Literature DB >> 11294390

Synthesis of thiophene-2-carboxamidines containing 2-aminothiazoles and their biological evaluation as urokinase inhibitors.

K J Wilson1, C R Illig, N Subasinghe, J B Hoffman, M J Rudolph, R Soll, C J Molloy, R Bone, D Green, T Randall, M Zhang, F A Lewandowski, Z Zhou, C Sharp, D Maguire, B Grasberger, R L DesJarlais, J Spurlino.   

Abstract

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.

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Year:  2001        PMID: 11294390     DOI: 10.1016/s0960-894x(01)00102-0

Source DB:  PubMed          Journal:  Bioorg Med Chem Lett        ISSN: 0960-894X            Impact factor:   2.823


  5 in total

1.  Synthesis and antibacterial activity of novel curcumin derivatives containing heterocyclic moiety.

Authors:  Othman A Hamed; Noha Mehdawi; Adham Abu Taha; Emad M Hamed; Mohammed A Al-Nuri; Ayman S Hussein
Journal:  Iran J Pharm Res       Date:  2013       Impact factor: 1.696

2.  Synthesis of novel (E)-1-(2-(2-(4(dimethylamino) benzylidene) hydrazinyl)-4-methylthiazol-5-yl)ethanone derivatives as ecto-5'-nucleotidase inhibitors.

Authors:  Sidra Hassan; Pervaiz Ali Channar; Fayaz Ali Larik; Aamer Saeed; Hamid Saeed Shah; Joanna Lecka; Jean Sévigny; Jamshed Iqbal
Journal:  R Soc Open Sci       Date:  2018-09-12       Impact factor: 2.963

3.  N-(2,4,6-Trimethyl-phen-yl)-1,3-thia-zol-2-amine.

Authors:  Ayesha Babar; Munawar Ali Munawar; M Nawaz Tahir; Ather Farooq Khan; Muhammad Ilyas Tariq
Journal:  Acta Crystallogr Sect E Struct Rep Online       Date:  2012-07-14

4.  Synthesis and Biological Evaluation of Bisthiazoles and Polythiazoles.

Authors:  Mohammed A Al-Omair; Abdelwahed R Sayed; Magdy M Youssef
Journal:  Molecules       Date:  2018-05-10       Impact factor: 4.411

5.  Synthesis of novel thiazole, pyranothiazole, thiazolo[4,5-b]pyridines and thiazolo[5',4':5,6]pyrano[2,3-d]pyrimidine derivatives and incorporating isoindoline-1,3-dione group.

Authors:  Mona A Hosny; Yasser H Zaki; Wafaa A Mokbel; Abdou O Abdelhamid
Journal:  BMC Chem       Date:  2019-03-26
  5 in total

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