新型吡唑并嘧啶和吡唑并喹唑啉的设计、合成与抗肿瘤活性评价。

Chemistry Department, Faculty of Sciences, University of Sharjah, Sharjah 27272, UAE.

Organometallic and Organometalloid Chemistry Department, National Research Centre, Dokki, Cairo 12622, Egypt.

Molecules. 2018 May 23;23(6):1249. doi: 10.3390/molecules23061249.

A series of -aryl-7-aryl-pyrazolo[1,5-]pyrimidines ⁻ and -aryl-pyrazolo[1,5-]quinazolines ⁻ were designed and synthesized via the reaction of 5-aminopyrazoles ⁻ with enaminones ⁻ or , respectively. The new compounds were screened for their in vitro antitumor activity toward liver (HepG-2) and breast (MCF-7) human cancer cells using 3-[4,5-dimethyl-2-thiazolyl)-2,5-diphenyl-2-tetrazolium bromide MTT assay. From the results, it was found that all compounds showed dose-dependent cytotoxic activities against both HepG-2 and MCF-7 cells. Two compounds and were selected for further investigations. Cell cycle analysis of liver (HepG-2) cells treated with and breast (MCF-7) cells treated with showed cell cycle arrest at G2/M phase and pro-apoptotic activity as indicated by annexin V-FITC staining.

通过 5-氨基吡唑与烯胺酮或反应，设计并合成了一系列 -芳基-7-芳基-吡唑并[1,5-a]嘧啶和 -芳基-吡唑并[1,5-a]喹唑啉。使用 3-[4,5-二甲基-2-噻唑基)-2,5-二苯基-2-四唑溴化 MTT 测定法，对新化合物进行了体外抗肝癌（HepG-2）和乳腺癌（MCF-7）人癌细胞的活性筛选。结果发现，所有化合物对 HepG-2 和 MCF-7 细胞均显示出剂量依赖性细胞毒性活性。选择了两种化合物和进行进一步研究。用和处理肝癌（HepG-2）细胞和乳腺癌（MCF-7）细胞的细胞周期分析表明，细胞周期停滞在 G2/M 期，并表现出凋亡活性，如 Annexin V-FITC 染色所示。