2-Methyl-6-(4-aminophenyl)-4,5-dihydro-3(2)-pyridazinone Synthon for Some New Annelated 1,2,3-Selena/Thiadiazoles and 2-Diazaphospholes with Anticipated Biological Activity and Quantum Chemical Calculations.

A convenient and efficient synthetic protocol for the new selenadiazole. Thiadiazole and diazaphosphole derivatives incorporating a pyridazine moiety originating from 4-(4-aminophenyl)-4-oxobutanoic acid () were described. All newly synthesized compounds were evaluated for their antimicrobial activity using the disk diffusion method, and their cytotoxicity was evaluated against brine shrimp lethality bioassay.

Synthesis of Some Mono- and Disaccharide-Grafting Phthalazine Derivatives and Some New -Nucleoside Analogues: Antibacterial Properties, Quantum Chemical Calculations, and Cytotoxicity.

A highly efficient and versatile synthetic approach for the synthesis of 4-(pyren-1-ylmethyl)-1-(d-glycosyloxy) phthalazine nucleosides ,, , -nucleosides , , , and acyclo nucleosides ,, , and - was described and fully characterized. Furthermore, a series of desired new nucleoside analogues containing Se of 4-(pyren-1-ylmethyl) phthalazine-1(2)-selenone - were synthesized. The structures of all reported compounds were confirmed by IR, H-NMR, C-NMR, MS and elemental analysis.

[4-(3-Amino-4-mehoxy-5-methylphenyl)-1-oxo-1H-phthalaz-2-yl] acetic acid hydrazide and its synergetic effect with KI as a novel inhibitor for low carbon steel corrosion in 0.5 M HSO.

We report the synthesis of novel [4-(3-amino-4-mehoxy-5-methyl phenyl)-1-oxo-1H-phthalaz-2-yl] acetic acid hydrazide (APPH), followed by its characterization using X-ray diffraction (XRD), Fourier transforms infrared (FT-IR) spectroscopy, H-NMR spectroscopy, and LC/MS. Further, the inhibition effect of the varying concentration of APPH on the corrosion of low steel (LCS) in 0.5 M HSO was investigated by weight loss and electrochemical measurements at 30 °C.

Design, synthesis, molecular docking and in silico ADMET profile of pyrano[2,3-d]pyrimidine derivatives as antimicrobial and anticancer agents.

Pyrano[2,3-d]pyrimidine derivatives were synthesized by treating cyclic compounds containing active methylene group with aldehyde and malononitrile in butanol. The behavior of pyrano[2,3-d]pyrimidine towards some electrophlies namely triethylorthoformate followed by nitrogen nucleophiles as isobutylamine, urea, phenylthiourea, p-toluidine, o-phenylenediamine, o-aminophenol, 2-amino-4-methyl-pyridine and acetic acid with the aim of obtaining some interesting non-mixed heterocyclic compounds. All synthesized compounds to some extent have shown good antimicrobial activity against different microbial strains that had been extracted by inhibiting cell wall synthesis.

Synthesis, Antiproliferative Activity, and Apoptotic Profile of New Derivatives from the Meta Stable Benzoxazinone Scaffold.

Background: Cancer exerts a huge strain on the health system. The emerging resistance to the current chemotherapies demands the continuous development of new anticancer agents with lower cost, higher efficacy, and greater specificity.

Objective: This study aimed at developing selective small molecules as targeted anticancer agents.

A green microwave method for synthesizing a more stable phthalazin-1-ol isomer as a good anticancer reagent using chemical plasma organic reactions.

Conventional synthesis of the phthalazine has already allowed affording the phthalazin-1-one phthalazin-1-ol dynamic equilibrium that decreases the anticancer activity due to diminishing the concentration of the phthalazin-1-ol product. Nowadays, pure phthalazin-1-ol () can be gaining by using green microwave tools that increase the power of the phthalazine nucleus as an anticancer drug. A microscopic thermal kinetic parameter like activation energy and the pre-exponential factor of the chemical plasma organic reactions affording pure phthalazin-1-ol (5) is calculated by using DFT simulation is obtained.

Eco-friendly sequential one-pot synthesis, molecular docking, and anticancer evaluation of arylidene-hydrazinyl-thiazole derivatives as CDK2 inhibitors.

One current approach in the treatment of cancer is the inhibition of cyclin dependent kinase (CDK) enzymes with small molecules. CDK are a class of enzymes, which catalyze the transfer of the terminal phosphate of a molecule of ATP to a protein that acts as a substrate. Among CDK enzymes, CDK2 has been implicated in a variety of cancers, supporting its potential as a novel target for cancer therapy across many tumor types.

Tc-gallic-gold nanoparticles as a new imaging platform for tumor targeting.

Early and accurate detection of tumor assists in identifying more effective therapies. Gold nanoparticles (GNPs) were synthesized by green synthesis method using gallic acid (GA) then characterized and labeled with technetium-99m. This new platform was biologically evaluated in both normal and solid tumor bearing mice.

Synthesis of bioactive quinazolin-4(3H)-one derivatives via microwave activation tailored by phase-transfer catalysis.

A series of nine new 2,3-disubstituted 4(3H)-quinazolin-4-one derivatives was furnished starting from the 2-propyl-4(3H)-quinazo-line-4-one (2). The reinvestigation of the key starting quinazolinone 2 was performed under microwave irradiation (MW) and solvent-free conditions. Combination of MW and phase-transfer catalysis using tetrabutylammonium benzoate (TBAB) as a novel neutral ionic catalyst was used for carrying out N-alkylation and condensation reactions of compound 2 as a simple, efficient and eco-friendly technique.

Synthesis and Reactivity of 6,8-Dibromo-2-ethyl-4H-benzo[d][1,3]oxazin-4-one Towards Nucleophiles and Electrophiles and Their Anticancer Activity.

Background: The genetic heterogeneity of tumor cells and the development of therapy-resistant cancer cells in addition to the high cost necessitate the continuous development of novel targeted therapies.

Methods: In this regard, 14 novel benzoxazinone derivatives were synthesized and examined for anticancer activity against two human epithelial cancer cell lines; breast MCF-7 and liver HepG2 cells. 6,8-Dibromo-2- ethyl-4H-benzo[d][1,3]oxazin-4-one was subjected to react with nitrogen nucleophiles to afford quinazolinone derivatives and other related moieties (3-12).

Preparation and characterization of yeast cell wall beta-glucan encapsulated humic acid nanoparticles as an enhanced aflatoxin B binder.

This study aimed to assess the effect of encapsulating humic acid inside yeast cell walls (YCW) to detoxify AFB in in vitro gastrointestinal models. Glucan Mannan Lipid Particles (GMLPs) from Saccharomyces cerevisiae cell walls showed the highest AFB adsorption in simulated gastric fluid (SGF) after 10 min, and in simulated intestinal fluid (SIF) after 1 h. GMLPs are hollow 3-4 micron porous microspheres that provide an efficient system for the synthesis and encapsulation of AFB-absorbing nanoparticles (NPs).

Novel Nicotinonitrile Derivatives Bearing Imino Moieties Enhance Apoptosis and Inhibit Tyrosine Kinase.

Background: Fused heterocyclic containing pyrazolopyridine systems have several medicinal activities including cytotoxic and carcinostatic activities.

Objective: To investigate the antiproliferative activity and associated mechanism(s) of a novel series of nicotinonitrile derivatives.

Method: The series has been synthesized by the reaction of hydrazonoyl chlorides with each of 4-(4- methoxyphenyl)-3-methyl-6-oxo-6,7-dihydro-1H-pyrazolo[3,4-b]pyridine-5-carbonitrile and 2-amino-4-(4- methoxyphenyl)-6,7-dihydro-5H-cyclopenta[b]pyridine-3-carbonitrile in dioxane in basic medium.

Synthesis, characterization, radiolabeling and biodistribution of a novel cyclohexane dioxime derivative as a potential candidate for tumor imaging.

Purpose: Dioxime derivative is reported to exhibit high affinity towards tumor cells. The objective of the present study is to synthesize a new dioxime derivative to be labeled with technetium-99m for using as a solid tumor marker.

Materials And Methods: ((2E,2',3E,3')-3,3'-(cyclohexane-1,2-diylbis (azanylylidene)) bis-(butan-2-one)dioxime) was synthesized by condensation of Butan-2,3-dione monooxime and diaminocyclohexane and labeled with Tc.

Efficient 1,3,4-Thiadiazole-4,5-dihydropyridazin-3(2H)-ones as Antimicrobial Agents.

A set of novel series of 1,3,4-thiadiazolyl-sulfanyl-4,5-dihydropyridazin-3(2H)-ones with anticipated antimicrobial activity has been synthesized. The synthetic protocol of the targeted compounds was accomplished by treating β-aroylacrylic acid 1 with 5-amino-1,3,4-thiadiazole-2-thiol (2) to afford the thia-Michael adduct 3. Afterwards, the obtained thia-Michael adduct 3 was cyclized to 4,5-dihydropyridazin-3(2H)-ones 4a-d and the non-cyclized product hydrazone 5 by using different hydrazines.

Utility of Pyrazolylchalcone Synthon to Synthesize Azolopyrimidines under Grindstone Technology.

A series of pyrazolyl-triazolo[1,5-a]pyrimidines, pyrazolyl-tetrazolo[1,5-a]pyrimidines, pyrazolyl-benzo[4,5]imidazo[1,2-a]pyrimidines and bis-azolopyrimidines were prepared by reaction of pyrazolyl-chalcones or its bis-pyrazolyl-chalcones with the appropriate heterocyclic amines as aminotriazole, aminotetrazole, 2-aminobenzimidazole and 4,6-dimethyl-1H-pyrazolo[3,4-b]pyridin-3-amine by grinding method. The newly synthesized compounds have been characterized on the basis of elemental analysis and spectral data (IR, H- and C-NMR, Mass). Moreover, the newly synthesized products were screened for their in vitro antibacterial activities and the results showed that compounds 5f and 11d exhibited excellent activities compared with penicillin G and streptomycin as reference drugs.

Design, synthesis, molecular modeling and biological evaluation of novel 1H-pyrazolo[3,4-b]pyridine derivatives as potential anticancer agents.

In trying to develop new anticancer agents, a series of 1H-pyrazolo[3,4-b]pyridine derivatives was designed and synthesized. Fifteen compounds were evaluated in vitro for their anti-proliferative activity against HePG-2, MCF-7, HCT-116, and PC-3 cell lines. Additionally, DNA binding affinity of the synthesized derivatives was investigated as a potential mechanism for the anticancer activity using DNA/methyl green assay and association constants assay.

SYNTHESIS, CHARACTERIZATION AND BIOLOGICAL EVALUATION OF NEW FUSED TRIAZINE DERIVATIVES BASED ON 6-METHYL-3-THIOXO-1,2,4-TRIAZIN-5-ONE.

A one-pot reaction of 6-methyl-3-thioxo-3,4-dihydro-[1,2,4]triazin-5-one 1 with selected aldehydes 2a-d and chloroacetic acid afforded the respective 2-arylidene-6-methyl-thiazolo[3,2-b][1,2,4]triazine-3,7-diones 4a-d. Compunds 4a-d could be also obtained via the reaction of 1 with chloroacetic acid in refluxing acetic acid to give 6-methyl-thiazolo[3,2-b][1,2,4]triazine-3,7-dione 3 then, Knoevenagel condensation of 3 with aldehydes 2a-d gave compounds 4a-d. Heterocyclization of 4a-c with hydrazine hydrate and phenylhy- drazine gave the corresponding pyrazolines 5a-c and 6a-c, respectively.

Synthesis, Antimicrobial and Anti-inflammatory Activity of Some New Benzoxazinone and Quinazolinone Candidates.

Benzoxazinones and quinazolinones have a wide spectrum of biological activity. In this paper we focused on studying the antimicrobial and anti-inflammatory activities of some newly synthesized benzoxazinone and quinazolinone derivatives. Thus we prepared 2-[α-benzoylaminostyryl]-6,8-dibromo-3,1-benzoxazin-4(H)-one 2 which underwent a reaction with primary and secondary amines, and hydrazine hydrate to give compounds 3, 4 and 5, respectively.

Synthesis and Regioselective Reaction of Some Unsymmetrical Heterocyclic Chalcone Derivatives and Spiro Heterocyclic Compounds as Antibacterial Agents.

A number of novel heterocyclic chalcone derivatives can be synthesized by thermal and microwave tools. Treatment of 4-(4-Acetylamino- and/or 4-bromo-phenyl)-4-oxobut-2-enoic acids with hydrogen peroxide in alkaline medium were afforded oxirane derivatives 2. Reaction of the epoxide 2 with 2-amino-5-aryl-1,3,4-thiadiazole derivatives yielded chalcone of imidazo[2,1-b]thiadiazole derivative 4 via two thermal routes.

Synthesis of novel steroidal curcumin derivatives as anti-Alzheimer's disease candidates: Evidences-based on in vivo study.

Alzheimer's disease (AD) is a complex disease in which a single monofunctional 'targeted' drug is uneffective for management. Hybrid drugs that impact multiple targets simultaneously are better at controlling such complex disease systems. Hybrid agents were synthesized through the combination of the steroid moiety with curcumin molecule.

Reactivity of 2-ethoxyquinazolin- 4-yl hydrazine and its use in synthesis of novel quinazoline derivatives of antimicrobial activity.

The reactions of 2-ethoxy-4-hydrazinoquinazoline 2 with diethyl oxalate and ethyl chloroacetate gave 6-ethoxy-2H-[1,2,4]triazino[4,3-c]quinazoline-3,4-dione 3 and 6-ethoxy-2,3-dihydro-4H-[1,2,4]triazino[4,3-c]quinazolin-4-one 4 respectively. A series of 5-ethoxy-2-X-[1,2,4]triazolo[1, 5-c]quinazolines 5a-d was also produced by reacting 2 with the acid chlorides namely: benzoyl, crotonyl, cinnamyl and 2-furoyl chlorides via Dimroth rearrangement. Also, 2 reacted with ethyl chloroformate giving 6.

Uses of 2-ethoxy-4(3H) quinazolinone in synthesis of quinazoline and quinazolinone derivatives of antimicrobial activity: the solvent effect.

2- Ethoxy-4(3H) quinazolinone 1 was synthesized and allowed to react with various halides, namely: alkyl, benzyl, allyl, acyl, haloacetyl, crotonyl, benzoyl, 2-furoyl and 1-naphthalenesulphonyl halides affording quinazoline and quinazolinone derivatives. The reactions of compound 1 with phosphorus oxychloride, phosphorus pentasulfide, ethyl chloroformate, ethyl chloroacetate, ?-bromoglucose tetraacetate, p-acylaminobenzenesulfonyl chloride, acrylonitrile, chalcone and chalcone oxide were also investigated. Depending on the reaction condition and reactant halide, the type of substituent (alkyl, acyl, aroyl, etc.

Cytotoxic activity of Vitex trifolia purpurea extracts.

Defatted 85% crude hot aqueous methanol extract of Vitex trifolia purpurea (AME) successively extracted with, chloroform and ethyl acetate. Cytotoxicity of (AME), chloroform methanol extract (CE), ethyl acetate methanol extract (EE) and the residue obtained from methanol extract after successive extraction (RME) have been evaluated on brine shrimp (Artemia salina) and Hep-G2 cell lines as well. In brine shrimp lethality bioassay the results revealed that the (RME) is the most potent one with LC50 value 173 microg/ml while LC50 values of (AME), (CE) and (EE) was 180, 199 and 286 microg/ml, respectively.

Antioxidant properties of methanolic extracts of the leaves of seven Egyptian Cassia species.

In the present study, antioxidant activity of methanolic extracts of the leaves of seven Egyptian Cassia species was investigated using two methods, the phosphomolyb-date method and 1,1 diphenyl-2-picrylhydrazyl radical (DPPH) scavenging activity method.· The results revealed that C. glauca is the most potent species and that the activity of other plant species decreases in the following order: C.