Recently the quinazoline derivatives have attracted much attention for their anticancer properties. In this study a series of new brominated quinazoline derivatives () were synthesized in two steps. In the first step we used N-bromosuccinimide to brominate the anthranilamid. Then in the second step we closed the quinazoline ring by different aromatic aldehydes. Our aldehydes contain different electron donating or electron withdrawing groups at different positions of the aromatic ring. The chemical structures of products were confirmed by spectroscopic methods such as IR, 1HNMR, 13CNMR, and mass spectroscopy. The cytotoxic activities of the compounds were assessed on three cancerous cell lines including MCF-7, A549, and SKOV3 using colorimetric MTT cytotoxic assay in comparison with cisplatin as a standard drug. Our results collectively indicated that and , exhibited the best anti-proliferative activities on three investigated cancerous cell lines.
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http://dx.doi.org/10.4103/1735-5362.253358 | DOI Listing |
Pest Manag Sci
December 2024
School of Pharmacy, Lanzhou University, Lanzhou, China.
Background: Plant diseases caused by plant pathogens pose a great threat to biodiversity and food security, and the problem of drug resistance caused by traditional antibiotics and fungicides is becoming more and more serious. It is urgent to develop new antibacterial molecules with low toxicity and high efficiency. Marinoquinoline A is an alkaloid isolated from marine actinomycetes and has a variety of pharmacological activities.
View Article and Find Full Text PDFBioorg Chem
December 2024
Department of Pharmaceutical Chemistry, Faculty of Pharmacy, Gazi University, 06330 Ankara, Türkiye. Electronic address:
Bacillus cereus sphingomyelinase C (B. cereus SMase), which plays a crucial role in bacterial virulence, has emerged as a new therapeutic target for treating opportunistic infections caused by this pathogen. It also shares catalytic domain similarity with human neutral sphingomyelinase 2 (nSMase2), which is implicated in Alzheimer's disease.
View Article and Find Full Text PDFJ Fungi (Basel)
November 2024
Department of Biosciences and Biotechnologies, Graduate School of Bioresources and Bioenvironment Sciences, Kyushu University, 744 W5-674, Motooka Nishi-ku, Fukuoka 819-0395, Japan.
(), the second most prevalent Candida pathogen globally, has emerged as a major clinical threat due to its ability to develop high-level azole resistance. In this study, two new 5,6-dihydrotetrazolo[1,5-]quinazoline derivatives ( and ) were synthesized and characterized using IR, LC-MS, H, and C NMR spectra. Along with 13 previously reported analogues, these compounds underwent in vitro antifungal testing against clinical isolates using a serial dilution method (0.
View Article and Find Full Text PDFJ Org Chem
December 2024
Chemistry and Materials Program, College of Engineering, Shibaura Institute of Technology, 3-7-5 Toyosu, Kohto-ku, Tokyo 135-8548, Japan.
Both enantiomers of 2-ethylquinazolin-4-ones bearing -CHO/CDO and CHO/CHO phenyl groups at the N3 position were prepared. These are isotopic atropisomeric compounds based on a remote and conformationally flexible H/D and C/C discrimination, and it was found that a CHCl solution of -CHO/CDO derivative shows a slight specific optical rotation. Furthermore, diastereomeric quinazolinone derivatives bearing a chiral carbon were prepared, and their stereochemical purities and rotational stability as well as the isotopic atropisomerism were verified by H NMR and chiral high-performance liquid chromatography (HPLC) analyses.
View Article and Find Full Text PDFChem Biol Drug Des
December 2024
College of Basic Medicine and Forensic Medicine, Henan University of Science and Technology, Luoyang, Henan, China.
Cervical cancer is the fourth most common cancer among women globally. Its development is closely linked to accelerated cell cycle progression and the inhibition of apoptosis in cervical cancer tissues. Gefitinib has demonstrated efficacy in inhibiting cervical cancer cells, and the 1,2,3-triazole structure is widely recognized for its role in inducing mitochondrial apoptosis in tumor cells.
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