11 p.-7 fig.-4 tab. 7 schem.
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.
This work was supported by the H2020-MSCA-ITN-2019 (860070 TUBINTRAIN), Ministerio de Ciencia e Innovación PID2019-104545RB−I00 (JFD), Proyecto de Investigación en Neurociencia Fundación Tatiana Pérez de Guzmán el Bueno 2020, and by the European Union NextGenerationEU (J.F.D.). Open Access Funding provided by $INSTITUTION within the CRUI-CARE Agreement.