Aim: To evaluate the cytotoxic activity of newly synthesized a series of novel HDAC inhibitors comprising sulfonamide as zinc binding group and Isatin derivatives as cap group joined by mono amide linker as required to act as HDAC inhibitors. Materials and Methods: The utilization of sulfonamide as zinc binding group joined by N-alkylation reaction with ethyl-bromo hexanoate as linker group that joined by amide reaction with Isatin derivatives as cap groups which known to possess antitumor activity in the designed of new histone deacetylase inhibitors and using the docking and MTT assay to evaluate the compounds. Results: Four compounds have been synthesized and characterized successfully by ART-FTIR, NMR and ESI-Ms. the compounds were synthesized and characterized by successfully by ART-FTIR, NMR and ESI- Ms. Assessed for their cytotoxic activity against human colon adenocarcinoma MCF-7 (IC50, I=105.15, II=60.00, III=54.11, IV=56.57, vorinostat=28.41) and hepatoblastoma HepG2 (IC50, I=63.91, II=135.18, III=118.85, IV=51.46, vorinostat=37.50). Most of them exhibited potent HDAC inhibitory activity and significant cytotoxicity. Conclusions: The synthesized compounds (I, II, III and IV) showed cytotoxicity toward MCF-7 and HepG2 cancer cell lines and their docking analysis provided a preliminary indication that they are viable [HDAC6] candidates.
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 MoreABSTRACT : This research involves the synthesis of five to seven heterocyclic compounds starting with Schiff’s bases which derived from oxime as a starting material. 1.3-oxazepine derivatives were prepared from adding different anhydrides to the Schiff bases, tetrazole and thiazolidinone derivatives synthesized from add sodium azide and thioglycolic acid to the same Schiff’s bases as a five members ring. Pyrimidine derivatives were prepared after the reaction of the azomethine group with acetyl chloride and then urea and thiourea to synthesis on derivatives contain the six members ring. Another step included identified and confirmed these compounds by FT- IR, 1HNMR, TLC and 13CNMR finally, step included the assay of biological activity
... Show MoreObjective:This study involved synthesis of a new series of different five-membered heterocyclic derivatives, testing their antioxidant activity, and examining their potential in vitro antimicrobial agents. Methods: The synthesis of the derivatives involved a three-step process. Initially, succinyl chloride was reacted with methanol, followed by a reaction with 80% hydrazine hydrate through a nucleophilic addition-elimination mechanism, resulting in the formation of succinohydrazide (I). This compound was then employed as a precursor for the synthesis of Schiff bases (II), and (III) by reacting it with m-nitro benzaldehyde and p-nitro benzaldehyde. Following this, a ring closure reaction was applied using thioglycolic acid, glycolic acid,
... Show MoreMetronidazole-MIPs were prepared by using (MDZ) as the template as well as allylchloride (AYC) or allylbromide (AYB) as monomer, used (TMPTA) tri-methylol propane tri-acrylate or ethylene glycol di-methyl acrylate (EGDMA) as cross-linker and initiator used (BP) benzyl peroxide. By using different plasticizers (di butyl Phthalate (DBPH), Nitrobenzene (NB), oleic acid (OA) and paraffin) for MDZ-MIP1 and (Di-butyl sebecate (DBS), Di-methyl acrylate (DMA), Tributylphosphate(TBP) and Tris(ethylhexyl phosphate (TEHP) ) for MDZ-MIP2. Membranes of MIPs were prepared in PVC matrix. The characterizations of each electrode were determined The Slope range from (55.083 - 43.711) mV/decade, Limit of Detection (8 X 10 -4- 2 X 10-6) and Linearity
... Show MoreSynthesis of new nucleoside analogues of the type : 3¢ , 3¢ - gem – di – C – nitromethly , expected to have useful application in the chemotherapeutic treatment of AIDS , cancer and microbial infections. The synthesis involved the condensation of the appropriate sugar derivative ( i.e . 3¢ , 3¢ – gem – di – C – nitromethly – 1– ribofuranose ) with nitrogen bases , such as , uracil and theophllin following a multi step scheme starting from diacetone golucose (1) (scheme 1) .The prepared compound were identified by spectroscopic methods ; ir , mass , 1H and 13C nmr.
The synthesis of nanoparticles (GNPs) from the reduction of HAuCl4 .3H2O by aluminum metal was obtained in aqueous solution with the use of Arabic gum as a stabilizing agent. The GNPs were characterized by TEM, AFM and Zeta potential spectroscopy. The reduction process was monitored over time by measuring ultraviolet spectra at a range of λ 520-525 nm. Also the color changes from yellow to ruby red, shape and size of GNP was studied by TEM. Shape was spherical and the size of particles was (12-17.5) nm. The best results were obtained at pH 6.
Neutral and semi-synthetic hydrophilic polymers are widely used
in pharmaceutical technology to fomlUlate as controlled release drugs
delivery systems ,cellulose derivatives is biocompatibilily, biodegradability , non-toxicity, its is a good candidate as drug carrier. In this study, polymers were used as cellulose derivatives like Methylcellulose (MC) & Soditun Carboxymetl1ylcellulose (NaCMC) as hydrogels for controlled delivery for two kinds of drugs, Cefotaxine
& Amoxycill ine trihydrate i n different media (Distilled water, Normal Saline & Buffer solution PH=2). It has been shown that for sodium Carboxymethylcellulnse the drug release rate is more than the Mcthylcellulose and that the release
... Show MoreStarting from bis (4,4'-diamino phenoxy) ethan(1), a variety of phenolicschiff bases (methylolic, etheric, epoxy) derivatives have been synthesized. All proposed structure were supported by FTIR, 1H-NMR, 13C-NMR Elemental analysis, some derivatives evaluated by thermal analysis (TGA).
New Derivatives for Known P- Jactam antibiotics were
synthesized utilizing the free amino group pres nt in the parent compounds as the site for derivatization. The objectives for this study
are to have new compounds which could have an increased potential resistance to the degradative enzymes knowing to be able to destroy
the antibacterial activity of 13· lactam antibiotics- Besides. these new
derivatives could be congeners of known agents, or may be a
pott:ntial pro-drugs for thes
... Show MoreThree mesoporous silica with different functional group were prepared by one-step synthesis based on the simultaneous hydrolysis and condensation of sodium silicate with organo - silane in the presence of template surfactant polydimethylsiloxane - polyethyleneoxide (PDMS - PEO). The prepared materials were characterized by Fourier transform infrared spectroscopy (FTIR), thermogravimetric analysis (TGA), atomic force microscopy (AFM) and nitrogen adsorption/desorption experiments. The results indicate that the preparation of methyl and phenyl functionalized silica were successful and the mass of methyl and phenyl groups bonded to the silica structure are 15, 38 mmol per gram silica. The average diameter of the silica particles are 103.51,
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