化学
广告
嘧啶
对接(动物)
组合化学
细胞周期蛋白依赖激酶2
立体化学
激酶
生物化学
蛋白激酶A
体外
医学
护理部
作者
Mohamed T. M. Nemr,Ahmed Elshewy,Mohammed L. Ibrahim,Ahmed M. El Kerdawy,Peter A. Halim
标识
DOI:10.1016/j.bioorg.2024.107566
摘要
In the current study, novel pyrazolo[3,4-d]pyrimidine derivatives 5a-h were designed and synthesized as targeted anti-cancer agents through dual CDK2/GSK-3β inhibition. The designed compounds demonstrated moderate to potent activity on the evaluated cancer cell lines (MCF-7 and T-47D). Compounds 5c and 5 g showed the most promising cytotoxic activity against the tested cell lines surpassing that of the used reference standard; staurosporine. On the other hand, both compounds showed good safety and tolerability on normal fibroblast cell line (MCR5). The final compounds 5c and 5 g showed a promising dual CDK2/GSK-3β inhibitory activity with IC
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