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.
In the present work, the phthalic acid (phthH2) and 1.10 phenonthroline (phen), and their complexes were synthesized and isolated as [M(phth)(phen)2], Mn(II), Fe(II), Co(II), Ni(II) Cu(II), Zn(II), and Cd(II) ions. These complexes were characterized by elemental analysis, melting point, conductivity, percentage metal, UV–Vis, FT-IR, and magnetic moment measurements. The molar conductance indicates that all the metal complexes in DMSO are nonelectrolytic. phthalic acid (phtha), and 1,10-Phenanthroline (phen), behaved as bidentate, coordinating to the metal ion through their two oxygen and two pyridinyl nitrogen atoms respectively, as corroborated by. Electronic spectra, FTIR, spectroscopy amusement indicated that all the metal complexes ad
... Show MoreBackground: Piezosurgery improved the split approach by making it safer, easier, and less prone to complications when treating extremely atrophic crests. Densah drills, with their unique design, expand the ridge by densifying bone in a reverse, non-cutting mode. Objective: To assess the effectiveness of sagittal piezosurgery, which involves cutting bone to the full implant depth and then expanding it using osseodensification drills. We use this technique to expand narrow alveolar bones and simultaneously place dental implants in the maxillary and mandibular arches. Methods: Fourteen patients received 31 dental implants. The maxillary arch received 19, and the mandible received 12 dental implants. This study will include patients who
... Show MoreThe discourse surrounding lingual sovereignty within the African postcolonial context is profoundly intertwined with the fabric of cultural identity and self-determination. Language serves not merely as a conduit for communication but as a repository for a people's collective consciousness, encapsulating their traditions, thoughts, and perspectives. In the realm of postcolonial literature, this dialogue often grapples with the paradox of expressing indigenous narratives through the linguistic tools of former colonizers. Chinua Achebe's seminal work, "Things Fall Apart," exemplifies this conundrum, artfully weaving the orature and culture of Umuofia within the English language. Achebe's choice to write in English—a language imposed upon hi
... Show MoreThis work involves the preparation of the ligand [KL] :- ÂÂÂÂÂÂ
K[4-(N-(5-methylisoxazol-3-yl) sulfamyl) phenylcarbamodithioate] from the reaction of sulfamethoxazole with Carbon disulfide in the presence of potassium hydroxide under reflux (4 hours) using methanol as asolvent. The prepared ligand was characterized using FT-IR, UV-Vis, 1H,13C–NMR spectroscopy, molar conductivity and melting point, Complexes for the above ligand [KL] with some bivalent transition and non-transition metals (Mn +2, Co+2 , Ni+2 ,
... Show MoreTransition metal complexes of Co(II), Ni(II), Cu(II), and Zn(II) with 2-(4-antipyrine azo)-4-nitroaniline derived from 4-aminoantipyrine and 4-nitroaniline were synthesized. Characterization of these compounds has been done on the basis of elemental analysis, electronic data, FT-IR, UV-Vis and 1HNMR, as well as magnetic susceptibility and conductivity measurements. The nature of the complexes formed were studied following the mole ratio and continuous variation methods, Beer's law obeyed over a concentration range (1×10-4 - 3×10-4 M). High molar absorbtivity of the complex solutions were observed. From the analytical data, the stoichiometry of the complexes has been found to be 1:2 (metal:ligand). On the basis of physicochemical data octa
... Show MoreSildenafil, tadalafil, and vardenafil are phosphodiesterase type 5 enzyme (PDE-5) inhibitors used for the treatment of male erectile dysfunction. This present study aims to investigate 55 herbal products indicated for men’s sexual health from the Malaysian market for adulteration of PDE-5 inhibitors and analogues. The screening and identification of 20 PDE-5 inhibitors and analogues in herbal products of various forms (powder, capsules, tablets, and pastels) were conducted using gas chromatography–electron impact-mass spectrometer (GC-EI-MS). The analysis has shown that 19 herbal products were adulterated with PDE-5 inhibitors and analogues. Unique ion fragmentations and the presence of molecular
... Show MoreIsradipine related to dihydropyridine (DHP) class of calcium channel blockers (CCBs). It is used to treat hypertension, angina pectoris, as well as Parkinson disease. It goes under the BCS class II drug (low solubility-high permeability). The drug will experience extensive first-pass metabolism in liver, thus, oral bio-availability will be approximately15 to 24 %.
The aim of the study is preparing stable oral oil in water (o/w) nanoemulsion of isradipine to promote the colloidial dispersion of isradipine in the nano range, so that it may be absorded by intestinal lymphatic transport in order to avoid hepatic first-pass metabolism (israpidi
... Show MoreAllosteric inhibition of EGFR tyrosine kinase (TK) is currently among the most attractive approaches for designing and developing anti-cancer drugs to avoid chemoresistance exhibited by clinically approved ATP-competitive inhibitors. The current work aimed to synthesize new biphenyl-containing derivatives that were predicted to act as EGFR TK allosteric site inhibitors based on molecular docking studies.
A new series of 4'-hydroxybiphenyl-4-carboxylic acid derivatives, including hydrazine-1-carbothioamide (S3-S6) and 1,2,4-triazole (S7-S10) derivatives, were synthesized and characterized using IR, 1HNMR, 13CNMR