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Synthesis and in vitro antitumor evaluation of some new thiophenes and thieno[2,3-d]pyrimidine derivatives.

Abstract：

:New thiophene (2-13) and thienopyrimidine (15-27) derivatives have been synthesized. Twenty three compounds were screened against five cell lines namely; hepatocellular carcinoma (liver) HepG-2, epidermoid carcinoma (larynx) Hep-2, mammary gland (breast) MCF-7, human prostate cancer PC-3 and epithelioid cervix carcinoma HeLa. The results revealed that compounds 15,16,17,24 and 25 showed the highest antitumor activity against all tested cell lines compared to Doxorubicin. In order to explain the expected mode of action of the observed anticancer activity, compounds 15,16,17,24 and 25 were selected to screen their DNA binding affinity and enzyme inhibitory activity against DNA polymerase, thymidylate synthase and tyrosine kinase. The results revealed that the tested compounds showed good DNA binding affinity as well as good inhibitory activity against the three enzymes which might explain the observed anticancer activity of the target compounds.

journal_name

Bioorg Chem

journal_title

Bioorganic chemistry

authors

Fouad MM,El-Bendary ER,Suddek GM,Shehata IA,El-Kerdawy MM

doi

10.1016/j.bioorg.2018.09.022

subject

Has Abstract

pub_date

2018-12-01 00:00:00

pages

587-598

eissn

0045-2068

issn

1090-2120

pii

S0045-2068(18)30733-8

journal_volume

81

pub_type

杂志文章

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