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Selective Treatment of Hypoxic Tumor Cells In Vivo: Phosphate Pre‐Prodrugs of Nitro Analogues of the Duocarmycins
Author(s) -
Tercel Moana,
Atwell Graham J.,
Yang Shangjin,
Ashoorzadeh Amir,
Stevenson Ralph J.,
Botting K. Jane,
Gu Yongchuan,
Mehta Sunali Y.,
Denny William A.,
Wilson William R.,
Pruijn Frederik B.
Publication year - 2011
Publication title -
angewandte chemie international edition
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 5.831
H-Index - 550
eISSN - 1521-3773
pISSN - 1433-7851
DOI - 10.1002/anie.201004456
Subject(s) - prodrug , in vivo , nitro , chemistry , pharmacology , phosphate , in vitro , tumor cells , biochemistry , cancer research , biology , organic chemistry , alkyl , microbiology and biotechnology
Hitting the hypoxic target : Combining a nitro prodrug with a water‐soluble phosphate converts duocarmycin analogues from highly toxic DNA‐alkylating agents to highly selective antitumor compounds. These prodrugs (see scheme) have outstanding activity against hypoxic tumor cells in vivo, cells which are usually considered the most resistant to conventional therapy.