Quinazoline compounds
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Design, synthesis, and in vitro antitumor activity of 6-aryloxyl substituted quinazoline derivatives
Quinazoline derivatives are a class of important antitumor drugs known as small molecule inhibitors that include epidermal growth factor receptor (EGFR) inhibitors. Based on the structure of poziotinib, a series of 6-aryloxyl substituted quinazoline derivatives were designed and synthesized. The molecular docking results suggested that compound 4m has different binding modes to the wild-type and mutated EGFR.
37p lyhuyenthu 31-01-2023 3 2 Download
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All the synthesized compounds were characterized by spectral studies and screened for their in vitro antibacterial activity against S. aureus and B. thuringiensis (gram positive), and E. coli and K. pneumoniae (gram negative) bacterial strains. On comparing with the standard drug gentamicin, compounds derived from 4-methoxy and 3,4,5-trimethoxy benzaldehyde, i.e. 5g and 5h, showed broad spectrum antibacterial activity and the remaining compounds showed weak to moderate activity.
10p langthannam 29-12-2021 12 0 Download
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Various thioxo-quinazolino[3,4-a]quinazolinones were prepared and evaluated for their cytotoxicity in MOLT-4 (lymphoblastic leukemia) and MCF-7 (breast adenocarcinoma) cell lines. Synthesis of the target compounds was started from isatoic anhydride. Successive reaction of isatoic anhydride with benzylamine and 2-nitrobenzaldehyde, reduction of the nitro group, and reaction with CS2 gave 12-benzyl-6-thioxo-6,7,11b,12-tetrahydro-13H-quinazolino[3,4-a]quinazolin13-one.
10p langthannam 29-12-2021 9 0 Download
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The presented work is devoted to the development of synthesis methods for novel 2-[(3-aminoalkyl-(alkaryl-, aryl-))-1H -1,2,4-triazolo]anilines. Abovementioned compounds were obtained via hydrazinolysis (Ing-Manske procedure) and acid hydrolysis of corresponding N -acylated{([1,2,4]triazolo[1,5- c ]quinazolin-2-yl)alkyl-(alkaryl-, aryl-)}amines. The regioselectivity of hydrazinolysis and hydrolysis were established. The features of spectral characteristics were studied and discussed.
10p tudichquannguyet 29-11-2021 10 1 Download
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Objectives of the dissertation: Research and synthesize and determine the hybrid compound structure containing Quinazoline frame. Research on carcinogenic activity and inhibition of acetylcholinesterase enzyme of synthetic compounds..
26p extraenglish 24-05-2021 19 3 Download
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Synthesis and structural determination of some 4-aminoquinazoline derivatives containing prop-2-yn-1-yloxy substituents at C-6 position; research and synthesize and determine the hybrid compound structure containing Quinazoline frame; research on carcinogenic activity and inhibition of acetylcholinesterase enzyme of synthetic compounds; studying protein docking and predicting the pharmacokinetic properties of some compounds that inhibit the enzyme acetylcholinesterase.
26p capheviahe27 23-02-2021 34 3 Download
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Chalcones have a place with the flavonoid family and show a few very important pharmacological activities. They can used as initial compounds for synthesis of several heterocyclic compounds. The compounds with the backbone of chalcones have been reported to possess various biological activities.
14p vijiraiya2711 27-05-2020 9 1 Download
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Although the development of antibiotic and antioxidant manufacturing, the problem of bacterial resistance and food and/or cosmetics oxidation still needs more effort to design new derivatives which can help to minimize these troubles.
15p vijiraiya2711 27-05-2020 12 1 Download
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The persistent appearance of viral strains that causes a resistant viral infection has led to continuous tri‑als for the design and development of novel antiviral compounds. Benzoquinazoline compounds have been reported to exhibit an interesting antiviral activity.
7p vijiraiya2711 27-05-2020 11 1 Download
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The quinazoline are an important class of medicinal compounds that possess a number of biological activities like anticancer, anticonvulsant and antioxidant etc.
12p vijiraiya2711 27-05-2020 10 1 Download
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Metolazone is a diuretic, saluretic and antihypertensive chemical compound from the quinazoline category that possesses medicinal features similar to those of other thiazide diuretic drugs. However, the pharmacokinetics of metolazone in the Chinese population has rarely been studied.
10p vimax2711 30-03-2020 29 1 Download
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Pyrrolo[3,4-c]pyrazole-4,6(1H,5H)-dione, pyrano[2,3-c]pyrazole-5-carbonitrile, pyrano[2,3-d]4-imidazolines, pyrido[2,1-b]benzimidazole, pyrido[2,1-b][1,3]benzoxazole, pyrido[2,1- b][1,3]benzothiazole and pyrido[2,1-b]quinazoline were synthesised from antipyrine derivatives with appropriate reagents such as maleimides, malononitrile, ethyl cyanoacetate, benzimidazole-2-acetonitrile, benzothiazole-2-acetonitrile, benzoxazol-2-acetonitrile, benzoylacetonitrile and other reagents.
8p kethamoi1 20-11-2019 8 1 Download
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Objectives of the dissertation: Research to improve the synthesis process of erlotinib hydrochloride drugs. Research on the synthesis and determination of quinazoline derivative structure. Research on the synthesis and determination of the structure of hybrid compounds of quinazoline derivatives and azides via triazole bridges.
26p xacxuoc4321 08-07-2019 30 5 Download