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Inventi Impact: Med Chem

Articles

  • Inventi:pmc/67822/23
    Design and Synthesis of New 4-(3,4,5-Trimethoxyphenyl) Thiazole–Pyrimidine Derivatives as Potential Antiproliferative Agents
    01-Oct-2023 Research 2023 : October-December
    Ashraf K El-Damasy, Heewon Jin, Mohamed A Sabry, Hyun Ji Kim, Mohammed M Alanazi, Seon Hee Seo, Eun-Kyoung Bang, Gyochang Keum

    A new series of 3,4,5-trimethoxyphenyl thiazole pyrimidines has been synthesized and biologically evaluated for its in vitro anticancer activity. Compounds 4a, 4b, and 4h with substituted piperazine showed the best antiproliferative activity. In the NCI-60 cell line screening, compound 4b 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 4a and 4h 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 4a, 4b, and 4h revealed their acceptable drug-likeness properties. In addition, compounds 4a, 4b, and 4h showed a high probability of targeting kinase receptors via Molinspiration and Swiss TargetPrediction.

    How to Cite this Article
    Attribution/ CC Compliant Citation: El-Damasy, Ashraf K., et al. "Design and Synthesis of New 4-(3, 4, 5-Trimethoxyphenyl) Thiazole -Pyrimidine Derivatives as Potential Antiproliferative Agents." Medicina 59.6 (2023): 1076. https://doi.org/10.3390/medicina59061076 http://creativecommons.org/licenses/by/4.0/ Some formatting elements, header, footer, logos, dates and pagination were modified while adapting this article.
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