Design, Synthesis, and Biological Evaluation of Novel 1,3,4-Thiadiazole Derivatives as Potential Antitumor Agents against Chronic Myelogenous Leukemia [electronic resource] : Striking Effect of Nitrothiazole Moiety
- Washington, D.C. : United States. Dept. of Energy, 2017.
Oak Ridge, Tenn. : Distributed by the Office of Scientific and Technical Information, U.S. Dept. of Energy
- Physical Description:
- Article numbers 59 : digital, PDF file
- Additional Creators:
- United States. Department of Energy, Nihon Gakujutsu Shinko?kai, and United States. Department of Energy. Office of Scientific and Technical Information
- Restrictions on Access:
- Free-to-read Unrestricted online access
- In an attempt to develop potent antitumor agents, new 1,3,4-thiadiazole derivatives were synthesized and evaluated for their cytotoxic effects on multiple human cancer cell lines, including the K562 chronic myelogenous leukemia cell line that expresses the Bcr-Abl tyrosine kinase. N-(5-Nitrothiazol-2-yl)-2-((5-((4-(trifluoromethyl)phenyl)amino)-1,3,4-thiadiazol-2-yl)thio)acetamide (2) inhibited the Abl protein kinase with an IC50 value of 7.4 µM and showed selective activity against the Bcr-Abl positive K562 cell line. Furthermore, a Bcr-Abl-compound 2 molecular modelling simulation highlighted the anchoring role of the nitrothiazole moiety in bonding and hydrophobic interaction with the key amino acid residues. These results provide promising starting points for further development of novel kinase inhibitors.
- Report Numbers:
- E 1.99:1425396
- Published through SciTech Connect.
Molecules 23 1 ISSN 1420-3049 AM
Mehlika Altıntop; Halil Ciftci; Mohamed Radwan; Belgin Sever; Zafer Kaplancıklı; Taha Ali; Ryoko Koga; Mikako Fujita; Masami Otsuka; Ahmet Özdemir.
Anadolu Univ., Eskisehir (Turkey)
Kumamoto Univ. (Japan)
SLAC National Accelerator Lab., Menlo Park, CA (United States)
Anadolu Univ. Scientific Research Projects Commission (Turkey)
- Funding Information:
View MARC record | catkey: 23493068