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.
The azo dye (LH) was used to synthesize a series of complexes with Fe(III), Co(II), Ru(III), and Rh(III) metal ions. The ligand (LH) was synthesized by the condensation reaction between tryptamine and 2-hydroxyquinoline. Due to the presence of effective donor atoms (-N=N- azo and OH hydroxyl groups), the ligand was subsequently refluxed with various metal ions, leading to the formation of nonelectrolytic [M:L] (1:2). These compounds were characterized using 1H and 13C-NMR, FT-IR, UV–Vis, mass spectrometry, TGA, DSC, and C.H.N. analysis, along with conductivity, magnetic susceptibility, and metal and chlorine content measurements. The results indicated that the ligand acts as a bidentate, with the complexes adopting an octahedral geometry.
... Show MoreTo synthesize new hydrazone derivatives of naproxen with enhanced anti-inflammatory activity and devoid the ulcerogenic side effects. Hydrazones were synthesized by conjugation of naproxen hydrazide with seven natural and synthetic aldehyde and ketone by using glacial acetic acid as catalyst. The synthesis has been carried out following simple methodology in excellent isolated yields.The structure of the synthesized derivatives has been characterized by elemental microanalysis (CHN), FTIR Spectroscopy, and other physicochemical properties.The anti- inflammatory activity of the synthesized compounds was evaluated in vivo using the egg-white induced edema model in rats, and the results of the biological assay was found to be comparable to Nap
... Show MorePurpose: To evaluate the usefulness of serum cyclin D1, CDK4, and CDK6 as biomarkers of treatment response and progression-free survival (PFS) in metastatic breast cancer (MBC). Methods: In a single-center prospective observational study, 74 women with hormone-receptor-positive (HR+)/ human epidermal growth receptor-2 (HER2)-negative metastatic breast cancer were recruited from the Oncology Hospital, Medical City in Baghdad, Iraq. The patients were treated with oral Palbociclib (125 mg) for 21 days, then continued with Letrozole (2.5 mg) for 7 days, and completed six treatment cycles. The candidates were divided into two groups based on therapeutic response: Group 1 responded to the palbociclib plus letrozole combination therapy, a
... 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
Azo ligand 11-(4-methoxyphenyl azo)-6-oxo-5,6-dihydro-benzo[4,5] imidazo[1,2-c] quinazoline-9-carboixylic acid was derived from 4-methoxyaniline and 6-oxo-5,6-dihydro-benzo[4,5]imidazo[1,2-c]quinazoline-9-carboxylic acid. The presence of azo dye was identified by elemental analysis and spectroscopic methods (FT-IR and UV-Vis). The compounds formed have been identified by using atomic absorption in flame, FT.IR, UV-Vis spectrometry magnetic susceptibility and conductivity. In order to evaluate the antibacterial efficiency of ligand and its complexes used in this study three species of bacteria were also examined. Ligand and its complexes showed good bacterial efficiencies. From the obtained data, an octahedral geometry was proposed for all p
... Show MoreBoth methotrexate and vitamin D3 are used in combination for the treatment of various diseases. The aim of this study is to highlight the effect of vitamin D3 on methotrexate-induced jejunum damage using biochemical and histopathological studies. Seven groups of both sexes of rats were selected and treated as follows: (Group I and Group II) : control 1,control 2 (I.P normal saline) daily for 14 and 21 days respectively ; (Group III and Group IV) :vitamin D3 groups (500 IU/rat/day) orally for 14 and 21 days, respectively;(Group V): once daily dose of methotrexate 20mg/kg, I.P injected for 4 days;(Group VI):vitamin D3 (500 IU/rat/day) once daily for 14 days and methotrexate (20 mg/kg I.P) injected only at day 10;.(Group
... Show MoreBoth methotrexate and vitamin D3 are used in combination for the treatment of various diseases. The aim of this study is to highlight the effect of vitamin D3 on methotrexate-induced jejunum damage using biochemical and histopathological studies. Seven groups of both sexes of rats were selected and treated as follows: (Group I and Group II) : control 1,control 2 (I.P normal saline) daily for 14 and 21 days respectively ; (Group III and Group IV) :vitamin D3 groups (500 IU/rat/day) orally for 14 and 21 days, respectively;(Group V): once daily dose of methotrexate 20mg/kg, I.P injected for 4 days;(Group VI):vitamin D3 (500 IU/rat/day) once daily for 14 days and methotrexate (20 mg/kg I.P) injected only at day 10;.(Group VII) vit
... Show MorePolyvinal alcohol was Cynoethylated , complex compound with Iodin in presence of Cu++ ions were preparated and their ultra violet (U.V) and infra red( IR) spectra were investigated. The prepared derivative and complexes were evaluated as antibacterial and antifungal agents following the standard dilution method. MIC(minimum inhibitory concentration) for each polymer using ten types of gram + ve and gram _ ve bacteria were determinated in addition to three types of fungi. The results obtainded showed that MIC, s were around 0.0011 × 103 molar for different polymetric derivatives tried.