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Biology‐Oriented Synthesis of a Tetrahydroisoquinoline‐Based Compound Collection Targeting Microtubule Polymerization
Author(s) -
Zimmermann Tobias J.,
Roy Sayantani,
Martinez Nancy E.,
Ziegler Slava,
Hedberg Christian,
Waldmann Herbert
Publication year - 2013
Publication title -
chembiochem
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 1.05
H-Index - 126
eISSN - 1439-7633
pISSN - 1439-4227
DOI - 10.1002/cbic.201200711
Subject(s) - noscapine , vinca , alkaloid , vinca alkaloid , colchicine , tubulin , microtubule , tetrahydroisoquinoline , stereochemistry , chemistry , hela , microtubule polymerization , biology , pharmacology , biochemistry , microbiology and biotechnology , cell , genetics , vincristine , chemotherapy , cyclophosphamide
In the third place: Inspired by the tetrahydroisoquinoline (THIQ) alkaloid noscapine, inhibitors of tubulin polymerization that bind to a site different from the colchicine and the vinca alkaloid binding sites have been synthesized. One compound is more potent than noscapine in HeLa cells and can overcome resistance to chemotherapeutics.