aminomethylated Resin

• 分子结构分类: 有机化合物 - 有机氧化合物
• 英文名称: aminomethylated Resin
• 英文别名: p-methylbenzhydrylamine hydrochloride salt resin；MBHA hydrochloride salt resin；aminomethyl Resin；Aminomethylpolystyrene resin hydrochloride；2-Propoxy-1-(3',4',5'-trimethoxyphenyl)-1-ethanone；2-propoxy-1-(3,4,5-trimethoxyphenyl)ethanone
• 化学式: CH₄NPol*ClH
• 分子量: 268.3
• InChiKey: DWLZLIXKOPXHJF-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  2.3
• 重原子数：
  19
• 可旋转键数：
  8
• 环数：
  1.0
• sp3杂化的碳原子比例：
  0.5
• 拓扑面积：
  54
• 氢给体数：
  0
• 氢受体数：
  5

反应信息

• 作为反应物：
  描述：

  aminomethylated Resin 、 3-氟-4-甲氧基苯甲醛 在 哌啶 、 溶剂黄146 作用下， 以 乙醇 为溶剂， 反应 48.0h， 以61%的产率得到(Z)-3-(3-fluoro-4-methoxyphenyl)-2-propoxy-1-(3,4,5-trimethoxyphenyl)prop-2-en-1-one
  参考文献：
  名称：

  Combretastatin-like chalcones as inhibitors of microtubule polymerization. Part 1: Synthesis and biological evaluation of antivascular activity

  摘要：

  The alpha-methyl chalcone SD400 is a potent inhibitor of tubulin assembly and possesses potent anticancer activity. Various chalcone analogues were synthesized and evaluated for their cell growth inhibitory properties against the K562 human chronic myelogenous leukemia cell line (SD400, IC50 0.21 nM; combretastatin A4 CA4, IC50 2.0 nM). Cell cycle analysis by flow cytometry indicated that these agents are antimitotic (SD400, 83% of the cells are in G(2)/M phase; CA4 90%). They inhibit tubulin assembly at low concentration (SD400, IC50 0.46 mu M; CA4, 0.10 mu M) and compete with [H-3] colchicine for binding to tubulin (8% [H-3] colchicine remained bound to tubulin after competition with SD400 or CA4). Upon treatment with SD400, remarkable cell shape changes were elicited in HUVEC cells, consistent with vasculature damaging activity. (C) 2009 Elsevier Ltd. All rights reserved.

  DOI：

  10.1016/j.bmc.2009.09.039
• 作为产物：
  描述：

  丙醇 、 2-溴-1-(3,4,5-三甲氧基苯基)乙酮 在 三氟化硼乙醚 、 silver carbonate 作用下， 以62%的产率得到aminomethylated Resin
  参考文献：
  名称：

  Combretastatin-like chalcones as inhibitors of microtubule polymerization. Part 1: Synthesis and biological evaluation of antivascular activity

  摘要：

  The alpha-methyl chalcone SD400 is a potent inhibitor of tubulin assembly and possesses potent anticancer activity. Various chalcone analogues were synthesized and evaluated for their cell growth inhibitory properties against the K562 human chronic myelogenous leukemia cell line (SD400, IC50 0.21 nM; combretastatin A4 CA4, IC50 2.0 nM). Cell cycle analysis by flow cytometry indicated that these agents are antimitotic (SD400, 83% of the cells are in G(2)/M phase; CA4 90%). They inhibit tubulin assembly at low concentration (SD400, IC50 0.46 mu M; CA4, 0.10 mu M) and compete with [H-3] colchicine for binding to tubulin (8% [H-3] colchicine remained bound to tubulin after competition with SD400 or CA4). Upon treatment with SD400, remarkable cell shape changes were elicited in HUVEC cells, consistent with vasculature damaging activity. (C) 2009 Elsevier Ltd. All rights reserved.

  DOI：

  10.1016/j.bmc.2009.09.039
• 作为试剂：
  描述：

  D-果糖-1-磷酸钡盐 在 哌啶 、 aminomethylated Resin 、 1-羟基苯并三唑 、 N,N'-二异丙基碳二亚胺 作用下， 以 二氯甲烷 、 N,N-二甲基甲酰胺 为溶剂， 反应 16.0h， 生成 propan-2-yl 5-[(4-propan-2-ylphenoxy)methyl]furan-2-carboxylate
  参考文献：
  名称：

  Modulation of FLT3-ITD and CDK9 in acute myeloid leukaemia cells by novel proteolysis targeting chimera (PROTAC)

  摘要：

  DOI：

  10.1016/j.ejmech.2022.114792

文献信息

• Propenone derivatives
  申请人：Kyowa Hakko Kogyo Co., Ltd.

  公开号：US05952355A1

  公开（公告）日：1999-09-14

  The present invention relates to propenone derivatives represented by the following formula (I): ##STR1## wherein R.sup.1 represents hydrogen, substituted or unsubstituted lower alkyl, substituted or unsubstituted aryl, or YR.sup.5 (wherein Y represents S or O; and R.sup.5 represents substituted or unsubstituted lower alkyl, substituted or unsubstituted aryl, substituted or unsubstituted heteroaryl, or a substituted or unsubstituted cyclic ether residue); R.sup.2 and R.sup.3 independently represent hydrogen, lower alkyl, or substituted or unsubstituted aralkyl, or alternatively R.sup.2 and R.sup.3 are combined to form substituted or unsubstituted methylene or ethylene; R.sup.4 represents hydrogen, hydroxy, lower alkyl, substituted or unsubstituted aralkyl, lower alkoxy, substituted or unsubstituted aralkyloxy, or halogen; and X represents substituted or unsubstituted indolyl; or pharmaceutically acceptable salts thereof.

  本发明涉及以下式(I)所代表的丙酮衍生物：##STR1##其中R.sup.1代表氢、取代或未取代的较低烷基、取代或未取代的芳基，或YR.sup.5（其中Y代表S或O；R.sup.5代表取代或未取代的较低烷基、取代或未取代的芳基、取代或未取代的杂芳基，或取代或未取代的环氧基残基）；R.sup.2和R.sup.3独立地代表氢、较低烷基，或取代或未取代的芳基烷基，或者R.sup.2和R.sup.3结合形成取代或未取代的亚甲基或乙烯基；R.sup.4代表氢、羟基、较低烷基、取代或未取代的芳基烷基、较低烷氧基、取代或未取代的芳基烷氧基，或卤素；X代表取代或未取代的吲哚基；或其药学上可接受的盐。
• Imidazonaphthyridines
  申请人：3M Innovative Properties Company

  公开号：US06194425B1

  公开（公告）日：2001-02-27

  Imidazonaphthyridine and tetrahydroimidazonaphthyridine compounds induce the biosynthesis of cytokines such as interferon and tumor necrosis factor. The compounds exhibit antiviral and antitumor properties. Methods of preparing the compounds and intermediates useful in the preparation of the compounds are also disclosed.

  咪唑并噻吩并噻吩衍生物和四氢咪唑并噻吩衍生物诱导细胞因子的生物合成，例如干扰素和肿瘤坏死因子。这些化合物具有抗病毒和抗肿瘤特性。还公开了制备这些化合物以及在制备这些化合物中有用的中间体的方法。
• SPIROHETEROCYCLIC DERIVATIVE COMPOUNDS AND DRUGS COMPRISING THE COMPOUNDS AS THE ACTIVE INGREDIENT
  申请人：ONO PHARMACEUTICAL CO., LTD.

  公开号：EP1553098A1

  公开（公告）日：2005-07-13

  Spiroheterocyclic ring derivatives of the formula (I) (wherein R1 is H, alkyl, alkenyl, etc.; R2 is keto, thioketo, alkyl, etc.; R3 is alkyl, alkenyl, etc.; AB ring is fused bi-cyclic ring or spiro ring), quaternary ammonium salts thereof, N-oxides thereof, non-toxic salts thereof, or pharmaceutical compositions comprising them, as an active ingredient. The compounds of the formula (I) regulate the effect of chemokine/chemokine receptor, they are used for prevention and treatment of various inflammatory diseases, allergic diseases, immunosuppression, cancer metastasis and acquired immune deficiency syndrome etc.

  公式（I）的Spiroheterocyclic环衍生物（其中R1是H，烷基，烯基等；R2是酮，硫酮，烷基等；R3是烷基，烯基等；AB环是融合的双环或螺环），其季铵盐，N-氧化物，非毒性盐或包含它们的药物组成物，作为活性成分。公式（I）的化合物调节趋化因子/趋化因子受体的作用，它们用于预防和治疗各种炎症性疾病，过敏性疾病，免疫抑制，癌症转移和获得性免疫缺陷综合症等。
• Imidazolyl derivatives
  申请人：——

  公开号：US20040176379A1

  公开（公告）日：2004-09-09

  The present invention is directed to imidazolyl derivatives of formula (I) where the substituents are defined in the specification, which are useful as agonists or antagonists of somatostatin receptors.

  本发明涉及式（I）的咪唑基衍生物，其中取代基在规范中有定义，其作为生长抑素受体的激动剂或拮抗剂具有实用性。
• Combretastatin a-4 derivatives having antineoplastic activity
  申请人：Lawrence James Nicholas

  公开号：US20050065213A1

  公开（公告）日：2005-03-24

  Compounds are disclosed that are designed to mimic the activity of combretastatin A-4 based on chalcone, aurone, or indanone structures, or involving benzoquinone or quinone rings. The anti-cancer activity of exemplified compounds is demonstrated in a range of in vitro and in vivo assays.

  公开了一些化合物，这些化合物是基于查尔酮、金合欢素或茚酮结构设计的，或涉及苯醌或醌环，旨在模仿紫杉醇A-4的活性。在一系列体外和体内试验中，展示了这些化合物的抗癌活性。