2-hydroxybenzene-1-sulfonyl chloride | 165661-52-9

• 分子结构分类: 有机化合物 - 苯类化合物 - 苯和取代衍生物
• 英文名称: 2-hydroxybenzene-1-sulfonyl chloride
• 英文别名: 2-hydroxy-benzenesulfonyl chloride；o-hydroxybenzenesulfonyl chloride；hydroxybenzenesulfonic chloride；2-hydroxybenzenesulfonyl chloride
• CAS: 165661-52-9
• 化学式: C₆H₅ClO₃S
• 分子量: 192.623
• InChiKey: VUGOTOYGNLHWPK-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  2.1
• 重原子数：
  11
• 可旋转键数：
  1
• 环数：
  1.0
• sp3杂化的碳原子比例：
  0.0
• 拓扑面积：
  62.8
• 氢给体数：
  1
• 氢受体数：
  3

反应信息

• 作为反应物：
  描述：

  methyl 4-(piperidin-4-yl)butanoate 、 2-hydroxybenzene-1-sulfonyl chloride 在 N,N-二异丙基乙胺 作用下， 以 四氢呋喃 为溶剂， 生成 methyl 4-(1-((2-hydroxyphenyl)sulfonyl)piperidin-4-yl)butanoate
  参考文献：
  名称：

  4-N-Hydroxy-4-[1-(sulfonyl)piperidin-4-yl]-butyramides as HDAC inhibitors

  摘要：

  A series of N-substituted 4-alkylpiperidine hydroxamic acids, corresponding to the basic structure of histone deacetylase (HDAC) inhibitors (zinc binding moiety-linker-capping group) has been previously reported by our group. Linker length and aromatic capping group connection were systematically varied to find the optimal geometric parameters. A new series of submicromolar inhibitors was thus identified, which showed antiproliferative activity on HCT-116 colon carcinoma cells.We report here the second part of the strategy used in our research group to find a new class of HDAC inhibitors, namely the SAR study for the compounds bearing a sulfonyl group on the piperidine nitrogen. In the present work, we have considered both sulfonamides and sulfonyl ureas. (C) 2011 Elsevier Ltd. All rights reserved.

  DOI：

  10.1016/j.bmcl.2011.09.042

文献信息

• [EN] SULFONAMIDES DERIVATIVES AS URAT1 INHIBITORS<br/>[FR] DÉRIVÉS SULFONAMIDES UTILISÉS EN TANT QU'INHIBITEURS D'URAT1
  申请人：PFIZER LTD

  公开号：WO2016034971A1

  公开（公告）日：2016-03-10

  The invention relates to sulfonamide derivatives, to their use in medicine, to compositions containing them, to processes for their preparation and to intermediates used in such processes. More particularly the invention relates to a sulfonamide URAT1inhibitor of formula (I), or a pharmaceutically acceptable salt thereof for use as a medicament, wherein R1, X1 and m as defined in the description, and to certain new sulfonamide URAT1 inhibitors. URAT1 inhibitors are potentially useful in the treatment of a wide range of disorders, particularly gout.

  这项发明涉及磺胺基衍生物，其在医学上的应用，含有它们的组合物，其制备方法以及用于这些方法的中间体。更具体地，该发明涉及一种磺胺基URAT1抑制剂的化学式(I)，或其药学上可接受的盐，用作药物，其中R1、X1和m如描述中所定义，并且涉及某些新的磺胺基URAT1抑制剂。URAT1抑制剂在治疗各种疾病，特别是痛风方面具有潜在的用途。
• Discovery of novel 1,3,5-triazine derivatives as potent inhibitor of cervical cancer via dual inhibition of PI3K/mTOR
  作者：Junbo Hu、Yanli Zhang、Na Tang、Yanju Lu、Peng Guo、Ziming Huang

  DOI：10.1016/j.bmc.2021.115997

  日期：2021.2

  anti-cancer activity against triple-negative breast cancer cells (MDA-MB321), human breast cancer cells (MCF-7), human cervical cancer cells (HeLa) and human liver cancer cells (HepG2), and it showed the greatest potency against HeLa cells. The effects of compound 6 h were further evaluated against the HeLa cells, where it showed significant attenuation of cell viability by inducing cell cycle arrest

  本研究描述了作为宫颈癌有效抑制剂的新型 1,3,5-三嗪衍生物的合成。最初测试这些化合物对 PI3K/mTOR 的抑制作用，显示出显着的抑制活性。针对 I 类 PI3K 同种型，例如 PI3Kα、PI3Kβ、PI3Kγ 和 PI3Kδ，对排名靠前的分子（化合物6h）进行了进一步测试，其中它对 PI3Kα 显示出最显着的活性。然后测试化合物6 h对三阴性乳腺癌细胞 (MDA-MB321)、人乳腺癌细胞 (MCF-7)、人宫颈癌细胞 (HeLa) 和人肝癌细胞 (HepG2) 的抗癌活性，它对 HeLa 细胞显示出最大的效力。化合物6 h的作用进一步针对 HeLa 细胞进行了评估，通过在 G1 期诱导细胞周期停滞，它显示出细胞活力的显着减弱。化合物6 h诱导细胞凋亡并减少 HeLa 细胞的迁移和侵袭。蛋白质印迹分析表明，6 小时抑制 PI3K 和 mTOR，并正调节 HeLa 细胞中的 Bcl-2
• [EN] CARBAMATES AS HIV PROTEASE INHIBITORS<br/>[FR] CARBAMATES INHIBITEURS DE PROTEASE DU VIH
  申请人：UNIV ILLINOIS

  公开号：WO2003078438A1

  公开（公告）日：2003-09-25

  Compounds useful for inhibiting HIV protease are disclosed. Methods of making the compounds, and their use as thereapeutic agents, for example, in treating wild-type HIV and of multidrug-resistant strains of HIV, also are disclosed.

  本发明揭示了用于抑制HIV蛋白酶的化合物。本发明还揭示了制备这些化合物的方法以及它们作为治疗剂的用途，例如用于治疗野生型HIV和多药耐药株的HIV。
• [EN] BENZOPYRANS AND PHARMACEUTICAL COMPOSITIONS CONTAINING THEM<br/>[FR] BENZOPYRANNES ET COMPOSITIONS PHARMACEUTIQUES LES CONTENANT
  申请人：NOVARTIS AG

  公开号：WO1996037490A1

  公开（公告）日：1996-11-28

  (EN) The invention provides novel 2,2-di(C1-5alkyl)- or trans-2,2-di(C1-5alkyl)-3,4-dihydro-3-hydroxy- -4-carboxamido-6-(N-arylsulfonamido)-2H-1-benzopyrans; and N-oxides, esters and salts thereof; processes for their production; and their uses as pharmaceuticals, e.g. as K+-channel openers, bronchodilators and agents for the suppression of airways hyperreactivity, e.g., for use in the treatment of asthma.(FR) Nouveaux 2,2-di(alkyle C1-5)- ou trans-2,2-di(alkyle C1-5)-3,4-dihydro-3-hydroxy-4-carboxamido-6-(N-arylsulfonamido)-2H-1-benzopyrannes et N-oxydes, esters et sels desdits benzopyrannes. La présente invention concerne en outre leur production, et leur utilisation en tant que produits pharmaceutiques, par ex. en tant qu'ouvreurs des vannes K+, bronchodilatateurs et agents de lutte contre l'hyperactivité des voies respiratoires, pour le traitement de l'asthme, par exemple.

  该发明提供了新型的2,2-二（C1-5烷基）-或反式-2,2-二（C1-5烷基）-3,4-二氢-3-羟基-4-羧酰胺基-6-（N-芳基磺酰胺基）-2H-1-苯并吡喃，并提供了其N-氧化物、酯和盐的制备方法，以及其作为制药用途的用途，例如作为K+通道开放剂、支气管扩张剂和抑制气道高反应性的药剂，例如用于哮喘的治疗。
• Pyrrolidine sulfonamides
  申请人：——

  公开号：US20040082566A1

  公开（公告）日：2004-04-29

  The present invention relates to pyrrolidine sulfonamides, pharmaceutical compositions containing them and their use as urotensin II antagonists.

  本发明涉及吡咯烷磺酰胺、含有它们的制药组合物以及它们作为尿钠肽II拮抗剂的用途。