支架跳跃已成为丰富小分子抗肿瘤药物合成库的​​实用策略。具体来说，它使化学家能够改进先导化合物的药效学、药代动力学和理化性质。支架跳跃开辟了已建立的专利化学领域之外的新分子领域。作者在这篇综述中提出了基于支架跳跃的双抑制抗肿瘤结构模板的药物设计策略。微小的修改、结构的刚性化和简化（闭环和开环）以及彻底的结构检修是药物化学家用来生成双功能抑制剂库的策略。此外，该综述还概述了支架跳跃（软件和程序）的计算方法和用于合成通过支架跳跃设计的模板的有机钯催化。药物化学家在提供双抑制抗肿瘤化学结构方面表现出了非凡的能力。基于支架跳跃的药物设计策略已经产生了大量药效学优越的双重调节抗肿瘤药物。需要一种涉及计算进步、合成方法进步和传统药物设计策略的综合方法来增加支架跳跃辅助药物发现活动的数量。

Scaffold hopping has emerged as a practical tactic to enrich the synthetic bank of small molecule antitumor agents. Specifically, it enables the chemist to refine the lead compound's pharmacodynamic, pharmacokinetic, and physiochemical properties. Scaffold hopping opens up fresh molecular territory beyond established patented chemical domains.The authors present the scaffold hopping-based drug design strategies for dual inhibitory antitumor structural templates in this review. Minor modifications, structure rigidification and simplification (ring-closing and opening), and complete structural overhauls were the strategies employed by the medicinal chemist to generate a library of bifunctional inhibitors. In addition, the review presents an overview of the computational methods of scaffold hopping (software and programs) and organopalladium catalysis leveraged for the synthesis of templates designed via scaffold hopping.The medicinal chemist has demonstrated remarkable prowess in furnishing dual inhibitory antitumor chemical architectures. Scaffold hopping-based drug design strategies have yielded a plethora of pharmacodynamically superior dual modulatory antitumor agents. An integrated approach involving computational advancements, synthetic methodology advancements, and conventional drug design strategies is required to increase the number of scaffold-hopping-assisted drug discovery campaigns.