| Autor: |
Abdullah Yahya Abdullah Alzahrani, Abdul Hameed, Abdul Rehman Khan, Julie Pelletier, Jean Sévigny, Jamshed Iqbal |
| Jazyk: |
angličtina |
| Rok vydání: |
2024 |
| Předmět: |
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| Zdroj: |
Results in Chemistry, Vol 7, Iss , Pp 101548- (2024) |
| Druh dokumentu: |
article |
| ISSN: |
2211-7156 |
| DOI: |
10.1016/j.rechem.2024.101548 |
| Popis: |
Herein, we describe the design, synthesis and biological evaluation of a series of novel non-nucleotide sulfonylurea and sulfonylthiourea based small molecule inhibitors of h-ENPP1, h-ENPP3 and e5′NT. Among the tested compounds, 3b inhibited h-ENPP1 with an IC50 value of 0.11 ± 0.01 µM. Similarly, 4b was found to be the most potent inhibitor tested against h-ENPP3 with an IC50 value of 0.038 ± 0.02 µM. Compound 3a revealed remarkable inhibitory potency against human ecto-5′-nucleotidase with an IC50 value of 0.83 ± 0.01 µM while compound 3b possessed IC50 value of 0.26 ± 0.05 µM against rat ecto-5′-nucleotidase. Antiproliferative activity of novel sulfonylurea and sulfonylthiourea derivatives was investigated on breast cancer cell line (MCF-7). Compound 4a showed anticancer activity against MCF-7 cell line with percentage inhibition of 64 and successfully arrested the viability of cancer cells. The compounds were not cytotoxic to the normal cells derived from baby hamster kidney (BHK-21). |
| Databáze: |
Directory of Open Access Journals |
| Externí odkaz: |
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