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From the Insoluble Dye Indirubin towards Highly Active, Soluble CDK2‐Inhibitors
Author(s) -
Jautelat Rolf,
Brumby Thomas,
Schäfer Martina,
Briem Hans,
Eisenbrand Gerhard,
Schwahn Stefan,
Krüger Martin,
Lücking Ulrich,
Prien Olaf,
Siemeister Gerhard
Publication year - 2005
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.200400108
Subject(s) - indirubin , indigo , chemistry , combinatorial chemistry , in vitro , natural product , enzyme , biochemistry , art , visual arts
In search of novel antitumor therapies . The natural product indirubin ( 1 ) is one of the class of indigo dyes, insoluble in aqueous systems, employed by mankind since the Bronze Age for textile coloring. In 1999 indirubin was reported to be a modest inhibitor of the enzyme CDK2, a key target in the ongoing search for novel antitumor therapies. With the guidance of X‐ray structures, indirubin was transformed to yield novel, soluble, almost colorless, highly potent CDK2 inhibitors that strongly inhibit the growth of the MCF7 tumor cell line in vitro.