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

• Published in: Medicina (Kaunas, Lithuania) Vol. 59; no. 6; p. 1076
• Main Authors: El-Damasy, Ashraf K, Jin, Heewon, Sabry, Mohamed A, Kim, Hyun Ji, Alanazi, Mohammed M, Seo, Seon Hee, Bang, Eun-Kyoung, Keum, Gyochang
• Format: Journal Article
• Language: English
• Published: Switzerland MDPI AG 01.06.2023; MDPI
• Subjects: ADME-Tox prediction; Antineoplastic Agents - pharmacology; Antineoplastic Agents - therapeutic use; Breast cancer; Cancer; Care and treatment; Cell division; Cell Line, Tumor; Cell Proliferation; Chromatography; Colorectal cancer; Design; Dose-Response Relationship, Drug; Drug Screening Assays, Antitumor; Humans; Kinases; NCI-60 screening; NMR; NSCL cancer cell line; Nuclear magnetic resonance; Pyrimidines; Pyrimidines - pharmacology; Pyrimidines - therapeutic use; Solvents; Structure-Activity Relationship; thiazole; Thiazoles - pharmacology; Thiazoles - therapeutic use; trimethoxyphenyl; Tumors; South Korea; United States > US; NSCL cancer cell line; ADME-Tox prediction; trimethoxyphenyl; NCI-60 screening; pyrimidines; thiazole
• ISSN: 1648-9144; 1010-660X; 1648-9144
• DOI: 10.3390/medicina59061076

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