{Reference Type}: Journal Article
{Title}: Total Synthesis of an Epothilone Analogue based on the Amide‒Triazole Bioisosterism.
{Author}: Colombo E;Coppini DA;Borsoi S;Fasano V;Bucci R;Bonato F;Bonandi E;Vasile F;Pieraccini S;Passarella D;
{Journal}: Chempluschem
{Volume}: 0
{Issue}: 0
{Year}: 2024 Jun 26
{Factor}: 3.21
{DOI}: 10.1002/cplu.202400413
{Abstract}: Epothilones are 16-membered macrolides that can act as microtubule-targeting agents to tackle cancer. Many synthetic analogues have been investigated for their activity, yet often based on macrolide structures. A notable exception is Ixabepilone, an azalide representing the only epothilone-like molecule approved by the FDA as a chemotherapeutic. Exploiting the amide-triazole bioisosterism, in this work we report the synthesis of the first generation of epothilones lacking the macrolide or azalide structure, with the ester or amide linkage replaced by a triazole unit. Together with the synthesis of this new analogue, computational and biological evaluations have been performed too.