当前位置： SCI文献检索 > BIOORGANIC CHEMISTRY期刊下所有文献 > Synthesis, cytotoxic evaluation, and molecular docking studies of novel quinazoline derivatives with benzenesulfonamide and anilide tails: Dual inhibitors of EGFR/HER2.

Synthesis, cytotoxic evaluation, and molecular docking studies of novel quinazoline derivatives with benzenesulfonamide and anilide tails: Dual inhibitors of EGFR/HER2.

Abstract：

:We synthesized a new series of 2-[(3-(4-sulfamoylphenethyl)-4(3H)-quinazolinon-2-yl)thio]anilide derivatives (2-16) and evaluated their cytotoxic activity against breast adenocarcinoma (MCF-7), colorectal adenocarcinoma (HT-29), and acute myeloid leukemia (HL-60 and K562) cells. To reveal their selectivity toward cancer cells, the compounds were also tested against the human fibroblast cell line, MRC-5. Compounds 1-5 exhibited potent cytotoxic activity against the tested cell lines with IC50 values of 0.65-3.86, 0.68-4.60, 0.41-1.45, 0.42-4.07, and 3.77-25.55 μM, respectively compared to sorafenib, the standard drug (IC50 2.50, 2.50, and 3.14 μM against MCF-7, HT-29, and HL60 cells, respectively). Interestingly, compounds 1-5 displayed selectivity toward the cancer cell lines over MRC-5 (IC50 3.77-25.55 μM). These compounds also displayed potent inhibitory activity against EGFR and HER2 kinases (IC50 0.09-0.43 and 0.15-0.33 μM, respectively) compared to the standard drug, sorafenib (IC50 0.11 and 0.13 μM, respectively). Likewise, compounds 1, 4, and 5 showed strong inhibitory activity against VEGFR2 (IC50 0.34, 0.28 and 0.39 μM, respectively) compared to sorafenib (IC50 0.17 μM). We also employed molecular docking to identify the structural features required for the EGFR/HER2 inhibitory activity of the new series. Ultimately, compounds 1, 4, and 5 were demonstrated to be candidates for further preclinical investigations.

journal_name

Bioorg Chem

journal_title

Bioorganic chemistry

authors

Alkahtani HM,Abdalla AN,Obaidullah AJ,Alanazi MM,Almehizia AA,Alanazi MG,Ahmed AY,Alwassil OI,Darwish HW,Abdel-Aziz AA,El-Azab AS

doi

10.1016/j.bioorg.2019.103461

subject

Has Abstract

pub_date

2020-01-01 00:00:00

pages

103461

eissn

0045-2068

issn

1090-2120

pii

S0045-2068(19)30853-3

journal_volume

95

pub_type

杂志文章

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