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Synthesis and Anticancer Activity of Functionalized Thieno[2,3-d]pyrimidine Compounds and Their Triazinyl and Tetrazinyl Derivatives
Russian Journal of Bioorganic Chemistry ( IF 1.1 ) Pub Date : 2020-05-01 , DOI: 10.1134/s106816202003005x
Walaa I. El-Sofany , Dalia Ahmed A. Othman , Asma M. Mahran , El-Manawaty A. May , Wael A. El-Sayed

Abstract New thienopyrimidine derivatives substituted with amino and hydrazinyl side chains were synthesized starting with 2-hydrazinyl substituted thienopyrimidine as a key compound. The newly synthesized compounds were studied for their anticancer activity against prostate cancer (PC3), lung carcinoma (A549), and hepatocellular carcinoma (HepG2) cell lines. Benzothienopyrimidine derivatives incorporating thioxoethanethioamide, pyrimidotetrazine carbothioamide, and hydrazinylglycine moieties exhibited high activities against PC3 or A549 cell lines. In addition, the thienopyrimidotriazine derivatives and their thienopyrimidinone analogues were preferentially active against the two cell lines. A number of the synthesized compounds also revealed moderate activities against PC3 and A549 cell lines.

中文翻译:

功能化噻吩并[2,3-d]嘧啶化合物及其三嗪基和四嗪基衍生物的合成及抗癌活性

摘要 以2-肼基取代的噻吩并嘧啶为关键化合物,合成了新型的氨基和肼基侧链取代的噻吩并嘧啶衍生物。研究了新合成的化合物对前列腺癌 (PC3)、肺癌 (A549) 和肝细胞癌 (HepG2) 细胞系的抗癌活性。包含硫代乙硫酰胺、嘧啶四嗪硫代酰胺和肼基甘氨酸部分的苯并噻吩并嘧啶衍生物对 PC3 或 A549 细胞系表现出高活性。此外,噻吩并嘧啶并三嗪衍生物及其噻吩并嘧啶酮类似物对两种细胞系具有优先活性。许多合成的化合物还显示出对 PC3 和 A549 细胞系的中等活性。
更新日期:2020-05-01
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