Search citation statements
Paper Sections
Citation Types
Year Published
Publication Types
Relationship
Authors
Journals
The behaviour of 2-benzyl-4H-3,1-benzoxazin-4-one towards nitrogen nucleophiles namely, amino acids, aromatic amines, sodium azide, and secondary amines has been investigated. Also the reaction of 3-amino-2-benzylquinazolin-4(3H)-one and 2-[2-benzyl-4-oxoquinazolin-3(4H)-yl]acetohydrazide with carbon electrophiles has been discussed. As well as The novel synthesized compounds were evaluated as chemosensor for detecting formyl, carbonyl group and revealed high-selectivity and specificity to detect metals ions in water samples and, agricultural crops. Qualitative and quantitative assays indicated appreciable selectivity of novel compounds 13 and 15 as a chemo sensor for Optical detection of Hg 2 + and Cr 2 + respectively.Recently, detecting, and quantitative determination of cations especially toxic heavy metals such as Cd 2 + , Pd 2 + , Hg 2 + , Pb 2 + , Cr 3 + , etc. by using Colorimetric sensors is one of the scientists aim in the synthetic organic chemistry, environmental, water analysis, and medical laboratories. [1][2][3][4][5][6] Among these toxicants' heavy metals, Cr 3 + and Hg 2 + ions have gotten significant attention due to their widespread pollution. [7,8] In the last decade or so, many organic chemosensors were prepared for the detection of various ions. [9][10][11][12] Herein, we will synthesis colorimetric chemosensors showing high selectivity and specificity toward toxic heavy ions present in water samples and agricultural crops namely tomatoes and courgettes. Due to their biological significance and other properties, 4H-3,1benzoxazin-4-one derivatives are vital class of compounds. [13][14][15][16][17][18][19][20] On the other hand, dynamic 4H-3,1-benzoxazin-4-one derivatives bearing saturated aliphatic substituents at site 2 such as À CH 3 , [21] À C 3 H 7 , [22] À C 3 H 7 (iso), [23,24] CH 2 COCH 3 , [25] CH 2 CN, [26] CH 2 CH 2 COOH, [27] and NHPh [28] are interesting heterocyclic derivatives of this group of compounds. The electronically unsaturated character of these rings made it easily opening and detect of nucleophile easily, (so called chemo sensors). Compounds 1a so called metastable benzoxazin-one derivative easily prepared and due to the benzyl group at the site 2 rises the electronically unsaturated character of the oxazinone ring and increases its affinity towards nucleophile. This is the target, which are wanting to prove it in this study. The other aim of this article is valuation of the synthesized compound as a chemosensor for detecting toxic ion. Quinazolinones have involved notable interest in medicinal chemistry and organic chemistry, while limited reports were achieved for checking the sensor activity of quinazolinone derivatives. Ailin Yuan et al., synthesized novel quinazolinone compound as a fluorescence sensor for the ferric ion. [29] Quinazolinone based sensors for amine vapors and Cu 2 + ion [30] have been developed. As an extension of our awareness in synthesis of quinazolinone heterocyclic, we report that some quinazolin-4(3H)-ones can be used as a simple and efficient...
The behaviour of 2-benzyl-4H-3,1-benzoxazin-4-one towards nitrogen nucleophiles namely, amino acids, aromatic amines, sodium azide, and secondary amines has been investigated. Also the reaction of 3-amino-2-benzylquinazolin-4(3H)-one and 2-[2-benzyl-4-oxoquinazolin-3(4H)-yl]acetohydrazide with carbon electrophiles has been discussed. As well as The novel synthesized compounds were evaluated as chemosensor for detecting formyl, carbonyl group and revealed high-selectivity and specificity to detect metals ions in water samples and, agricultural crops. Qualitative and quantitative assays indicated appreciable selectivity of novel compounds 13 and 15 as a chemo sensor for Optical detection of Hg 2 + and Cr 2 + respectively.Recently, detecting, and quantitative determination of cations especially toxic heavy metals such as Cd 2 + , Pd 2 + , Hg 2 + , Pb 2 + , Cr 3 + , etc. by using Colorimetric sensors is one of the scientists aim in the synthetic organic chemistry, environmental, water analysis, and medical laboratories. [1][2][3][4][5][6] Among these toxicants' heavy metals, Cr 3 + and Hg 2 + ions have gotten significant attention due to their widespread pollution. [7,8] In the last decade or so, many organic chemosensors were prepared for the detection of various ions. [9][10][11][12] Herein, we will synthesis colorimetric chemosensors showing high selectivity and specificity toward toxic heavy ions present in water samples and agricultural crops namely tomatoes and courgettes. Due to their biological significance and other properties, 4H-3,1benzoxazin-4-one derivatives are vital class of compounds. [13][14][15][16][17][18][19][20] On the other hand, dynamic 4H-3,1-benzoxazin-4-one derivatives bearing saturated aliphatic substituents at site 2 such as À CH 3 , [21] À C 3 H 7 , [22] À C 3 H 7 (iso), [23,24] CH 2 COCH 3 , [25] CH 2 CN, [26] CH 2 CH 2 COOH, [27] and NHPh [28] are interesting heterocyclic derivatives of this group of compounds. The electronically unsaturated character of these rings made it easily opening and detect of nucleophile easily, (so called chemo sensors). Compounds 1a so called metastable benzoxazin-one derivative easily prepared and due to the benzyl group at the site 2 rises the electronically unsaturated character of the oxazinone ring and increases its affinity towards nucleophile. This is the target, which are wanting to prove it in this study. The other aim of this article is valuation of the synthesized compound as a chemosensor for detecting toxic ion. Quinazolinones have involved notable interest in medicinal chemistry and organic chemistry, while limited reports were achieved for checking the sensor activity of quinazolinone derivatives. Ailin Yuan et al., synthesized novel quinazolinone compound as a fluorescence sensor for the ferric ion. [29] Quinazolinone based sensors for amine vapors and Cu 2 + ion [30] have been developed. As an extension of our awareness in synthesis of quinazolinone heterocyclic, we report that some quinazolin-4(3H)-ones can be used as a simple and efficient...
Background: Cancer exerts a huge strain on the health system. The emerging resistance to the current chemotherapies demands the continuous development of new anticancer agents with lower cost, higher efficacy, and greater specificity. Objective: Development of selective small molecules targeted anticancer agents Methods: The behavior of benzoxazinone 2 towards nitrogen nucleophiles such as hydrazine hydrate, formamide, ethanolamine, aromatic amines, and thiosemcarbazide was described. The behavior of the amino quinazolinone 3 towards carbon electrophiles and P2S5 was also investigated. The antiproliferative activity of 17 new benzoxazinone derivatives was examined against the growth of three human cancer cell lines; liver HepG2, breast MCF-7, and colon HCT-29, in addition to the normal human fibroblasts WI-38 and the selectivity index was calculated. The possible molecular pathways such as the cell cycle and apoptosis were investigated. Results: Derivatives 3, 7, 8, 10, 13, and 15 had a significant (less than 10 µM) antiproliferative activity against the three cancer cell lines investigated. Derivative 7 showed the best antiproliferative profile comparable to that of doxorubicin. The selectivity index for all the effective derivatives ranged from ~5-12 folds indicating high selectivity against the cancer cells. Derivative 15 caused ~ 7-fold and 8-fold inductions in the expression of p53 and caspase3, respectively. It also caused a ~ 60% reduction in the expression of both topoisomerase II (topoII) and cyclin-dependent kinase 1 (cdk1). Derivatives 3, 7, and 8 had a similar profile; ~ 6-8-fold increases in the expression of p53 and caspase3 but these compounds were devoid of any significant effect on the expression of topoII and cdk1. Derivatives 10 and 13 were also similar and resulted in a ~6-fold elevation in the expression of caspase3, and more than 60% downregulation in the expression of topoII. The results of the gene expression of topoII and caspase 3 were confirmed by the measurement of the topoII concentration and caspase3 activity in the HepG2 cells. Conclusion: Six derivatives exerted their antiproliferative activity by arresting the cell cycle (decreasing cdk1), preventing the DNA duplication (downregulating topo II), and by inducing apoptosis (inducing p53 and caspase3). One common feature in all the six active derivatives is the presence of free amino group. These compounds have merit for further investigations.
scite is a Brooklyn-based organization that helps researchers better discover and understand research articles through Smart Citations–citations that display the context of the citation and describe whether the article provides supporting or contrasting evidence. scite is used by students and researchers from around the world and is funded in part by the National Science Foundation and the National Institute on Drug Abuse of the National Institutes of Health.
hi@scite.ai
10624 S. Eastern Ave., Ste. A-614
Henderson, NV 89052, USA
Copyright © 2024 scite LLC. All rights reserved.
Made with 💙 for researchers
Part of the Research Solutions Family.