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ID: ALA1147469
Journal: Bioorg Med Chem Lett
Title: Design and synthesis of de novo cytotoxic alkaloids through mimicking taxoid skeleton.
Authors: Geng X, Geney R, Pera P, Bernacki RJ, Ojima I.
Abstract: Based on a common pharmacophore model and the hypothesis that the baccatin core of taxoids is a scaffold securing the proper orientation of the side chains, a bicyclic alkaloid scaffold was designed as a baccatin surrogate. Using this scaffold, two novel macrocyclic and open-chain 'taxoid-mimicking' compounds were synthesized. Two of these 'taxoid-mimics', 2 and 3, were found to possess cytotoxicity with micromolar level IC50 values against human breast cancer cell lines.
CiteXplore: 15177459