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Synthesis and anticancer activity of new dihydropyrimidinone derivatives.

Abstract：

:A series of dihydropyrimidinone derivatives bearing various N-heterocyclic moieties was designed and synthesized. Twelve new compounds were screened for their cytotoxic activity using 60 cancer cell lines according to NCI (USA) protocol. Compound 19 showed a significant activity against NCI-H460, SK-MEL-5, and HL-60 (TB) cell lines with growth inhibition 88%, 86% and 85%, respectively, and was found to be more safe on normal cells when compared to doxorubicin. Enzyme inhibition assay was performed for compound 19 against mTOR (IC50 = 0.64 μM) and VEGFR-2 (IC50 = 1.97 μM) to show high potency in comparison to rapamycin (IC50 = 0.43 μM) and sorafenib (IC50 = 0.3 μM) as references, respectively. Cell cycle analysis of A549 cells treated with 19 showed cell cycle arrest at G2/M phase and pro-apoptotic activity as indicated by annexin V-FITC staining.

journal_name

Eur J Med Chem

journal_title

European journal of medicinal chemistry

authors

Mostafa AS,Selim KB

doi

10.1016/j.ejmech.2018.07.004

subject

Has Abstract

pub_date

2018-08-05 00:00:00

pages

304-315

eissn

0223-5234

issn

1768-3254

pii

S0223-5234(18)30560-9

journal_volume

156

pub_type

杂志文章

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