Abstract
Some new derivatives of substituted-4(3H)-quinazolinones were synthesized and evaluated for their in vitro antitumor and antimicrobial activities. The results of this study demonstrated that compound 5 yielded selective activities toward NSC Lung Cancer EKVX cell line, Colon Cancer HCT-15 cell line and Breast Cancer MDA-MB-231/ATCC cell line, while NSC Lung Cancer EKVX cell line and CNS Cancer SF-295 cell line were sensitive to compound 8. Additionally, compounds 12 and 13 showed moderate effectiveness toward numerous cell lines belonging to different tumor subpanels. On the other hand, the results of antimicrobial screening revealed that compounds 1, 9 and 14 are the most active against Staphylococcus aureus ATCC 29213 with minimum inhibitory concentration (MIC) of 16, 32 and 32 μg/mL respectively, while compound 14 possessed antimicrobial activities against all tested strains with the lowest MIC compared with other tested compounds. In silico study, ADME-Tox prediction and molecular docking methodology were used to study the antitumor activity and to identify the structural features required for antitumor activity.
Highlights
Cancer, a continuing to be a major health problem worldwide, is the leading cause of human mortality exceeded only by cardiovascular diseases1
The results of this study demonstrated that compound 5 yielded selective activities toward NSC Lung Cancer EKVX cell line, Colon Cancer HCT-15 cell line and Breast Cancer MDA-MB-231/ATCC cell line, while NSC Lung Cancer EKVX cell line and CNS Cancer SF-295 cell line were sensitive to compound 8
Synthesis of 2-mercapto-6-methyl-3-phenylquinazolin-4(3H)-one as starting material in 90% yield was achieved by the reaction of 5-methylanthranilic acid with 2-phenylisothiocyanate in absolute ethanol25. 2-Mercapto-6-methyl-3-phenylquinazolin-4(3H)-one was reacted with ethyl 2-bromoacetate in dry acetone in the presence of potassium carbonate at room temperature to afford ethyl 2-[(6-methyl-4-oxo-3-phenyl-3,4-dihydroquinazolin-2-yl) thio]acetate (1) in 95% yield, and the latter compound was heated with hydrazine hydrate in ethanol to furnish 2-[(6-methyl4-oxo-3-phenyl-3,4-dihydroquinazolin-2-yl)thio]acetohydrazid (2) in 90% yield
Summary
A continuing to be a major health problem worldwide, is the leading cause of human mortality exceeded only by cardiovascular diseases. Several techniques have been adopted for the treatment and eradication of cancerous cells These techniques involved surgery, radiation, immunotherapy, chemotherapy and chemoprevention. The spread of antibiotic resistance among pathogenic bacteria has become a major problem for the clinical management of infectious diseases. The spread of antibiotic resistance among pathogenic bacteria has become a major problem for the clinical management of infectious diseases6 Such medical health problems have encouraged many medicinal chemists to search for Quinazolines are frequently used in medicine because of their wide spectrum of biological activities. The development of a novel and efficient anticancer agent that can be used for prophylaxis as well as the treatment of bacterial infections in cancer patients remains an important goal in medicinal chemistry
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