Design, synthesis, anti-inflammatory, analgesic screening, and molecular docking of some novel 2-pyridyl (3H)-quinazolin-4-one derivatives

Eweas, Ahmad F.; El‐Nezhawy, Ahmed O. H.; Baiuomy, Ayman R.; Awad, Mohamed M

doi:10.1007/s00044-012-0097-8

Cited by 10 publications

(5 citation statements)

References 15 publications

Supporting

Mentioning

Contrasting

Order By: Relevance

“…The anticancer activity of 1-substituted -3-(4-oxo-2-phenylquinazolin-3(4H)-yl) urea and thiourea analogues can be enhanced by making minor substitution. On the basis of literature survey and drug designing tool molecules can be further screened for anti-inflammatory, analgesic and anti-oxidant activity [28][29][30]. The results obtained following the synthetic procedures for the preparation of 1-substituted -3-(4-oxo-2-phenylquinazolin-3(4H)-yl) urea and thiourea analogues are presented in (Table 3).…”

Section: Resultsmentioning

confidence: 99%

“…SS-02 showed a significant difference in cell viability at the lowest dose tested than basal and SS-04 showed significant difference at most of the tested concentrations as compared to basal. On the basis of literature survey and drug designing tool molecules can be further screened for anti-inflammatory, analgesic and anti-oxidant activity [28][29].…”

Section: Anti-cancer Activitymentioning

confidence: 99%

See 1 more Smart Citation

Design and synthesis of novel 1-substituted -3-(4-oxo-2-phenylquinazolin-3(4H)-yl) urea and thiourea analogues targeting on TACE, as potent anticancer agents

Sandhya¹,

Snehal²,

Bansode³

2020

GSC Biol. and Pharm. Sci.

View full text Add to dashboard Cite

1-substituted phenyl quinazolinones analogues were designed by performing molecular modelling studies against tumour necrosis factor alpha converting enzyme (TACE PDB Id: 2A8H) and in-silico Lipinski properties for drug likeness. From QSAR studies, it could be concluded that the urea and thiourea groups play a crucial role in enhancing cytotoxic effects of compounds. Substitution of halogens like trifluoromethyl, chloro and allylic functional group may enhance the cytotoxic effect of urea and thiourea analogues. Substitution of phenyl and benzoyl ring were not found effective against cancer. Also, the presence of substituted aromatic ring at position 3 and methyl or thiol group at position 2 are essential for antimicrobial activities of quinazolinone. The synthesized compounds were characterized by TLC, MP, IR, NMR and Mass spectral data and were screened for their anticancer activity. The in vitro anticancer studies were performed on six selected compounds using MTT assay against MDA MB-231 cell line using paclitaxel as a standard. The synthesized 1-substituted -3-(4-oxo-2-phenylquinazolin-3(4h)-yl) urea and thiourea derivatives exhibited significant anticancer activities.

show abstract

Section: Resultsmentioning

confidence: 99%

Section: Anti-cancer Activitymentioning

confidence: 99%

Design and synthesis of novel 1-substituted -3-(4-oxo-2-phenylquinazolin-3(4H)-yl) urea and thiourea analogues targeting on TACE, as potent anticancer agents

Sandhya¹,

Snehal²,

Bansode³

2020

GSC Biol. and Pharm. Sci.

View full text Add to dashboard Cite

show abstract

“…Arbutin is also found in bearberry, strawberry, wheat, and in trace amounts in tea, coffee, red wine, and broccoli. Although the studies on bioavailability of chalcones from food sources are limited, synthetic chalcones are reported to have important and diverse pharmacological applications [26][27][28][29][30][31][32][33][34][35][36][37]. In an effort to search for novel antiglycating agents, and as a continuation of our ongoing project on the synthesis, spectral characterization, and applications of chalcone intermediates and various heterocycles [38][39][40][41][42][43], we thought it worthwhile to evaluate B-ring 4-alkoxychalcones (1)(2)(3)(4)(5)(6)(7)(8)(9)(10)(11)(12).…”

Section: Introductionmentioning

confidence: 99%

Evaluation of 4-alkoxychalcones as a new class of antiglycating agents: a combined experimental and docking study

Abbas

Kalsoom

Hadda³

et al. 2014

Res Chem Intermed

View full text Add to dashboard Cite

A series of 4-alkoxychalcones (1-12) has been evaluated for their in vitro antiglycation activity. Compound 2 (IC 50 = 89.07 ± 1.3 lM), compound 3 (IC 50 = 266.82 ± 4.6 lM), and compound 5 (IC 50 = 285.79 ± 1.9 lM) showed an excellent antiglycation potential better than the standard (rutin, IC 50 = 294.50 ± 1.5 lM). Additionally, all the compounds of this series were evaluated for their cytotoxicity against Artemia salina (brine shrimp) and one tumor cell line, namely human Prostate Cancer cell line (PC-3). All the compounds showed low toxicity against brine shrimp with LD 50 values much lower than the standard etoposide. Similarly, a much lower toxicity was observed for all the compounds against PC-3 cell line compared to doxorubicin, a standard reference drug used for this study. The molecular docking studies were also carried out to support the experimental results. A good correlation was found between experimental and theoretical results. The compounds of this series are therefore excellent antiglycating agents with no or very little cytotoxicity and represent a new class of antiglycating agents that deserve to be focused on for further research and in vivo studies in the future.

show abstract

“…They are most abundantly found trace elements present in biological systems together with iron and most of the metalloproteins have these elements [30][31][32][33]. These metal ions are nowadays present in several inorganic pharmaceuticals used as drugs against a variety of diseases, ranging from antibacterial and antifungal to anticancer applications [34][35][36][37][38][39][40][41]. In addition to that, the N-heterocycles, pyrazolones and quinazolinone derivatives as ligands affect the environment of the complex in such a way that their lipophilicity increases which is a major factor in designing a drug [42][43][44][45][46][47][48][49][50][51][52][53].…”

Section: Introductionmentioning

confidence: 99%

Metal Complexes as Potential Antimicrobial Agent: A Review

Hossain¹

2018

AJHC

View full text Add to dashboard Cite

Metal ions play many critical functions in humans. Deficiency of some metal ions can lead to disease like pernicious anemia resulting from iron deficiency, growth retardation arising from insufficient dietary zinc, and heart disease in infants owing to copper deficiency. Antibiotic resistance has been growing at an alarming rate and consequently the activity of antibiotics against Gram-negative and Gram-positive bacteria has dropped dramatically day by day. In this sense there is a strong need to synthesis new substances that not only have good spectrum of activity, but having new mechanisms of action. Inorganic compounds particularly metal complexes have played an important role in the development of new metal based drugs. A significantly rising interest in the design of metal complexes as drugs and diagnostic agents is currently observed in the area of scientific inquiry, specifically termed medicinal inorganic chemistry. In this review our main focused on research undertaken over the past few decades which has sought to possess preclinical pharmacological screenings like anti-bacterial, anti-fungal, anti-inflammatory, anti-cancer, DNA-interaction and anti-tumor action of synthetic metal complexes.

show abstract

Design, synthesis, anti-inflammatory, analgesic screening, and molecular docking of some novel 2-pyridyl (3H)-quinazolin-4-one derivatives

Cited by 10 publications

References 15 publications

Design and synthesis of novel 1-substituted -3-(4-oxo-2-phenylquinazolin-3(4H)-yl) urea and thiourea analogues targeting on TACE, as potent anticancer agents

Design and synthesis of novel 1-substituted -3-(4-oxo-2-phenylquinazolin-3(4H)-yl) urea and thiourea analogues targeting on TACE, as potent anticancer agents

Evaluation of 4-alkoxychalcones as a new class of antiglycating agents: a combined experimental and docking study

Metal Complexes as Potential Antimicrobial Agent: A Review

Contact Info

Product

Resources

About