Pyrano[3,2-c]quinoline derivatives have been synthesized and utilized to obtain various new hetero-annulated triazolopyrimidine, containing quinoline, pyran, 1,2,4-triazine and pyrimidine in good yields. Newly synthesized compounds have been characterized by spectral data and elemental analysis. Most of the synthesized compounds showed moderate to weak antiproliferative activity on most cancer cell lines, especially leukemia and breast cancer cell lines. The open chain formimidic acid ethyl ester is slightly more potent than hetero-annulated systems. The most active compounds were further investigated for caspase activation, Bax activation and Bcl-2 down regulation compared to doxorubicin as a standard, and indeed exhibited mainly cell cycle arrest at the Pre-G1 and G2/M phases. The transcription effects of 5a and 5b on the p53 were assessed and compared with the reference doxorubicin. The results revealed an increase of 12–19 in p53 level compared to the test cells and that p53 protein level of 5a and 5b was significantly inductive (991, and 639 pg/mL, respectively) in relation to doxorubicin (1263 pg/mL)

吡喃并[3,2- c ]喹啉衍生物已被合成并用于获得各种新的杂环三唑并嘧啶，它们以良好的产率包含喹啉，吡喃，1,2,4-三嗪和嘧啶。新合成的化合物已通过光谱数据和元素分析进行​​了表征。大多数合成的化合物对大多数癌细胞系，尤其是白血病和乳腺癌细胞系，显示出中等至弱的抗增殖活性。开链甲亚氨酸乙酯比异环系统的效力稍强。与阿霉素相比，对最具活性的化合物的半胱天冬酶激活，Bax激活和Bcl-2下调进行了进一步研究，实际上它们主要在Pre-G1和G2 / M期表现出细胞周期停滞。的转录效应评估p53上的5a和5b并与参考阿霉素比较。结果显示，与阿霉素（1263 pg / mL）相比，与测试细胞相比，p53水平增加了12–19，而5a和5b的p53蛋白水平则具有显着诱导性（分别为991和639 pg / mL）。