Antitumor, cytotoxic, and antioxidant evaluation of six heterocyclic compounds containing different heterocycle moieties

Radwan, Tasneem Mokhtar; El‐Hashash, Maher A.; Wasfy, A. A. F.; Abdallah, S. A.

doi:10.1002/jhet.3847

Cited by 6 publications

(2 citation statements)

References 32 publications

(55 reference statements)

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“…As a reference medication, using doxorubicin (DOX), among the most powerful cancer treatments. IC 50 , or the amount of a material (in μg/mL) blocks tumour cell's ability to proliferate in 50% relative to the baseline, unexamined cells is how the activity data are expressed [ 76 ]. The estimated IC 50 values are shown in Table 6 , and they show that the studied drugs, HL and The Co(II) chelates ( 1 ), have great cytotoxic effect towards Hela cellular lines give IC 50 values of 10.14±0.7 and 19.67±2.0 μg/mL, respectively.…”

Section: Data and Analysismentioning

confidence: 99%

Synthesis, characterization, DFT calculations and biological activity of new Schiff base complexes

Alkhatib,

Alsulami

2023

Heliyon

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Section: Data and Analysismentioning

confidence: 99%

Synthesis, characterization, DFT calculations and biological activity of new Schiff base complexes

Alkhatib,

Alsulami

2023

Heliyon

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“…Such activity includes anti-fungal, anti-hypertensive, anti-microbial, anti-viral, anti-tumor, anti-convulsant, anti-inflammatory, anti-cancer, and so on. 5–10 Enzyme inhibition studies, which are important in pharmaceutical research, have led to the discovery of a wide variety of drugs that are useful in treating a number of diseases. According to recent studies, several quinazolinone derivatives with diverse side groups have anti-urease activity.…”

Section: Introductionmentioning

confidence: 99%

Synthesis of quinazolinone derivatives containing an acyl hydrazone skeleton as potent anti-urease agents enzyme kinetic studies and anti-oxidant properties

Baltaş

2022

Journal of Chemical Research

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This paper covers the synthesis, in vitro urease inhibition, enzyme kinetic parameters, and anti-oxidant studies of a novel series of quinazolinone derivatives containing an acyl hydrazone skeleton. Compounds 3a, 3b, 5a, and 5b, having IC50 values ranging from 1.86 ± 0.07 to 6.38 ± 0.11 µg mL−1, show greater inhibitory activity than the standard inhibitor, thiourea. Among the products, (2-[2-(3-methoxybenzyl)-4-oxoquinazolin-3(4 H)-yl]acetohydrazide) proves to be the most potent, exhibiting enzyme inhibition activity with an IC50 value of 1.86 ± 0.07 µg mL−1. Kinetic studies involving the Lineweaver–Burk plots reveal that the inhibition mechanism of the most active compounds (3a, 3b, 5a, and 5b) on urease activity are found to be in competitive mode. Also, the anti-oxidant activity and radical-scavenging properties of the synthesized compounds are evaluated using cupric reducing anti-oxidant activity, ferric reducing anti-oxidant capacity, 2,2′-azinobis-(3-ethylbenzothiazoline-6-sulfonic acid), and 2,2-diphenyl-1-picrylhydrazyl assays. Compounds 3a, b and 5a, b have good anti-oxidant properties and radical-scavenging activity at various final concentrations.

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Design and Synthesis of Metastable 4H‐3,1‐Benzoxazin‐4‐one and 3‐aminoquinazoline‐4(3H)‐one for Detecting Cations in Water Samples and Agricultural Crops

et al. 2021

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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...

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Antitumor, cytotoxic, and antioxidant evaluation of six heterocyclic compounds containing different heterocycle moieties

Cited by 6 publications

References 32 publications

Synthesis, characterization, DFT calculations and biological activity of new Schiff base complexes

Synthesis, characterization, DFT calculations and biological activity of new Schiff base complexes

Synthesis of quinazolinone derivatives containing an acyl hydrazone skeleton as potent anti-urease agents enzyme kinetic studies and anti-oxidant properties

Design and Synthesis of Metastable 4H‐3,1‐Benzoxazin‐4‐one and 3‐aminoquinazoline‐4(3H)‐one for Detecting Cations in Water Samples and Agricultural Crops

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