14770-84-4Relevant academic research and scientific papers
Synthesis and evaluation of new 2-aminothiophenes against: Mycobacterium tuberculosis
Thanna, Sandeep,Knudson, Susan E.,Grzegorzewicz, Anna,Kapil, Sunayana,Goins, Christopher M.,Ronning, Donald R.,Jackson, Mary,Slayden, Richard A.,Sucheck, Steven J.
, p. 6119 - 6133 (2016/07/06)
Tuberculosis (TB) and its drug resistant forms kills more people than any other infectious disease. This fact emphasizes the need to identify new drugs to treat TB. 2-Aminothiophenes (2AT) have been reported to inhibit Pks13, a validated anti-TB drug target. We synthesized a library of 42 2AT compounds. Among these, compound 33 showed remarkable potency against Mycobacterium tuberculosis (Mtb) H37RV (MIC = 0.23 μM) and showed an impressive potency (MIC = 0.20-0.44 μM) against Mtb strains resistant to isoniazid, rifampicin and fluoroquinolones. The site of action for the compound 33 is presumed to be Pks13 or an earlier enzyme in the mycolic acid biosynthetic pathway. This inference is based on structural similarity of the compound 33 with known Pks13 inhibitors, which is corroborated by mycolic acid biosynthesis studies showing that the compound strongly inhibits the biosynthesis of all forms of mycolic acid in Mtb. In summary, these studies suggest 33 represents a promising anti-TB lead that exhibits activity well below toxicity to human monocytic cells.
Discovery of a novel class of 2-ureido thiophene carboxamide checkpoint kinase inhibitors
Janetka, James W.,Almeida, Lynsie,Ashwell, Susan,Brassil, Patrick J.,Daly, Kevin,Deng, Chun,Gero, Thomas,Glynn, Roberta E.,Horn, Candice L.,Ioannidis, Stephanos,Lyne, Paul,Newcombe, Nicholas J.,Oza, Vibha B.,Pass, Martin,Springer, Stephanie K.,Su, Mei,Toader, Dorin,Vasbinder, Melissa M.,Yu, Dingwei,Yu, Yan,Zabludoff, Sonya D.
scheme or table, p. 4242 - 4248 (2009/04/10)
Checkpoint kinase-1 (Chk1, CHEK1) is a Ser/Thr protein kinase that mediates the cellular response to DNA-damage. A novel class of 2-ureido thiophene carboxamide urea (TCU) Chk1 inhibitors is described. Inhibitors in this chemotype were optimized for cellular potency and selectivity over Cdk1.
SUBSTITUTED HETEROCYCLES AND THE USES THEREOF
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Page/Page column 55, (2010/02/12)
This invention relates to novel compounds having the structural formula (I) and to their pharmaceutical compositions and to their methods of use. These novel compounds provide a treatment or prophylaxis of cancer.
