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 MoreA series of coumarin derivatives linked to amino acid ester side chains were synthesized and evaluated of their antibacterial and antifungal activity. The coumarin derivatives was alkylated by the ethyl bromoacetate and then using potassium carbonate to get alkylated hymecromone. Conventional solution method for amide bond formation was used as a coupling method between the carboxy-protected amino acids with acetic acid side chain of coumarin derivatives. The DCC/ HOBt coupling reagents were used for peptide bond formation. The proposed analogues were successfully synthesized and their structural formulas were consistent with the proposed struct
... Show MoreOur goal in this research, some new nucleoside analogues was synthesized. Starting from ?-D glucose which was converted to per acetylated ?-D gluco pyronoside then converted to active from(1-Bromo Sugar (2) as a sugar moiety.The base moiety 2-substituted benzimidazole was prepared from condensation of phenylene diamine with different aromatic aldehydes, which were subjected to amino alkylation via Mannich reaction forming new nucleobase derivatives. Condensation of nucleobase with bromo sugar through nucleophilic substitution of anomeric carbon with nitrogen forming new protected nucleoside analogues then hydrolyzed with sodium methoxide in methanol to obtain our target, the free nucleoside analogues. All prepared compound were identified b
... Show MoreIn this research some new nucleoside analogues were synthesized. Starting from α-D- glucose which was protected to glucose penta acetat α-D- glucose pyronside (1). Which was converted to active form 1-bromo protected sugar (2) as a sugar moiety. The base moiety 2-substituted imidazoline (3,4) was prepared from condensation of ethylene diamine with two kind of aromatic aldehydes, which were subjected to amino alkylation via Mannich reaction forming new nucleaobase derivatives (5-10). Condensation of nucleobase with bromo sugar through nucleophilic substitution of anomeric carbon with nitrogen forming new protected nucleoside analogues (11-16). De blocking of these nucleoside analogues with sodium methoxide in methanol afforded our targe
... Show MoreBackground: In this study, a targeted drug delivery system has been developed based on nanoporous particles covered with cadmium sulfide and loaded with 5-flourouracil. The nanoparticles loaded drug exerts a cooperative antineoplastic activity.
Results: The development of nanoparticles loaded anticancer agent for possible application in targeted treatment of cancer where the drug release is triggered by externally applied UV irradiation. In addition, the treatment of cancer cells with drug loaded magnetic material leads to a decrease in viability of the cells due to the activity of cadmium nanoparticles. Upon exposure to low power UV light (365 nm) the loaded 5-flourouracil is released which indu
... Show MoreNew Azo compounds containing an 1,8-naphthalimide moiety were synthesized from 1, 8-naphthalic anhydride by a reaction with p-phenylenediamine or benzidine to produce 1,8-naphthalimide derivatives (1 or 2), which were converted to diazonium salt derivatives by using sodium nitrite and acetic acid at 0-5 áµ’C. The diazonium salt was subjected to a coupling reaction with different substituted phenol in alkaline media at 0-5 áµ’c to produce azo compound derivatives (3-14).
The New Azo compound derivatives (3-14) were identified by 1H-NMR, 13C-NMR, and FTIR and by measuring characteristic physical properties and specific reactions. Also, the ability of the prepared azo compounds to work as acid-
... Show MoreInthis study new derivatives of Schiff bases and nucleoside analogues have been synthesized from the starting material D-glucose after a series of reactions. Derivative 1 was prepared from D-glucose then react with P-bromoacetophenone gave derivative 2 was reacted with dimethyl sulfoxide and acetic anhydride for dehydration a molecule of water gave 3. The spiro ring was prepared at 3-position from the reaction of 3 derivative with 1-phenyl-2–thioureagave 4. The protection group at 1 position was removed by using acetic acid fllowed by periodate oxidation to obtain 6. Reaction of 6 with hydrazide derivative at once and dtriazole derivative at another gave 8 and 9 respectively. Compound 6 was reduced to gave derivative 7. The 1-hydroxylgrou
... 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