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Design and Synthesis of New 4-(3,4,5-Trimethoxyphenyl)Thiazole-Pyrimidine Derivatives as Potential Antiproliferative Agents.

Ashraf K El-DamasyHeewon JinMohamed A SabryHyun Ji KimA F M Motiur RahmanSeon Hee SeoEun-Kyoung BangGyochang Keum
Published in: Medicina (Kaunas, Lithuania) (2023)
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.
Keyphrases
  • molecular docking
  • papillary thyroid
  • squamous cell carcinoma
  • risk assessment
  • young adults
  • human health
  • signaling pathway
  • protein kinase
  • electronic health record
  • lymph node metastasis
  • adverse drug