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Synthesis of Nine‐Membered, Masked Enediyne Analogues with DNA Intercalators and Its DNA Cleaving Activities
Author(s) -
Takahashi Takashi,
Tanaka Hiroshi,
Yamada Haruo,
Matsumoto Takuyuki,
Sugiura Yukio
Publication year - 1997
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.199715241
Subject(s) - enediyne , dna , chemistry , neocarzinostatin , chromophore , intercalation (chemistry) , stereochemistry , molecule , combinatorial chemistry , biochemistry , photochemistry , organic chemistry
Ten times more active in cleaving DNA than other known enediynes, these effective hybrid compounds combine the nine‐membered enediyne structure of the kedarcidin chromophore with the DNA intercalating group—a naphthoate group—of the neocarzinostatin chromophore. The precursor 1 of the active molecule is provided with a phthalate “trigger” and can generate linear DNA even in concentrations as low as 10–20μ M .