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.
New ligands, N1, N4-bis (benzo[d]thiazol-2- ylcarbamothioyl) succinamide (L1) and N1, N4- bis (benzylcarbamothioyl)succinamide (L2), derived from succinyl chloride and 2-amino benzothiazole or benzylamine, respectively, have been used to prepare a set of transition metal complexes with the general formula [M2(L)Cl4], where L=L1 or L2, M = Mn(II), Ni(II), Cu(II), Cd(II), Co(II), Zn(II) or Hg(II). The synthesized compounds were characterized using various analytical techniques including TGA, 13C NMR, mass spectroscopy, 1H and Fourier-transform infrared (FTIR) spectroscopy, magnetic measurement, molar conductivity, electronic spectrum, (%M, %C, %H, %N) and atomic absorption flame (AAF) analysis. The results showed that (L1, L2) bin
... Show Moreنظرة عامة: تُعرَّف المادة أو العامل الذي يمكن أن يؤثر على الحمض النووي أو الكروموسومات على أنه سم جيني. قد يؤدي تلف الحمض النووي في الخلية الجسدية إلى حدوث طفرة جسدية ، والتي قد تحفز التحول الخبيث ، في حين أن الضرر الذي يلحق بالخلية الجرثومية قد يؤدي إلى تغيير خاصية وراثية (طفرة في السلالة الجرثومية) (سرطان). أحد الأحماض الدهنية الأحادية غير المشبعة الأحادية غير الأساسية هو حمض البالميتوليك. بعد حمض الأوليك
... Show MoreRheumatoid arthritis is an autoimmune diseasecharacterized by chronic inflammationthat affects joints and cartilage. Bone complications such asRA-relatedosteoporosis are one of the most extra-articular manifestations. Many inflammatory mediators are released during RA disease pathophysiology; these mediators stimulate osteoclast genesis of bone by direct effects on RANKL and OPG. The study aimedto measure RANKL, OPG in RA patients treated with Etanercept only and other groups treated with Methotrexate onlyat baseline and after three months to evaluate bone state. An observational case-control prospective study was done on 30 RA patients who received MTX, 30 RA patients who received ETN, and 30 healthy,age-matched control groups. The
... Show MoreThe discovery of novel therapeutic molecules is always difficult, and there are a variety of methodologies that use the most diverse and innovative medicinal chemistry approaches. One such approach is the deuteration technique: Deuteration is the process of substituting deuterium for hydrogen in a molecule. When compared to the drug molecule, its deuterated analogues may retain the features of the original molecule and, in some cases, improve its pharmacological activity, with fewer side effects and lower toxicity. Metronidazole is a commonly used antibiotic to treat anaerobic bacterial infections, protozoal and microaerophilic bacterial infections. Met
... Show MoreIn this study, new derivatives of Schiff bases of 2-thio-5-aryl1,3,4-oxadiazole have been synthesized. The structures of these derivatives were characterized from their melting points, infrared spectroscopy and elemental analysis. The Schiff bases derivatives were tested for inhibition of E-coli and were all found to be active.
The Mannich base ligand was synthesized in an ethanol medium through a condensation reaction of 2-mercaptobenzimidazole and ciprofloxacin at room temperature. Subsequently, several metal complexes of this ligand were prepared. To characterize both the base ligand and the metal complexes, various techniques were employed, including elemental analysis, FT-IR spectroscopy, UV-Vis spectroscopy, molar conductivity measurements, magnetic moment determination, and melting point analysis. The results were shown that the metal complexes formed have the formula [Cr(L)2Cl2] Cl.H2O and [Rh(L)2(H2O)2] Cl3.H2O, where L= mannich base ligand. Based on spectroscopic analytical, coordination with metal ions involves the 'N' donor atom of mannich base
... Show MoreWith 549,393 new cases recorded in 2018, bladder cancer is one of the most common malignancies worldwide. Urinary bladder cancer is the cause of about 3 percent of all new cancer diagnoses and 2.1 percent of all cancer deaths. This study aims to evaluate the efficiency of the N-myc downstream-regulated gene 1(NDRG1) as a biomarker for bladder cancer patients in the Iraqi population. One hundred individuals in the case-control study were enrolled and divided into two groups. The first group included 50 patients diagnosed with a bladder mass and investigated by undergoing cystoscopy examination for transurethral resection of bladder tumor (TURB). The second group included 50 healthy individuals who had normal bladder tissue. The resul
... Show MoreUnregulated epigenetic modifications, including histone acetylation/deacetylation mediated by histone acetyltransferases (HATs) and histone deacetylases (HDACs), contribute to cancer progression. HDACs, often overexpressed in cancer, downregulate tumor suppressor genes, making them crucial targets for treatment. This work aimed to develop non‐hydroxamate benzoic acid–based HDAC inhibitors (HDACi) with comparable effect to the currently four FDA‐approved HDACi, which are known for their poor solubility, poor distribution, and significant side effects. All compounds were structurally verified using FTIR, 1HNMR, 13CNMR, and mass spectrometry. In silico ana