التفاصيل البيبلوغرافية
| العنوان: |
Synthesis of thiazole linked chalcones and their pyrimidine analogues as anticancer agents |
| المؤلفون: |
Chekrapani Kesari (9284751), Koteshwar Rao Rama (9284748), Khwajanezrabodin Sedighi (10131779), Jan Stenvang (584397), Fredrik Björkling (290637), Shravankumar Kankala (5962184), Niranjan Thota (7388711) |
| سنة النشر: |
2021 |
| المجموعة: |
Smithsonian Institution: Digital Repository |
| مصطلحات موضوعية: |
Biophysics, Biochemistry, Medicine, Cell Biology, Neuroscience, Pharmacology, Cancer, Environmental Sciences not elsewhere classified, Chemical Sciences not elsewhere classified, Anticancer activity, chalcone derivatives, medicinal chemistry, pyrimidines, thiazoles |
| الوصف: |
A series of nine novel thiazole linked chalcones, (E)-3-(4-methyl-2-(4(trifluoromethyl)phenyl)thiazol-5-yl)-1-phenylprop-2-en-1-one derivatives 7–15 were synthesized. To establish the structure–activity relationship (SAR), furthermore, the corresponding, ring-closed pyrimidine analogs 17–23 were synthesized. The derivatives thus obtained were evaluated for their anti-cancer activity against three genetically different colorectal cancer (CRC) cell lines. Thiazole derivatives 7, 9, and 10 showed anti-cancer activity with GI50 values ranging from 0.19 to 100 µM. Importantly, compounds 7 and 10 outperformed the standard drug cisplatin in the tested cell lines and thus show promise for further optimization. Some of pyrimidine derivatives retain activity comparable to cisplatin in the HT-29 cell line, e.g. compounds 17 and 18 with IC50 of 25 µM, however, none of these compounds demonstrated improved antiproliferative activity as compared with the starting thiazole, thus the enone linker was critical for obtaining more active compounds in this series. |
| نوع الوثيقة: |
article in journal/newspaper |
| اللغة: |
unknown |
| العلاقة: |
https://figshare.com/articles/journal_contribution/Synthesis_of_thiazole_linked_chalcones_and_their_pyrimidine_analogues_as_anticancer_agents/13920707Test |
| DOI: |
10.6084/m9.figshare.13920707.v1 |
| الإتاحة: |
https://doi.org/10.6084/m9.figshare.13920707.v1Test |
| حقوق: |
CC BY 4.0 |
| رقم الانضمام: |
edsbas.5B1C1955 |
| قاعدة البيانات: |
BASE |
