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Synthesis and biological activity of polyalthenol and pentacyclindole analogues.

Abstract：

:A series of indole sesquiterpenes analogues of polyalthenol and pentacyclindole have been synthesized starting from ent-halimic acid in order to test their biological activity. These analogues include diverse oxidation levels at the sesquiterpenyl moiety and different functionalization on the indole ring. All synthetic derivatives were tested against a representative panel of Gram positive and Gram negative bacterial strains, and the human solid tumour cell lines A549 (non-small cell lung), HBL-100 (breast), HeLa (cervix), SW1573 (non-small cell lung), T-47D (breast) and WiDr (colon). Overall, the compounds presented activity against the cancer cell lines. The resulting lead, displaying a polyalthenol scaffold, showed GI50 values in the range 1.2-5.7 μM against all cell lines tested.

journal_name

Eur J Med Chem

journal_title

European journal of medicinal chemistry

authors

Marcos IS,Moro RF,Costales I,Basabe P,Díez D,Gil A,Mollinedo F,Pérez-de la Rosa F,Pérez-Roth E,Padrón JM

doi

10.1016/j.ejmech.2013.12.012

subject

Has Abstract

pub_date

2014-02-12 00:00:00

pages

265-79

eissn

0223-5234

issn

1768-3254

pii

S0223-5234(13)00799-X

journal_volume

73

pub_type

杂志文章

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