Biology-oriented synthesis of a tetrahydroisoquinoline-based compound collection targeting microtubule polymerization.
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.
Max Planck Institute of Molecular Physiology, Department of Chemical Biology, Otto-Hahn-Strasse 11, 44227 Dortmund, Germany.
Tobias J
TJ
Zimmermann
Sayantani
S
Roy
Nancy E
NE
Martinez
Slava
S
Ziegler
Christian
C
Hedberg
Herbert
H
Waldmann
D001665:Binding Sites; D002460:Cell Line; D049109:Cell Proliferation / Q000187:drug effects; D020090:Chromosome Segregation / Q000187:drug effects; D006367:HeLa Cells; D006801:Humans; D008870:Microtubules / Q000378:metabolism*; D008941:Spindle Apparatus / Q000187:drug effects / Q000378:metabolism; D013237:Stereoisomerism; D044005:Tetrahydroisoquinolines / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology; D050257:Tubulin Modulators / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology
D044005:Tetrahydroisoquinolines; D050257:Tubulin Modulators