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Novel Bleomycin Analogues: Synthesis, Antitumor Activity, and Interaction with DNA by Zhi‐Dong Xu; Min Wang; Su‐Long Xiao; Yan‐Juan Zhang; Ming Yang is a Chemistry article available to read on EtoBox.

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## Abstract The novel analogues **11**–**16** of bleomycin A~6~ (**3**) were obtained by selective protection of the primary‐amine function of the __β__‐aminoalaninamide moiety of **3** by means of coordination with Cu^II^ ions, condensation with an aliphatic or aromatic acid R′COOH in the presence of dicyclohexylcarbodiimide, and demetalization (__Scheme__). The antitumor activity against HeLa and BGC‐823 __in vitro__, binding property with CT‐DNA, and cleavage potency towards pBR322 DNA were also studied (__Tables 1__–__3__). All the compounds **11**–**16** displayed significant antitumor activity, which was enhanced as the hydrophobicity of the C‐terminus substituent R′ increased, but decreased as the DNA‐binding affinity increased. There was a negative relationship between DNA‐cleavage potency and binding affinity to DNA in this series of compounds.

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Author

Zhi‐Dong Xu; Min Wang; Su‐Long Xiao; Yan‐Juan Zhang; Ming Yang

Publisher

John Wiley and Sons; Wiley (John Wiley & Sons); Wiley-Blackwell; Wiley (ISSN 0018-019X)

Published

2004

Language

EN

Field

Chemistry (Physical Sciences)