Synthesis,Anticancer Screening of Some Novel Trimethoxy Quinazolines and VEGFR2, EGFR Tyrosine Kinase Inhibitors Assay; Molecular Docking Studies

A new series of 8-methoxy-2-trimethoxyphenyl-3-substituted quinazoline-4(3)-one compounds were designed, synthesized, and screened for antitumor activity against three cell lines, namely, Hela, A549, and MDA compared to docetaxel as reference drug. The molecular docking was performed using Autodock Vina program and 20 ns molecular dynamics (MD) simulation was performed using GROMACS 2018.1 software. Compound 6 was the most potent antitumor of the new synthesized compounds and was evaluated as a VEGFR2 and EGFR inhibitor with (IC50, 98.1 and 106 nM respectively) compared to docetaxel (IC50, 89.3 and 56.1 nM respectively). Compounds 2, 6, 10, and 8 showed strong cytotoxic activities against the Hela cell line with IC50 of, 2.13, 2.8, 3.98, and 4.94 µM, respectively, relative to docetaxel (IC50, 9.65 µM). Compound 11 showed strong cytotoxic activity against A549 cell line (IC50, 4.03 µM) relative to docetaxel (IC50, 10.8 µM). Whereas compounds 6 and 9 showed strong cytotoxic activity against MDA cell line (IC50, 0.79, 3.42 µM, respectively) as compared to docetaxel (IC50, 3.98 µM).     

Numerical study on heat loss from the surface of solar collector tube filled by oil-NE-PCM/Al2O3 in the presence of the magnetic field

Journal of Thermal Analysis and Calorimetry - The natural convection of the oil-NE-PCM/Al2O3 inside the parabolic trough collector is studied. To simulate nanoencapsulate-phase change material...     

Design,synthesis, cytotoxicity and molecular modeling studies of some novel fluorinated pyrazole-based heterocycles as anticancer and apoptosis-inducing agents

Molecular Diversity - 3,5-Diamino-4-(3-trifluoromethylphenyldiazenyl)-1H-pyrazole was used as a starting scaffold for the synthesis of new pyrazole-based heterocycles to study their effects on the...     

The metrizability of L-topological groups

In this study, we study the metrizability of the notion of L-topological group defined by Ahsanullah 1988. We show that for any (separated) L-topological group there is an L-pseudo-metric (L-metric), in sense of Gähler which is defined using his notion of L-real numbers, compatible with the L-topology of this (separated) L-topological group. That is, any (separated) L-topological group is pseudo-metrizable (metrizable).     

Molluscicidal activity of methomyl and cardenolide extracts from Calotropis procera and Adenium arabicum against the land snail Monacha cantiana

In this work, we have evaluated the molluscicidal activity of two cardenolide extracts from Adenium arabicum Balf f. [the benzene (B) and methanol (M) extracts], one cardenolide extract from Calotropis procera (Aiton) W.T. Aiton (extract C), and methomyl against the harmful land snail Monacha cantiana (Montagu). The contact LD?? values for the above mentioned plant extracts were 12.62, 34.63, and 34.35 mg·kg?1 of body weight, respectively, while the LD?? for methomyl was 116.62 mg·kg?1, that is, the plant extracts were 9.24, 3.37, and 3.4 times more toxic than methomyl. In addition, a simple colorimetric method, based on Kedde reagent, was modified to determine cardenolide concentrations in plant extracts. Thin layer chromatography analysis (TLC) showed several cardiac glycosidal compounds in each plant extract. The results proved that cardiac glycosides are promising candidate compounds that could be used to control land snails, or exploited to develop new, effective, and environmentally friendly molluscicides.