(2S)-(1-hydroxypropyl)-pyrrolidine | 400836-64-8

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 吡咯烷类
• 英文名称: (2S)-(1-hydroxypropyl)-pyrrolidine
• 英文别名: 1-[(2S)-pyrrolidin-2-yl]propan-1-ol
• CAS: 400836-64-8
• 化学式: C₇H₁₅NO
• 分子量: 129.202
• InChiKey: LFTVAAQLOUXONP-PKPIPKONSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  0.6
• 重原子数：
  9
• 可旋转键数：
  2
• 环数：
  1.0
• sp3杂化的碳原子比例：
  1.0
• 拓扑面积：
  32.3
• 氢给体数：
  2
• 氢受体数：
  2

反应信息

• 作为产物：
  描述：

  bisebromoamide 在 sodium tetrahydroborate 、 盐酸 、 水 作用下， 以 甲醇 为溶剂， 反应 50.0h， 生成 (2S)-(1-hydroxypropyl)-pyrrolidine
  参考文献：
  名称：

  Bisebromoamide, a Potent Cytotoxic Peptide from the Marine Cyanobacterium Lyngbya sp.: Isolation, Stereostructure, and Biological Activity

  摘要：

  A novel cytotoxic peptide, termed bisebromoamide (1), has been isolated from the marine cyanobacterium Lyngbya sp. Its planar structure was determined by 1D and 2D NMR spectroscopy. The absolute stereostructure of 1 was determined by chemical degradation followed by chiral HPLC analysis. Bisebromoamide (1) exhibited potent protein kinase inhibition: the phosphorylation of ERK in NRK cells by PDGF-stimulation was selectively inhibited by treatment with 10-0.1 mu M of 1.

  DOI：

  10.1021/ol9020546

文献信息

• Revised structure and structure–activity relationship of bisebromoamide and structure of norbisebromoamide from the marine cyanobacterium Lyngbya sp.
  作者：Hiroaki Sasaki、Toshiaki Teruya、Hidesuke Fukazawa、Kiyotake Suenaga

  DOI：10.1016/j.tet.2010.11.106

  日期：2011.2

  sp. The planar structure of these peptides was elucidated through the extensive application of 1D and 2D NMR techniques. The absolute stereostructure of 1 was determined by chemical degradation followed by chiral HPLC analysis. Recently, Tao and co-workers achieved synthesis of bisebromoamide, and the configuration of thiazoline moiety was revised. We re-investigated the stereochemistry of thiazoline

  从海洋蓝藻Lyngbya sp。中分离到了新的强大的细胞毒性肽比斯溴酰胺（1）和诺溴溴酰胺（2）。这些肽的平面结构通过1D和2D NMR技术的广泛应用得以阐明。的绝对立体1用化学降解，然后通过手性HPLC分析测定的。最近，Tao和他的同事实现了比色溴酰胺的合成，并修改了噻唑啉部分的构型。我们重新研究了1的噻唑啉部分的立体化学。比西溴酰胺的结构-活性关系（1）使用天然和合成类似物进行了研究。此外，双歧溴酰胺（1）可以有效抑制蛋白激酶：用10–0.1μM的1处理可以选择性地抑制PDGF刺激NRK细胞中ERK的磷酸化。
• Estrogen receptor modulators
  申请人：DiNinno P Frank

  公开号：US20050234245A1

  公开（公告）日：2005-10-20

  The present invention relates to compounds and derivatives thereof, their cynthesis, and their use as estrogen receptor modulators. The compound of the instant invention are ligands for estrogen receptors and as such may be useful for treatment or prevention of a variety of conditions related to estrogen functioning including: bone loss, bone fractures, osteoporosis, cartilage degeneration, endometriosis, uterine fibroid desease, hot flashes, increased levels of LDL cholestterol, cardiovascular disease, impairment of cognitive functioning, cerebral degenerative disorders, restenosis, gynecomastia, vascular smooth muschle cell proliferation, obesity, incontinence, and cancer, in particular of the breast, uterus and prostate.

  本发明涉及化合物及其衍生物，它们的合成以及它们作为雌激素受体调节剂的用途。本发明的化合物是雌激素受体的配体，因此可能对与雌激素功能相关的多种疾病的治疗或预防有用，包括：骨质流失、骨折、骨质疏松症、软骨退化、子宫内膜异位症、子宫肌瘤病、潮热、低密度脂蛋白胆固醇水平增高、心血管疾病、认知功能障碍、脑退行性疾病、再狭窄、男性乳房增大、血管平滑肌细胞增殖、肥胖、失禁以及癌症，特别是乳腺、子宫和前列腺癌。
• PEPTIDIC COMPOUND AND USE OF SAME
  申请人：Suenaga Kiyotake

  公开号：US20120122797A1

  公开（公告）日：2012-05-17

  An object of the present invention is to provide a novel compound having an antitumor/anticancer effect. Specifically, the present invention provides a compound represented by Formula (I), a derivative thereof or a salt of the same. In Formula (I), R 1 represents an alkyl group, an alkenyl group, a cycloalkyl group, an amino group, a monoalkylamino group, a dialkylamino group, an aryl group, a heteroaryl group, an aralkyl group or an alkoxy group; R 2 represents a substituted or unsubstituted amino group or a substituted or unsubstituted nitrogen-containing heterocyclic group; and R 3 represents hydrogen, halogen, alkyl, methoxy, cyano, trifluoromethyl, acetylamino or amino. In Formula (I), N-Me-Ala may be substituted with N-Me-Gly, N-Me-Ser, N-Me-Thr, Ala, Gly, Ser or Thr; N-Me-Phe may be substituted with Phe, Tyr or N-Me-Tyr; and D-Leu may be substituted with L-Leu.

  本发明的目的是提供一种具有抗肿瘤/抗癌作用的新化合物。具体而言，本发明提供由式（I）表示的化合物，其衍生物或其盐。在式（I）中，R1表示烷基，烯基，环烷基，氨基，单烷基氨基，双烷基氨基，芳基，杂环芳基，芳基烷基或烷氧基；R2表示取代或未取代的氨基或取代或未取代的含氮杂环基；R3表示氢，卤素，烷基，甲氧基，氰基，三氟甲基，乙酰氨基或氨基。在式（I）中，N-Me-Ala可以被N-Me-Gly，N-Me-Ser，N-Me-Thr，Ala，Gly，Ser或Thr替代；N-Me-Phe可以被Phe，Tyr或N-Me-Tyr替代；D-Leu可以被L-Leu替代。
• Differentiation-Promoting Effects of Okeaniamides A and B from an <i>Okeania</i> sp. Marine Cyanobacterium on Preadipocytes
  作者：Kaori Ozaki、Yuka Asato、Noriyuki Natsume、Shunya Tojo、Shimpei Sumimoto、Arihiro Iwasaki、Kiyotake Suenaga、Toshiaki Teruya

  DOI：10.1021/acs.jnatprod.3c00256

  日期：2023.6.23
• US7138426B2
  申请人：——

  公开号：US7138426B2

  公开（公告）日：2006-11-21