Design, synthesis, and anticancer evaluation of acetamide and hydrazine analogues of pyrimidine,Journal of Heterocyclic Chemistry

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Design, synthesis, and anticancer evaluation of acetamide and hydrazine analogues of pyrimidine
Journal of Heterocyclic Chemistry ( IF 2.0 ) Pub Date : 2020-01-24 , DOI: 10.1002/jhet.3867
Jabeena Khazir _{1,

2} , Bilal Ahmad Mir ₃ , Gousia Chashoo ₄ , Tariq Maqbool ₅ , Darren Riley ₂ , Lynne Pilcher ₂

Affiliation

A library of acetamide and hydrazine analogues were generated on the pyrimidine ring through a multistep reaction starting from 5‐nitro‐pyrimidine‐4,6‐diol and pyrimidine‐4,6‐diol, respectively. The synthesized analogues were screened for in vitro cytotoxic activity against various human cancer cell lines like HCT‐1 and HT‐15 (colon), MCF‐7(breast), PC‐3 (prostrate), SF268 (CNS) using MTT method. From the bioassay results, it was observed that even though many of the synthesized derivatives exhibited a good potency against various screened cancer cell lines, compound 14a from the acetamide series was found to show potent anticancer activity on all the tested cancer cell lines with IC₅₀ value of 0.36μM on CNS cell line and 1.6μM on HT‐21 cell line, and compound 19xxi from hydrazine series of pyrimidine showed potent activity against three tested cancer cell lines with IC₅₀ value of 0.76μM on HT‐29 cell line, 2.6μM on HCT‐15, and 3.2μM on MCF‐7 cell line.

中文翻译：

嘧啶的乙酰胺和肼类似物的设计，合成和抗癌评估

乙酰胺和肼类似物的文库是通过从5-硝基-嘧啶-4,6-二醇和嘧啶-4,6-二醇分别开始的多步反应在嘧啶环上生成的。使用MTT方法筛选了合成的类似物对各种人类癌细胞系（如HCT-1和HT-15（结肠），MCF-7（乳腺癌），PC-3（前列腺），SF268（CNS））的体外细胞毒性活性。从生物测定结果中观察到，即使许多合成的衍生物对多种筛选的癌细胞系均显示出良好的效力，但发现乙酰胺系列化合物14a对所有测试的具有IC _50的癌细胞系均具有有效的抗癌活性。化合物19xxi在CNS细胞系上为0.36μM，在HT-21细胞系上为1.6μM嘧啶的肼系列化合物显示出对三种测试癌细胞系的有效活性，HT‐29细胞系的IC ₅₀值为0.76μM，HCT‐15细胞的IC ₅₀值为2.6μM，MCF-7细胞系的IC ₅₀为3.2μM。

更新日期：2020-01-24

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