Recently, some prostate cancer patients have acquired resistance to the second -generation drugs (anzalutamide and apalutamide) prescribed for the treatment of this disease due to the emergence of the F876L mutation, which represents a challenge to modern medicine. In this study, a new series of 2-thiohydantoin derivatives were prepared through the reaction of different derivatives of maleimide (1c-4c) with isothiocyanate derivatives. The prepared compounds were diagnosed using FT-IR,1H-NMR ,13C-NMR, Mass spectra. The prepared series compounds has been studied against prostate cancer cells. The MTT assay was used to determine the activity of the prepared compounds against prostate cancer cells. The data indicated, depending on the IC50 values, that some of the prepared compounds have anti-prostate cancer activity. The results indicate that compounds 1d and 2d have good anti-prostate cancer activity compared to the rest of the compounds. The prepared series of compounds were also studied against selected types of bacteria and fungi, as the results showed that some of the compounds in the series had anti-bacterial and anti-fungal activity.
In the present research synthesis and study of biological activity a series of new polymers modified of chitosan with compounds containing azo group. Beginning diazonium salt produced from 3,3'-dimethyl-[1,1'-biphenyl]-4,4'-diamine reacted with concentrated HCl acid and sodium nitrite. The coupling reaction between diazonium salt with substituted aromatic aldehyde to produce Azo derivatives )1-6(. Azo Schiff bases Chitosan )7-12( were synthesized by condensation of Chitosan with Azo derivatives )1-6( in ethanol with some drops of glacial acetic acid. The structural modifications of Chitosan ring (linked to a bioactive azo moiety) were expected to give new derivatives )7-12( with a diverse range of biological functions. These compounds' st
... Show MoreNatural polymers are often non-toxic, biodegradable, biocompatible, and safe. A novel ligand was synthesized as a natural polymer using chitosan and oleander plant extract [(2R,3S,4R,5S)-5-(acetoxyamino)-4-hydroxy-3,6-dimethoxytetrahydro-2H-pyran-2-yl) methyl (16R)-3-(((2S,4S,5R)-4-methoxy-2,5-dimethyltetrahydro-2H-pyran-2-yl)oxy-10,13,16-trimethyl-17-(5-oxo-2,5-dihydrofuran-3-yl) hexadecahydro-14H-cyclopenta [a] phenanthren-14-yl) phthalate] (Chitosan-Ph-Oleander). This ligand and its complexes with several metals (Cr+3, Mn+2, Fe+3, Ni+2, Cu+2, Zn+2) were characterized using FTIR, UV-visible and 1H-NMR spectroscopy, as well as by molar conductivity, magnetic moment, and TGA analysis. The biological activity for the prepared polymer
... Show MoreIn this study, synthesis of polymer Nanocomposites through the blending of prepared polymers with polyvinyl alcohol (a synthetic polymer) or chitosan (a natural polymer) then mixed with nano oxide silica by many steps. The new compound [I] was obtained via reaction of 3,3’-dimethoxybiphenyl-4,4’-diamine as starting material with malic anhydride in DMF then treatment with ammonium persulfate (NH4 )2 S2 O8 (as the initiator) in order to produce polymer [II]. Also, we prepared new polymers [III-V] by using the same starting material (3,3’-dimethoxybiphenyl-4,4’-diamine) with glutaric acid or adipic acid or isophthalic acid in DMF and pyridine. In this study, new polymer blending [VI-IX] and [X-XIII] were synthesized from a prepared pol
... Show MoreIn 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 MoreAim: 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 w
... Show MoreThis work includes the synthesis of new ester compounds containing two 1,3,4-oxadiazole rings, 15a-c and 16a-c. This was done over seven steps, starting with p-acetamido-phenol 1 and 2-mercaptobenzoimidazole 2. The structure of the products was determined using FT-IR, 1H NMR, and mass spectroscopy. The evaluation of the antimicrobial activities of some prepared compounds was achieved against four types of bacteria (two types of gram-positive bacteria; Staphylococcus aureus and Bacillus subtilis, and two types of gram-negative bacteria, Pseudomonas aeruginosa and E. Coli), as well as against one types of fungus (C. albino). The results show moderate activit against the study bacteria, and the theoretical analysis of the toxi
... Show MoreIsatin is a heterocyclic molecule that belongs to one of the most important classes of organic compounds known as indolines. Isatin, isatin analogs, and their Schiff bases have recently attracted a lot of attention in medicinal chemistry. Isatin, itself, shows various biological activities such as antiviral, anticancer, antimicrobial, anti-inflammatory, analgesic, antioxidant, and anticonvulsant. Bis- Schiff bases containing isatin moiety have been known to possess a wide spectrum of pharmacological activities. This review offers up-to-date information on the most active isatin bis-Schiff bases, which would include anticancer, antimicrobial, antiviral, anticonvulsant, anti-inflammatory, and analgesic activities. These observations c
... Show MoreIsatin is a heterocyclic molecule that belongs to one of the most important classes of organic compounds known as indolines. Isatin, isatin analogs, and their Schiff bases have recently attracted a lot of attention in medicinal chemistry. Isatin, itself, shows various biological activities such as antiviral, anticancer, antimicrobial, anti-inflammatory, analgesic, antioxidant, and anticonvulsant. Bis- Schiff bases containing isatin moiety have been known to possess a wide spectrum of pharmacological activities. This review offers up-to-date information on the most active isatin bis-Schiff bases, which would include anticancer, antimicrobial, antiviral, anticonvulsant, anti-inflammatory, and analgesic activities. These observations c
... Show MorePreparation and Identification of some new Pyrazolopyrin derivatives and their Polymerizations study