新型吡唑并[3,4-d]嘧啶衍生物的设计、合成与抗肿瘤评价
Design, Synthesis, and Antitumor Evaluation of Novel Pyrazolo[3,4-d]pyrimidine Derivatives.
作者信息
Kandeel Manal M, Mohamed Lamia W, Abd El Hamid Mohammed K, Negmeldin Ahmed T
机构信息
Pharmaceutical Organic Chemistry Department, Faculty of Pharmacy, Cairo University, Cairo, Egypt.
出版信息
Sci Pharm. 2012 Jul-Sep;80(3):531-45. doi: 10.3797/scipharm.1204-23. Epub 2012 Jun 25.
A new series of pyrazolo[3,4-d]pyrimidines has been synthesized. The new compounds were tested for their antitumor activity on 60 different cell lines, and some of the compounds were found to have potent antitumor activity. In particular, 2-hydroxybenzaldehyde [1-(4-chlorophenyl)-3-methyl-1H-pyrazolo-[3,4-d]pyrimidin-4-yl]hydrazone (VIIa) was found to be the most effective among the other derivatives, showing IC50 values of 0.326 to 4.31 μM on 57 different cell lines.
已合成了一系列新的吡唑并[3,4 - d]嘧啶。对这些新化合物在60种不同细胞系上进行了抗肿瘤活性测试，发现其中一些化合物具有强效抗肿瘤活性。特别是，发现2 - 羟基苯甲醛[1 - (4 - 氯苯基)-3 - 甲基 - 1H - 吡唑并[3,4 - d]嘧啶 - 4 - 基]腙（VIIa）在其他衍生物中最为有效，在57种不同细胞系上显示出0.326至4.31μM的IC50值。
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