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

被引：4

作者：

El-Damasy, Ashraf K. ^{[1
,2
]}

Jin, Heewon ^{[1
]}

Sabry, Mohamed A. ^{[2
]}

Kim, Hyun Ji ^{[1
]}

Alanazi, Mohammed M. ^{[3
]}

Seo, Seon Hee ^{[4
]}

Bang, Eun-Kyoung ^{[1
]}

Keum, Gyochang ^{[1
,5
]}

机构：

[1] Korea Inst Sci & Technol KIST, Brain Sci Inst, Ctr Brain Technol, Seoul 02792, South Korea

[2] Mansoura Univ, Fac Pharm, Dept Med Chem, Mansoura 35516, Egypt

[3] King Saud Univ, Coll Pharm, Dept Pharmaceut Chem, Riyadh 11451, Saudi Arabia

[4] Korea Inst Sci & Technol KIST, Brain Sci Inst, Ctr Brain Disorders, Seoul 02792, South Korea

[5] Korea Univ Sci & Technol UST, KIST Sch, Div Biomed Sci & Technol, Seoul 02792, South Korea

来源：

MEDICINA-LITHUANIA | 2023年 / 59卷 / 06期

基金：

新加坡国家研究基金会;

关键词：

trimethoxyphenyl; thiazole; pyrimidines; NCI-60; screening; NSCL cancer cell line; ADME-Tox prediction; TYROSINE KINASE INHIBITOR; BIOLOGICAL EVALUATION; CANCER; DASATINIB;

D O I：

10.3390/medicina59061076

中图分类号：

R5 [内科学];

学科分类号：

1002 ; 100201 ;

摘要：

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 & mu;M dose. Compounds 4a and 4h at 10 & mu;M 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.

引用

页数：16

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