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Updated: Jun 7, 2026

Functionalized Spirocyclic Heterocycle Synthesis and Cytotoxicity Assay
Published on: February 9, 2021
Design and synthesis of macrocyclic indoles targeting blood coagulation cascade Factor XIa
Stephen Hanessian1, Andreas Larsson, Tomas Fex
1Department of Chemistry, Université de Montréal, Montréal, QC, Canada. stephen.hanessian@umontreal.ca
Abstract:
The synthesis of a series of novel macrocyclic compounds designed to target blood coagulation Factor XIa is described. The compounds were evaluated for their inhibition of a small set of serine proteases. Several compounds displayed modest activity and good selectivity for Factor XIa. Within the series, a promising lead structure for developing novel macrocyclic inhibitors of thrombin was identified.
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