Maytansinol Derivatives: Side Reactions as a Chance for New Tubulin Binders,Chemistry - A European Journal

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Maytansinol Derivatives: Side Reactions as a Chance for New Tubulin Binders
Chemistry - A European Journal ( IF 3.9 ) Pub Date : 2021-11-17 , DOI: 10.1002/chem.202103520
Paola Marzullo ₁ , Zlata Boiarska ₁ , Helena Pérez-Peña ₁ , Anne-Catherine Abel ₂ , Beatriz Álvarez-Bernad ₃ , Daniel Lucena-Agell ₃ , Francesca Vasile ₁ , Maurizio Sironi ₁ , Karl-Heinz Altmann ₄ , Andrea E Prota ₂ , J Fernando Díaz ₃ , Stefano Pieraccini ₁ , Daniele Passarella ₁

Affiliation

Exploring the maytansinol acylation reaction, we have discovered previously unreported structural modifications of the maytansine scaffold. This permitted the synthesis and full characterization of a series of novel maytansinoids. A comprehensive biochemical evaluation and X-ray crystallography structure determinations of tubulin-maytansinoids identified potent tubulin binders. Moreover, our investigation allowed us to evaluate the impact of the structural modifications described.

中文翻译：

美登醇衍生物：副反应是新微管蛋白粘合剂的机会

探索美登醇酰化反应，我们发现了以前未报道的美登醇支架结构修饰。这使得一系列新型美登木素的合成和全面表征成为可能。微管蛋白-美登素的综合生化评估和 X 射线晶体结构测定确定了有效的微管蛋白结合剂。此外，我们的调查使我们能够评估所描述的结构修改的影响。

更新日期：2021-11-30

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