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Novel 4-arylaminoquinazolines bearing N,N-diethyl(aminoethyl)amino moiety with antitumour activity as EGFRwt-TK inhibitor.

ABSTRACT: Herein, four novel 4-arylaminoquinazoline derivatives with N,N-diethyl(aminoethyl)amino moiety were designed, synthesised and evaluated on biological activities in vitro. All synthesised compounds have inhibitory effects against tumour cells (SW480, A549, A431 and NCI-H1975). In particular, 4-(3-chloro-4-(3-fluorobenzyloxy)phenylamino)-6-(5-((N,N-diethyl(aminoethyl))aminomethyl)furan-2-yl)quinazoline (6a) and 6-(5-((N,N-diethylethyl)aminomethyl)furan-2-yl)-4-(4-(E)-(propen-1-yl)phenylamino)quinazoline (6d) were potent antitumour agents which showed high antiproliferative activities against tumour cells in vitro. Moreover, compound 6a could induce late apoptosis of A549 cells at high concentrations and arrest cell cycle of A549 cells in the G0/G1 phase at tested concentrations. Also, compound 6a could inhibit the activity of wild type epidermal growth factor receptor tyrosine kinase (EGFRwt-TK) with IC50 value of 15.60?nM. Molecular docking showed that compound 6a formed three hydrogen bonds with EGFRwt-TK, while lapatinib formed only two hydrogen bonds with the receptor protein. It is believed that this work would be giving a reference for developing anti-cancer drugs targeted EGFR-TK.

SUBMITTER: Zhang Y

PROVIDER: S-EPMC6758725 | biostudies-literature | 2019 Dec

REPOSITORIES: biostudies-literature

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Novel 4-arylaminoquinazolines bearing N,N-diethyl(aminoethyl)amino moiety with antitumour activity as EGFRwt-TK inhibitor.

Zhang Yaling Y Chen Li L Li Xiabing X Gao Li L Hao Yunxia Y Li Baolin B Yan Yaping Y

Journal of enzyme inhibition and medicinal chemistry 20191201 1

Herein, four novel 4-arylaminoquinazoline derivatives with N,N-diethyl(aminoethyl)amino moiety were designed, synthesised and evaluated on biological activities in vitro. All synthesised compounds have inhibitory effects against tumour cells (SW480, A549, A431 and NCI-H1975). In particular, 4-(3-chloro-4-(3-fluorobenzyloxy)phenylamino)-6-(5-((N,N-diethyl(aminoethyl))aminomethyl)furan-2-yl)quinazoline (6a) and 6-(5-((N,N-diethylethyl)aminome ...[more]

PMID: 31530043

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Project description:Insufficient and unbalanced biomass supply inhibited soybean [Glycine max (L.) Merr.] yield formation in the maize-soybean relay strip intercropping (IS) and monoculture soybean (SS). A field experiment was conducted to explore the soybean yield increase mechanism of DA-6 in IS and SS treatments. In this 2-year experiment, compact maize "Denghai 605" and shade-tolerant soybean "Nandou 25" were selected as cultivated materials. DA-6 with four concentrations, i.e., 0 mg/L (CK), 40 mg/L (D40), 60 mg/L (D60), and 80 mg/L (D80), were sprayed on soybean leaves at the beginning of flowering stage of soybean. Results showed that DA-6 treatments significantly (p < 0.05) increased soybean grain yield, and the yield increase ratio was higher in IS than SS. The leaf area index values and net photosynthesis rate of IS peaked at D60 and were increased by 32.2-49.3% and 24.1-27.2% compared with the corresponding CK. Similarly, DA-6 treatments increased the aboveground dry matter and the amount of soybean dry matter accumulation from the R1 stage to the R8 stage (VDMT) and highest at D60 both in IS and SS. D60 increased the VDMT by 29.0-47.1% in IS and 20.7-29.2% in SS. The TR G at D60 ranged 72.4-77.6% in IS and 61.4-62.5% in SS. The MDA content at D60 treatment was decreased by 38.3% in IS and 25.8% in SS. The active grain-filling day in IS was about 7 days longer than in SS. In D60 treatment, the Vmean and Vmax increased by 6.5% and 6.5% in IS and 5.7% and 4.3% in SS compared with the corresponding CK. Although the pod number and hundred-grain weight were significantly (p < 0.05) increased by DA-6 treatments, the grains per pod were maintained stable. The pod number and hundred-grain weight were increased by 30.1-36.8% and 4.5-6.7% in IS and 6.3-13% and 3.6-5.6% in SS. Thus, the grain yield at D60 was increased by 36.7-38.4% in IS and 21.7-26.6% in SS. DA-6 treatments significantly (p < 0.05) increased soybean grain yield and peaked D60 treatments both in IS and SS.

Dataset Information

Novel 4-arylaminoquinazolines bearing N,N-diethyl(aminoethyl)amino moiety with antitumour activity as EGFRwt-TK inhibitor.

Publications

Novel 4-arylaminoquinazolines bearing <i>N</i>,<i>N</i>-diethyl(aminoethyl)amino moiety with antitumour activity as EGFR<sup>wt</sup>-TK inhibitor.

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