5-Fluorouracil is one of the commonly used chemotherapy drugs in anticancer therapy; unfortunately treatment with 5-FU by solely has many drawbacks low lipophilicity, low permeability, low molecular weight, and its relatively poor plasma protein binding; also a brief half-life therefore frequent administration is required to maintain the optimal therapeutic plasma level which in addition to its poor selectivity, drug resistance and limited penetration to cancer cells; leads to increased incidence of side-effects to healthy cells/tissues and low response rates. In order to minimize these drawbacks; 5-FU was chemically conjugated with pyrrolidine dithiocarbamate (PDTC) in a mutual prodrug moiety (S-(9H-purin-6-yl) 3-((pyrrolidine-1-carbonothioyl)thio)propanethioate) "compound [IV]" with (chloroacetic acid) and (chloroethanol) being the linkers ;synthesized prodrug and intermediates were characterized and identified using FTIR ,1H NMR and all the results shown good agreements with the proposed chemical structures of the synthesized compounds. ; in-vitro preliminary cytotoxicity study was conducted for compound [IV] and 5-FU on CAL 51 and B16V cell lines ,results showed enhanced cytotoxic effects for [IV] over 5-FU.
Background. Vitex negundo is a medicinal plant rich in bioactive phytochemicals, particularly phenolic and flavonoid compounds, which have been associated with antioxidant and anticancer activities. Natural plant-derived compounds have gained increasing attention as potential alternatives for cancer therapy due to their lower toxicity and diverse pharmacological properties. Aim. To evaluate the antioxidant and anticancer activities of aqueous and alcoholic leaf extracts of Vitex negundo through phytochemical analysis, antioxidant assessment, and cytotoxic evaluation against the human breast cancer cell line (MCF-7). Methods. Leaves of Vitex negundo were extracted using aqueous and 80% methanolic solvents by Soxhlet extraction. Total flavono
... Show MorePlatinum nanoparticles (PtNPs) exhibit promising biomedical properties, but concerns about biocompatibility and synthesis-related toxicity remain. This study aimed to develop eco-friendly PtNPs using aqueous broccoli extract as a natural reducing and stabilizing agent, and to assess their multifunctional biomedical potential. PtNPs were synthesized through sonochemical reduction of K₂PtCl₆ in broccoli extract, followed by purification and comprehensive physicochemical characterization. UV–Vis confirmed nanoparticle formation at 253 nm, while XRD and FTIR analyses verified the crystalline FCC structure and phytochemical capping. TEM revealed mainly spherical PtNPs with an average core size of 14.83 ± 7.67 nm. Conversely, DLS showe
... Show MoreA series of imidazole [1,2-a] pyridine sulfonamide derivatives was designed and synthesized starting from 2-aminopyridine. In first step, 2-amino pyridine was reacted with 4-bromo phenacyl bromide in the presence of MgO leading to the afford the corresponding imidazole [1,2-a] pyridine scaffold (Panda et al., 2022 [1] ). This intermediate was subsequently subjected to chlorosulfonation using chlorosulfonic acid to afford imidazo [1,2-a] pyridine −3- sulfonyl chloride (Amer, 2009 [2] ). Thereafter, derivative (Amer, 2009 [2] ) was treated with a variety of drugs containing an amine group [4-amino-5-chloro-N-(2- (diethyl amino) ethyl) -2-methoxy benzamide, 4-amino -N-(pyridin-2-yl) benzene sulfonamide and 4-(amino methyl) cyclohexane −1-c
... Show MoreMetal complexes of Mn(II), Co(II), Ni(II), Cu(II), Cd(II), Zn(II), Hg(II), Pd(II), and Pt(II) with Schiff base ligand (LH) derived from 2,5-dichloroaniline and 2-hydroxy-5-metheylbenzalaldehyde were synthesized and characterized using a variety of spectrophotometric techniques The findings of the spectroscopic analysis indicated that (LH) behaved as a binary coordinating agent to the metal ion by the N and O atoms, and the geometry shape of the complexes was octahedral, with the exception of the Pd and Pt complexes, which had a square planar geometry. Using the DPPH radical scavenging method, we investigated the antimicrobial activity of the compound against Staphylococcus aureus and Escherichia coli, as well as the antifungal activity of t
... 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 MoreIn-vitro biological activities of the free new H4L ( indole-7-thiocarbohydrazone) ligand and its Ni(II), Pd(II) , Pt(II), Cu(II), Ag(I), Zn(II) and Cd(II) complexes are screened against two cancerous cell lines, that revealed significant activity only for [Cu2Cl2(H4L)2(PPh3)2] after 72 h treatment by the highest tested concentrations. The Copper(I) complex was characterized by X-ray Crystallography and the NMR spectra, whereas it has been confirmed to have momentous cytotoxicity against ovarian, breast cancerous cell lines (Caov-3, MCF-7). The apoptosis-inducing properties of the Cu(I) complex have been investigated through fluorescence microscopy visualization, DNA fragmentation analysis and propidium iodide flow cytometry.