Design and Synthesis of New 4-(3,4,5-Trimethoxyphenyl)Thiazole–Pyrimidine Derivatives as Potential Antiproliferative Agents
A new series of 3,4,5-trimethoxyphenyl thiazole pyrimidines has been synthesized and biologically evaluated for its in vitro anticancer activity. Compounds <b>4a</b>, <b>4b</b>, and <b>4h</b> with substituted piperazine showed the best antiproliferative activity....
| Main Authors: | , , , , , , , |
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| Format: | Article |
| Language: | English |
| Published: |
MDPI AG
2023-06-01
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| Series: | Medicina |
| Subjects: | |
| Online Access: | https://www.mdpi.com/1648-9144/59/6/1076 |
| Summary: | A new series of 3,4,5-trimethoxyphenyl thiazole pyrimidines has been synthesized and biologically evaluated for its in vitro anticancer activity. Compounds <b>4a</b>, <b>4b</b>, and <b>4h</b> with substituted piperazine showed the best antiproliferative activity. In the NCI-60 cell line screening, compound <b>4b</b> showed promising cytostatic activity against multiple cell lines. Notably, it elicited a GI value of 86.28% against the NSCL cancer cell line HOP-92 at a 10 μM dose. Compounds <b>4a</b> and <b>4h</b> at 10 μM showed promising GI values of 40.87% and 46.14% against HCT-116 colorectal carcinoma and SK-BR-3 breast cancer cell lines, respectively. ADME-Tox prediction of compounds <b>4a</b>, <b>4b,</b> and <b>4h</b> revealed their acceptable drug-likeness properties. In addition, compounds <b>4a</b>, <b>4b</b>, and <b>4h</b> showed a high probability of targeting kinase receptors via Molinspiration and Swiss TargetPrediction. |
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| ISSN: | 1010-660X 1648-9144 |