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Lignopurines: a new family of hybrids between cyclolignans and purines. Synthesis and biological evaluation.

Abstract：

:A new family of hybrids between cyclolignans related to podophyllic aldehyde, a non-lactonic cyclolignan, and purines were prepared and evaluated against several human tumour cell lines. Both fragments, cyclolignan and purine, were linked through aliphatic and aromatic chains. The influence on the cytotoxicity of the purine substitution and the nature of the linker is analyzed. The new family was slightly less cytotoxic than the parent podophyllic aldehyde, although the selectivity is maintained or even improved and among the linkers used, the presence of an aromatic ring gave the most potent and selective derivatives within the new series tested. Cell cycle and confocal studies demonstrate that these derivatives interfere with the tubulin polymerization and arrest cells at the G(2)/M phase, in the same way than the parent compounds podophyllotoxin and podophyllic aldehyde do.

journal_name

Eur J Med Chem

journal_title

European journal of medicinal chemistry

authors

Castro MÁ,Miguel del Corral JM,García PA,Rojo MV,Bento AC,Mollinedo F,Francesch AM,San Feliciano A

doi

10.1016/j.ejmech.2012.10.026

subject

Has Abstract

pub_date

2012-12-01 00:00:00

pages

377-89

eissn

0223-5234

issn

1768-3254

pii

S0223-5234(12)00630-7

journal_volume

58

pub_type

杂志文章

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