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Medicinal chemistry insights into novel CDC25 inhibitors.
European Journal of Medicinal Chemistry ( IF 6.7 ) Pub Date : 2020-04-26 , DOI: 10.1016/j.ejmech.2020.112374
Yucen Tao 1 , Xia Hao 1 , Xiao Ding 1 , Srinivasulu Cherukupalli 1 , Yuning Song 2 , Xinyong Liu 1 , Peng Zhan 1
Affiliation  

Cell division cycle 25 (CDC25) phosphatases, a kind of cell cycle regulators, have become an attractive target for drug discovery, as they have been found to be over-expressed in various human cancer cells. Several CDC25 inhibitors have achieved significant attention in clinical trials with possible mechanistic actions. Prompted by the significance of CDC25 inhibitors with medicinal chemistry prospect, it is an apt time to review the various drug discovery methods involved in CDC25 drug discovery including high throughput screening (HTS), virtual screening (VS), fragment-based drug design, substitution decorating approach, structural simplification approach and scaffold hopping method to seek trends and identify promising new avenues of CDC25 drug discovery.



中文翻译:

新型CDC25抑制剂的药物化学见解。

细胞分裂周期25(CDC25)磷酸酶,一种细胞周期调节剂,已成为药物发现的有吸引力的靶标,因为已发现它们在各种人类癌细胞中过表达。几种CDC25抑制剂已在临床试验中引起了广泛关注,并可能具有机械作用。CDC25抑制剂具有药用化学前景的重要性提示,现在是时候回顾涉及CDC25药物发现的各种药物发现方法,包括高通量筛选(HTS),虚拟筛选(VS),基于片段的药物设计,替代装饰方法,结构简化方法和支架跳跃方法以寻找趋势并确定CDC25药物发现的有希望的新途径。

更新日期:2020-06-27
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