cas 117174-87-5, 1-(2,4,5-TRIMETHYLPHENYL)-2-THIOUREA | Articles data ｜lookchem

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117174-87-5

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Synthesis of thiophene-2-carboxamidines containing 2-aminothiazoles and their biological evaluation as urokinase inhibitors
The serine protease urokinase (uPa) has been implicated in the progression of both breast and prostate cancer. Utilizing structure based design, the synthesis of a series of substituted 4-[2-amino-1,3-thiazolyl]-thiophene-2-carboxamidines is described. Further optimization of this series by substitution of the terminal amine yielded urokinase inhibitors with excellent activities.
Wilson, Kenneth J.,Illig, Carl R.,Subasinghe, Nalin,Hoffman, James B.,Jonathan Rudolph,Soll, Richard,Molloy, Christopher J.,Bone, Roger,Green, David,Randall, Troy,Zhang, Marie,Lewandowski, Frank A.,Zhou, Zhao,Sharp, Celia,Maguire, Diane,Grasberger, Bruce,DesJarlais, Renee L.,Spurlino, John
p. 915 - 918
(2007/10/03)

Improved Procedures for the Preparation of Cycloalkyl-, Arylalkyl-, and Arylthioureas
An improved procedure for the preparation of arylthioureas consists of the reaction of benzoyl isothiocyanate with anilines in acetone and debenzoylation of the resultant N-aryl-N'-benzoylthioureas with 5percent aqueous sodium hydroxide.Bicycloalkylthioureas and N-(arylalkyl)thioureas (e.g. 9H-9-fluorenylthiourea) are directly prepared from the corresponding isothiocyanates and ammonia.
Rasmussen, C. R.,Villani, F. J.,Weaner, L. E.,Reynolds, B. E.,Hood, A. R.,et al.
p. 456 - 459
(2007/10/02)

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Chemical Properties

Melting Point: 160-162 °C
Boiling Point: 307.8 °C at 760 mmHg
Flash Point:139.9 °C
Density: 1.167 g/cm³
Vapor Pressure: 0.00071mmHg at 25°C
Refractive Index: 1.656
PKA: 13.41±0.70(Predicted)
PSA: 70.14000
LogP: 3.04060

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