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Hybrid compounds with two redox centres: modular synthesis of chalcogen-containing lapachones and studies on their antitumor activity.

Abstract：

:Chalcogen-containing β-lapachone derivatives were synthesized using a straightforward methodology and evaluated against several cancer cell lines (leukaemia, human colon carcinoma, prostate, human metastatic prostate, ovarian, central nervous system and breast), showing, in some cases, IC50 values below 1 μM. The cytotoxic potential of the lapachones evaluated was also assayed using non-tumor cells: human peripheral blood mononuclear cells, two murine fibroblast lines (L929 and V79 cells) and MDCK (canine kidney epithelial cells). These compounds could provide promising new lead derivatives for anticancer drug development. This manuscript reports important findings since few authors have described C-3 substituted β-lapachone with potent antitumor activity. The methodology employed allowed the preparation of the compounds from lapachol within a few minutes in a green approach.

journal_name

Eur J Med Chem

journal_title

European journal of medicinal chemistry

authors

Vieira AA,Brandão IR,Valença WO,de Simone CA,Cavalcanti BC,Pessoa C,Carneiro TR,Braga AL,da Silva EN

doi

10.1016/j.ejmech.2015.06.044

subject

Has Abstract

pub_date

2015-08-28 00:00:00

pages

254-65

eissn

0223-5234

issn

1768-3254

pii

S0223-5234(15)30119-7

journal_volume

101

pub_type

杂志文章

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