAMUEL J; DUONG TIEN T; NAGPAL SUNIL; VULIGONDA VIDYASAGAR; TENG MIN; CHANDRARATNA ROSHANTHA A
权利人:ALLERGAN SALES INC
摘要:2,2-Dialkyl-4-aryl-substituted benzopyran and benzothiopyran derivatives of the formula where the symbols have the meaning described in the specification, have retinoid negative hormone and/or antagonist-like biological activities. The invented RAR antagonists can be administered to mammals, including humans, for the purpose of preventing or diminishing action of RAR agonists on the bound receptor sites. Specifically, the RAR agonists are administered or coadministered with retinoid drugs to prevent or ameliorate toxicity or side effects caused by retinoids or vitamin A or vitamin A precursors. The retinoid negative hormones can be used to potentiate the activities of other retinoids and nuclear receptor agonists.

专利号:US-2002156054-A1
优先权日:1995-09-01
标题:Synthesis and use of retinoid compounds having negative hormone and/or antagonist activities