天然产物
微管蛋白
微管
化学
组合化学
细胞毒性
结合
表面改性
脚手架
生物物理学
立体化学
生物化学
体外
计算机科学
生物
细胞生物学
数学分析
物理化学
数据库
数学
作者
Zlata Boiarska,Helena Pérez‐Peña,Anne‐Catherine Abel,Paola Marzullo,Beatriz Álvarez‐Bernad,Francesca Bonato,Benedetta Santini,Dragos Horvath,Daniel Lucena‐Agell,Francesca Vasile,Maurizio Sironi,J. Fernando Dı́az,A.E. Prota,Stefano Pieraccini,Daniele Passarella
标识
DOI:10.1002/chem.202203431
摘要
Maytansinoids are a successful class of natural and semisynthetic tubulin binders, known for their potent cytotoxic activity. Their wider application as cytotoxins and chemical probes to study tubulin dynamics has been held back by the complexity of natural product chemistry. Here we report the synthesis of long-chain derivatives and maytansinoid conjugates. We confirmed that bulky substituents do not impact their high activity or the scaffold's binding mode. These encouraging results open new avenues for the design of new maytansine-based probes.
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