4-prop-2-ynoxy-N-(4H-thiochromeno[4,3-d][1,3]thiazol-2-yl)benzamide | 1431658-51-3

• 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: 4-prop-2-ynoxy-N-(4H-thiochromeno[4,3-d][1,3]thiazol-2-yl)benzamide
• CAS: 1431658-51-3
• 化学式: C₂₀H₁₄N₂O₂S₂
• 分子量: 378.475
• InChiKey: WAMZWZSSDBRKFW-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  4
• 重原子数：
  26
• 可旋转键数：
  4
• 环数：
  4.0
• sp3杂化的碳原子比例：
  0.1
• 拓扑面积：
  105
• 氢给体数：
  1
• 氢受体数：
  5

反应信息

• 作为产物：
  描述：

  4-(prop-2-ynyloxy)benzoic acid 、 4H-苯并噻喃并[4,3-d]噻唑-2-胺 在 N,N-二异丙基乙胺 作用下， 以 N,N-二甲基甲酰胺 为溶剂， 反应 14.0h， 以81%的产率得到4-prop-2-ynoxy-N-(4H-thiochromeno[4,3-d][1,3]thiazol-2-yl)benzamide
  参考文献：
  名称：

  Tricyclic thiazoles are a new class of angiogenesis inhibitors

  摘要：

  Tricyclic thiazoleamine derivatives that were identified as hits in a screen against human umbilical vein endothelial cell proliferation were subjected to a structure-activity relationship study. Two structurally superimposable scaffolds-4H-thiochromeno[4,3-d]thiazol-2-amine and 5,6-dihydro-4H-benzo[6,7]cyclo hepta[1,2-d] thiazol-2-amine derivatives-yielded low-micromolar inhibitors, and two among them 37 and 43 also exhibited antiangiogenic activity in an endothelial tube formation assay. Thus, 37 and 43 can serve as leads to develop a novel class of antiangiogenic agents. (C) 2013 Elsevier Ltd. All rights reserved.

  DOI：

  10.1016/j.bmcl.2013.02.067

文献信息

• Tricyclic thiazoles are a new class of angiogenesis inhibitors
  作者：Shridhar Bhat、Joong Sup Shim、Jun O. Liu

  DOI：10.1016/j.bmcl.2013.02.067

  日期：2013.5

  Tricyclic thiazoleamine derivatives that were identified as hits in a screen against human umbilical vein endothelial cell proliferation were subjected to a structure-activity relationship study. Two structurally superimposable scaffolds-4H-thiochromeno[4,3-d]thiazol-2-amine and 5,6-dihydro-4H-benzo[6,7]cyclo hepta[1,2-d] thiazol-2-amine derivatives-yielded low-micromolar inhibitors, and two among them 37 and 43 also exhibited antiangiogenic activity in an endothelial tube formation assay. Thus, 37 and 43 can serve as leads to develop a novel class of antiangiogenic agents. (C) 2013 Elsevier Ltd. All rights reserved.