Small molecules drug conjugate mutual prodrug design (SMDC) composed of folate and lethal agent conjugate, rigidly bonded via hydrophilic bridge and self immolative disulfide bond ; represent new interesting approaches for cancer treatment , the component of SMDC intended for targeting folate receptor , along with greater conservation of component until reaching the target tumor tissue . The designing and synthesis of compound VI and VIII derived from 6-Mercaptopurine (6-MP) and Methotrexate ( MTX) conjugate altogether as mutual prodrugs were processed forward successfully by multistep reaction procedures , and by Thin Layer Chromatography (TLC) for preliminary detection of products and their intermediates, along with their purity. The structures of two final compounds and their intermediates were proclaimed by melting point measurement, infrared spectrometry and ¹HNMR analysis given results greatly correspond with theoretical proposed chemical structure of synthesized compounds. Furthermore, cytotoxic activity evaluation on cell line level had been done for two final compounds against human breast tumor cell (MCF-7) and human ovarian tumor cell (SKO-3) types of cancer cell line and the results were confirmed which show greater cytotoxic tumor activity of two final compounds, while compound VI possess optimal activity proportional with increased number of 6-MP molecules.
In the present paper, chitosan Schiff base has been synthesized from chitosan’s reaction with the salicyldehyde. The AuNPs was manufacture by extract of onion peels as a reducing agent. The Au NPs that have been prepared were characterized through the UV-vis spectroscopy, XRD analyses and SEM microscopy. The polymer blends of the chitosan Schiff base / PVP has been prepared through using the approach of solution casting. Chitosan Schiff base / PVP Au nano-composites was prepared. Nano composites and polymer blends have been characterized by FTIR which confirm the formation of Schiff base by revealing a new band of absorption at 1651cm-1 as a result of the (C=N) imine group. SEM, DSC and TGA confirms the thermal stability of the pr
... Show MoreConjugate heat transfer has significant implications on heat transfer characteristics, particularly in thick wall applications and small diameter pipes. In this study, a three-dimensional numerical investigation was carried out using commercial CFD software “ANSYS FLUENT” to study the influence of conjugate heat transfer of laminar flow in mini channels at constant heat flux wall conditions. Two parameters were studied and analyzed: the wall thickness and thermal conductivity and their effect on heat transfer characteristics such as temperature profile and Nusselt number. Thermal conductivity of (0.25, 10, 202, and 387) W/m2C and wall thickness of (1, 5, and 50) mm were used for a channel of (1*2) mm cross
... Show MoreFisetin is a plant flavonoid found in strawberries and other fruits and vegetables such as apples, persimmons, and onions. It has many pharmacological effects like anti-inflammatory, antioxidant, cardioprotective, neuroprotective, and anti-carcinogenicity which are attributed to its ability to reduce oxidative stress which considers the main reason for different disease conditions. Genotoxicity refers to the genetic material destruction within the cell which can be caused by different chemicals as well as radiation. The present study evaluates the effect of orally-administered fisetin daily for seven constitutive days on genotoxicity induced by cyclophosphamide in rats’ bone marrow and spleen cells. Results showed that fisetin exh
... Show MoreA novel Schiff base (SB) ligand, abbreviated as HDMPM, resulted from the condensation of 2-amino-4-phenyl-5-methyl thiazole and 4-(diethylamino)salicyaldehyde, and its metal complexes with [Co(II), Cu(II), Ni(II), and Zn(II)] ions in high yield were formed. The physico-chemical techniques such as elemental analysis, molar conductance, IR, 1H and 13C NMR, mass spectroscopy, and electronic absorption studies were utilized to characterize the synthesized compounds. The studied compounds were examined for their possible anticancer activity against a number of human cancerous cell lines, including A549 lung carcinoma, HepG2 liver cancer, HCT116 colorectal cancer, and MCF-7 breast cancer cell lines, with doxorubicin serving as the standard. The s
... Show MoreThe present study was designed to synthesize a number of new Ceftriaxone derivatives by its involvement with a series of different amines, through the chemical derivatization of its 2-aminothiazolyl- group into an amide with chloroacetyl chloride, which on further conjugation with these selected amines will produce compounds with pharmacological effects that may extend the antimicrobial activity of the parent compound depending on the nature of these moieties.
Ceftriaxone was first equipped with a spacer arm (linker) by the action of chloroacetyl chloride in aqueous medium and then further reacted with seven different aliphatic and aromatic amines which resulted in the production of the aimed final target products. The syntheses
... Show MoreThe amino thiadiazole [I] on treatment with aromatic aldehydes yielded Schiff bases [IIa-c], which cyclized to thiazolidinone [IIIa-c] derivatives by reaction with thioglycolic acid. Reaction of carbon disulfide and methyl iodide with [I] gavedithiomethyl [IV] which on treatment with o-phenylenediamine gave the condensed N-Imidazolythiadiazolylamine [V], However, reaction of [I] with phenylisocyanate and phenylisothiocyanate afforded the carbamideand carbothiamide derivatives [VI. VII] ac. The structure of these compounds was characterized from their melting point, FTIR spectroscopy and elementalanalysis
Coumarin derivatives have shown different biological activities, such as antifungal, antibacterial antiinflammatory, and antioxidant activities, besides antibiotic resistance modulating effects, and anti-HIV, hepatoprotective, and antitumor effect. So, new coumarin derivatives (hydrazones and an amide) were synthesized through multisteps reactions. All the synthesized target compounds were characterized by FT-IR spectroscopy, 1HNMR analysis. The compounds then evaluated for their anti-bacterial activity by means of well-diffusion method against two gram-positive bacteria (Staphylococcus aureus, Streptococcus pneumoniae) and two gram-negative bacteria (E.coli and Pseudomonas aeruginosa). The highest activity was demonstr
... Show MoreThe MTX was converted to MTX nanoparticles by the modified method based on changing the pH gradually . For the first time MTX NPs+Meropenem complex were prepared and evaluated as a potential tool to overcome antimicrobial resistance and to improve pharmacokinetics of the drug, the results showed that the antibacterial activity of complex (MTX NPs plus MEM) has increased (from 1( µg/ml) to >0.5( µg/ml) for p1 , from 2( µg/ml) to 1( µg/ml) for p10 and from 8( µg/ml) to 4( µg/ml) for p48).
Myelosuppression is one of the serious adverse effects of cancer chemotherapy that lead to life threatening febrile neutropenia and considered a limiting factor for successful therapy. Cyclophosphamide a widely used anticancer drugs, induces severe bone marrow suppression by damaging hematopoietic stem cells. As cancer incidence expands globally, the demand for an effective myeloprotective therapy during cancer treatment is also increasing.Nigella sativa seed oil, a well-known plant extract that widely used for various health conditions. This study aims to evaluate the myeloprotective activity of Nigella sativa seed oil in cyclophosphamide-induced myelosuppression mice model. Myelosuppression induced by single intraperitoneal injection o
... Show MoreNon-steroidal anti-inflammatory drugs (NSAIDs) contain free –COOH which thought to be responsible for the GI irritation associated with all traditional NSAIDs. The esterification of this group is one of an approach to ultimate aim for reduce the gastric irritation; so in this study we synthesized and preliminarily evaluated new ester compounds as new analogues with expected selectivity toward COX-2 enzyme. Synthetic procedures have been successfully developed for the generation of the target compounds (III a and b). The synthetic approach involved multi-steps procedures which include: Synthesis of 4-hydroxy benzene sulphonamide ( I b ), synthesis of Naproxen and Ibuprofen acyl chloride and then reacting them with 4-hydroxy benzene sulphon
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