Background: Chemotherapeutic medication treatment for cancer is typically used in conjunction with other techniques as part of a routine regimen. It is well established that the capacity of different chemotherapeutic drugs to induce apoptosis is correlated with their anticancer efficacy. Quinazolinone-based drugs have demonstrated excellent responses from several cancer cell types. These substances have a lot of potential for use as building blocks in the creation of apoptosis inducers. Objective: To assess the new quinazolinone derivatives (M1 and M2) that were recently synthesized for their potential to halt wound healing and to use the acridine orange/propidium iodide (AO/PI) double stain to assess their capacity to induce apoptosis in the chosen cancer cell lines. Methods: Using the breast carcinoma cell line (MCF-7) and the lung adenocarcinoma cell line (A549), two quinazolinone derivatives (M1 and M2) were investigated for their capacity to inhibit wound healing and induce apoptosis. Results: In both cell lines, the chemicals were found to be effective inducers of apoptosis and to considerably limit wound healing. Conclusions: In cancer cell lines (MCF-7 and A549), compounds M1 and M2 efficiently inhibited wound repair and triggered apoptosis.
Background: Isoxazoles are an important class of five-membered unsaturated heterocyclic compounds. They show several applications in diverse areas such as pharmaceuticals, agrochemistry and industry. Isoxazoles are also found in natural sources showing insecticidal, plant growth regulation and pigment functions. Current study was conducted for synthesis of twenty five new Isoxazole derivatives and to evaluate the in vitro antibacterial activities of these derivatives. Methods: Benzaldoxime and their substituted [I] ae were prepared via addition-elimination reactions between aromatic aldehyde and hydroxylamine hydrochloride. In a second step, para-or meta-substituted benzaldoximes [I] ae were reacted with N-chlorosucceinimide in DMF to yield
... Show MoreIn this research , phthallic anhydride ring is opened with 4-methyl aniline and acetone as a solvent to results the compound [I] that reacted with dimethyl sulphate and anhydrous sodium carbonate formation to phathalate ester [II], while the acid hydrazide compound [III], was obtained from mixed the compound [II]with hydrazine hydrate, Synthesis four type of shiff bases[IV]a-d was synthesized from the reaction of acid hydrazide [III] with aromatic aldehyde or ketone , when reacted Shiff bases with phthalic anhydride or naphthalicanhydride,I get eight derivatives of oxazepine [V]a-d , [VI]a-d. The bacterial activity of the new compounds studied by four species of bacteria: Esherichia Coli, Enterobactecloacae (Gram negative) and staphylococcu
... Show MoreA novel series of chitosan derivatives were synthesized via reaction of chitosan with carbonyl compounds and grafted it’s by with different amine compounds substituted hydrogen. The produced polymers were characterized by different analyses FTIR, 1HCNMR, XRD, DSC and TGA. Solubility in water as well as many solvent was investigated, antibacterial activity of chitosan and its derivatives against two types of bacteria E. coli and S. aureus was also investigated. The results showed that derivatives sort of have antibacterial activities against Esherichia coli (Gram negative) better than chitosan whilst compound IX has better antibacterial against Staphylococcus aureus (Gram positive). SEM analysis showed that increase of surface roughness wi
... Show MoreThe formation and structural investigation of three new Mannich bases are reported. The synthesis of these compounds was accomplished via a multicomponent one-pot reaction using CaCl2 as a catalyst. The reaction of the benzaldehyde, m-bromoaniline and cyclohexanone or 4-methylcyclohexanone resulted in the formation of L1 and L3, respectively. The synthesis of L2 was achieved by mixing benzaldehyde, o-bromoaniline and cyclohexanone. The isolated compounds were characterised using a range of analytical and spectroscopic techniques. These include; NMR (1H and 13C-NMR), ESMS, FTIR, electronic spectroscopy, microanalyses and melting points. The NMR data for L1 and L2 indicated the presence of one isomer in solutions, on the NMR time scale. How
... Show MoreAlteration in the backbone structure of the endogenously released opioid peptides Leu5/Met5 enkephalins may result in compounds having comparable profile of pharmacological activity but with different physicochemical properties and side effects. Phthalyl amino acid and phthalyl esters are among the derivatives that have been synthesized and evaluated for their antibacterial and antifungal activities.This study was conducted to evaluate the possible analgesic activity of phthalyl-tyrosyl-glycin sodium that has been recently synthesized by our team.The study was carried out on 24 albino mice using hot plate method. The animals were allocated in to three groups; the first group received saline and represent a control g
... Show MoreIn recent years, infectious diseases are increasingly being encountered in clinical settings. Due to the development of antibiotic resistance and the outbreak of these diseases caused by resistant pathogenic bacteria, the pharmaceutical companies and the researchers are now searching for new unconventional antibacterial agents. Recently, in this field, the application of nanoparticles is an emerging area of nanoscience and nanotechnology. For this reason, nanotechnology has a great deal of attention from the scientific community and may provide solutions to technological and environmental challenges. A common feature that these nanoparticles exhibit their antimicrobial behavior against pathogenic bacteria. In this report, we evaluate
... Show MoreSchiff bases of Ceftizoxime sodium were synthesized in an attempt to improve the antimicrobial spectrum of Ceftizoxime. Aminothiazole ring of Ceftizoxime is linked directly through an imino group to different aromatic aldehydes reacted by nucleophilic addition using trimethylamine (TEA), as a catalyst and refluxed in methanol. The antimicrobial activity was evaluated for such Schiff bases using disc diffusion method. Molecular docking was conducted on certain penicillin-binding proteins (PBPs) and carboxypeptidases using 1- click docking software. Schiff bases of Ceftizoxime were prepared with reasonable yields and their chemical structures were confirmed by spectral analysis (FTIR, 1H-NMR) and elemental microanalysis (CHNS). The antibacter
... Show MoreTo synthesize new hydrazone derivatives of naproxen with enhanced anti-inflammatory activity and devoid the ulcerogenic side effects. Hydrazones were synthesized by conjugation of naproxen hydrazide with seven natural and synthetic aldehyde and ketone by using glacial acetic acid as catalyst. The synthesis has been carried out following simple methodology in excellent isolated yields.The structure of the synthesized derivatives has been characterized by elemental microanalysis (CHN), FTIR Spectroscopy, and other physicochemical properties.The anti- inflammatory activity of the synthesized compounds was evaluated in vivo using the egg-white induced edema model in rats, and the results of the biological assay was found to be comparable to Nap
... Show MoreBreast cancer (BC) is the most common malignant tumor in women and the leading cause of cancer deaths worldwide. This work was conducted to estimate the roles of oxidative stress, vitamin B12, homocysteine (HCY), and DNA methylation in BC disease progression. Sixty BC patients (age range 33–80 years) and 30 healthy controls were recruited for this study. Patients with BC were split to group 1 consisted of stage II BC women (low level), and group 2 consisted of patients in stages III and IV (high level). Malondialdehyde (MDA), glutathione peroxidase 3 (GPX3), HCY, and vitamin B12 levels in the study groups were measured. Also, the 5-methylcytosine (5mC) global DNA methylation levels were evaluated. The results showed a significant
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