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.
In this study, synthesised new ligand: potassium 2,2'-(quinoxaline-2,3- diyl)bis(1-phenylhydrazinecarbodithioate) (L). The ligand synthesised by reacting N1,N2-dip-tolyloxalamide as the starting material with CS2 and KOH to add the CS2 group and then with phenylendiammine to achieve (L). The ligand used in the synthesis of complexes with (CoII, NiII and CdII). The new ligand and its complexes characterised by FT-IR, UV-Vis, 1H, 13C-NMR, Mass spectroscopy, and elemental analysis, in addition to the above techniques were using magnetic moment, atomic absorption, chloride content, and melting point to describe the metal complexes.
In this work, a series of new Nucleoside analogues (D-galactopyranose linked to oxepanebenzimidazole moiety) was synthesized via multisteps synthesis. The first step involved preparation of two benzimidazoles 2-styrylbenzimidazole and 2-(phenyl ethynyl) benzimidazole via reaction of phenylenediamine with cinnamic acid or ?-phenyl propiolic acid. Electrophilic addition of the prepared benzimidazoles by three anhydrides in the second step afforded (4-6) and (14-16) which in turn were treated with 1,2,3,4-di-O-isopropylidene galactopyranose in the third step to afford a series of the desirable protected nucleoside analogues (7-9) ,(17-19)which after hydrolysis in methanolic sodium methoxidein the fourth step afforded the free nucleoside analog
... Show MoreThe synthesis and characterisation of new macrocyclic binuclear metal(II) complexes derived from dithiocarbamate (DTC) ligand are reported. The reaction of a bis-secondary amine, CS2 and KOH resulted in the formation of the free ligand. Two approaches were implemented to synthesis the macrocyclic bis(dithiocarbamate) complexes; (i) from the reaction of the free ligand with a metal ion, and (ii) via a one-pot reaction. In the free ligand approach, complexes were obtained by the reaction of dithiocarbamate salt with the metal ions; CoII, ZnII and CdII. However, the one-pot reaction is based on the mixing of the bissecondary amine, CS2, KOH and metal(II) chloride. Physico-chemical analyses were implemented to characterise the ligand and its
... Show MoreThe research study included the synthesis of a new series of heterocyclic derivatives containing the antibiotic Levofloxacin. The first way provides for the reaction of Levofloxacin with thionyl chloride in benzene as a solvent to give an acid chloride derivative. A new class of acid hydrazide synthesized from Levofloxacin was studied. Schiff bases were produced via the reaction of acid hydrazide with substituted aromatic ketones in methanol. The next stage involved the response of Schiff bases with thioglycolic acid and mono chloroacetic acid in DMF to produce derivatives of the antibiotic levofloxacin that have five heterocyclic members, including the derivatives thiazolidine-4-one and oxazolidine-5-one. The FTIR, 1HNMR, a
... Show MoreTill now, isatin derivatives have received a lot of interest in organic and medicinal chemistry due to their significant biological and pharmacological activities. Schiff’s and Mannich bases of isatins are an effective group of heterocyclic derivatives that play a significant role in medicinal chemistry as antimicrobial agents. In light of these facts, new Schiff bases and Mannich bases of isatin were synthesized. The monomer Mannich bases; 3(a-e) have been synthesized by reacting isatin with different secondary amines, piperidine, morpholine, and pyrrolidine, dimethylamine, diphenylamine, separately, and formaldehyde, while the dimer (5) formed by using piperazine and formaldehyde which then react separately with Phenylhydrazine
... Show More1,3,4-oxadizole and pyrazole derivatives are very important scaffolds for medicinal chemistry. A literature survey revealed that they possess a wide spectrum of biological activities including anti-inflammatory and antitumor effects.
To describe the synthesis and evaluation of two classes of new niflumic acid (NF) derivatives, the 1,3,4-oxadizole derivatives (compounds 3 and (4A-E) and pyrazole derivatives (compounds 5 and 6), as EGFR tyrosine kinase inhibitors in silico and in vitro.
The designed compounds were synthesized using convent