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Development of Tailor‐Made Cytostatics Activable by Acid‐Catalyzed Hydrolysis for Selective Tumor Therapy
Author(s) -
Tietze Lutz F.,
Beller Matthias,
Fischer Roland,
Lögers Michael,
Jähde Eckhard,
Glüsenkamp KarlHeinz,
Rajewsky Manfred F.
Publication year - 1990
Publication title -
angewandte chemie international edition in english
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 5.831
H-Index - 550
eISSN - 1521-3773
pISSN - 0570-0833
DOI - 10.1002/anie.199007821
Subject(s) - catalysis , in vitro , cytotoxic t cell , chemistry , hydrolysis , cancer research , cleavage (geology) , ketone , tumor cells , methanol , biochemistry , combinatorial chemistry , medicine , biology , organic chemistry , paleontology , fracture (geology)
The diamidophosphate 1, which is hardly toxic at physiological pH (7.2) , undergoes cleavage at pH 6.2 (the pH value found in tumor cells) to glucose, methanol, and a cytotoxic ketone ( t ½ = 15 h). The survival rate of tumor cells can thereby be decreased in vitro by a factor of 5×10 4 .

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