Aim: pyrimidine and pyrazole have various biological and pharmaceutical applications such as antibacterial, antifungal, antileishmanial, anti-inflammatory, antitumor, and anti-cancer. Introduction: In this search, the goal is to prepare pyrimidine-pyrazoles and study their anticancer activity. Methods: 1-allyl-4-oxo-6-(3,4,5-trimethoxyphenyl)-1,4-dihydropyrimidine-5-carbonitrile bearing pyrazoles (4,6-8) have been synthesized. Firstly, the reaction of 1-allyl-2-(methylthio)-4-oxo-6-(3,4,5-trimethoxyphenyl)-1,4-dihydropyrimidine-5-carbonitrile (1) with chalcones 2a-b produced the intermediates 3a-b. The latter was reacted with hydrazine hydrate to give the targets 4a-b. On the other hand, hydrazinolysis of compound 1 yielded the hydrazino derivative 5 which upon reaction with chalcones 2c-i or 1,3-bicarbonyl compounds afforded the compounds 6-8. Finally, the new compounds were characterized by spectral data (IR, 1H NMR, 13C NMR) and elemental analysis. Moreover, they were evaluated for Panc-1, MCF-7, HT-29, A-549, and HPDE cell lines as anti-cancer activity Results: All the tested compounds 3,4,6-8 showed IC50 values > 50 μg/mL against the HPDE cell line. Compounds 6a and 6e exhibited potent anticancer activity where the IC50 values in the range of 1.7-1.9, 1.4-182, 1.75-1.8, and 1.5-1.9 μg/mL against Panc-1, MCF-7, HT-29, and A-549 cell lines. Conclusion: New pyrimidine-pyrazole derivatives were simply synthesized, in addition, some of them showed potential anticancer activity.

中文翻译：

---

带有吡唑部分的新型1-烯丙基-4-氧代-6-(3,4,5-三甲氧基苯基)-1,4-二氢嘧啶-5-甲腈的设计、合成和抗癌评价

目的：嘧啶和吡唑具有多种生物和药物应用，例如抗菌、抗真菌、抗利什曼药、抗炎、抗肿瘤和抗癌。简介：本次研究的目标是制备嘧啶-吡唑并研究其抗癌活性。方法：合成了带有吡唑(4,6-8)的1-烯丙基-4-氧代-6-(3,4,5-三甲氧基苯基)-1,4-二氢嘧啶-5-甲腈。首先，1-烯丙基-2-(甲硫基)-4-氧代-6-(3,4,5-三甲氧基苯基)-1,4-二氢嘧啶-5-甲腈(1)与查耳酮2a-b反应生成中间体3a-b。后者与水合肼反应得到目标物4a-b。另一方面，化合物1的肼解产生肼基衍生物5，其与查尔酮2c-i或1,3-联羰基化合物反应后得到化合物6-8。最后，通过光谱数据（IR、1H NMR、13C NMR）和元素分析对新化合物进行了表征。此外，还评估了它们对 Panc-1、MCF-7、HT-29、A-549 和 HPDE 细胞系的抗癌活性结果：所有测试化合物 3、4、6-8 均显示 IC50 值 > 50 μg /mL 针对 HPDE 细胞系。化合物6a和6e表现出有效的抗癌活性，其中针对Panc-1、MCF-7、HT-29和A的IC50值范围为1.7-1.9、1.4-182、1.75-1.8和1.5-1.9 μg/mL -549细胞系。结论：简单地合成了新的嘧啶-吡唑衍生物，并且其中一些衍生物表现出潜在的抗癌活性。