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Caffeine-hydrazones as anticancer agents with pronounced selectivity toward T-lymphoblastic leukaemia cells.

Abstract：

:We report design and synthesis of set of novel anticancer agents based on caffeine-hydrazones bearing 2-hydroxyaryl- or 2-N-heteroaryl moiety. Anticancer activity evaluation using seven cancer cell lines and two non-malignant cell lines demonstrated that several derivatives display significant anticancer activity and great selectivity index toward T-lymphoblastic leukaemia cells. In general, hydrazones bearing 2-N-heteroaryl moiety are more active and selective than those with 2-hydroxyaryl moiety. Tested compounds exhibit dose-dependent inhibition of both RNA and DNA synthesis, with some exceptions. Antimicrobial activities were tested on set of twelve bacterial and yeast strains, however prepared compounds were not active, suggesting for a molecular target specific for eukaryotic cells.

journal_name

Bioorg Chem

journal_title

Bioorganic chemistry

authors

Kaplánek R,Jakubek M,Rak J,Kejík Z,Havlík M,Dolenský B,Frydrych I,Hajdúch M,Kolář M,Bogdanová K,Králová J,Džubák P,Král V

doi

10.1016/j.bioorg.2015.03.003

subject

Has Abstract

pub_date

2015-06-01 00:00:00

pages

19-29

eissn

0045-2068

issn

1090-2120

pii

S0045-2068(15)00021-8

journal_volume

60

pub_type

杂志文章

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