Novel pyridine bearing pentose moiety-based anticancer agents: design, synthesis, radioiodination and bioassessments.

Pyridine compounds are one of the most important heterocyclic derivatives showing wide ranges in biological and pharmacological activities. Green chemistry eliminates or reduces the generation of hazardous compounds. It prevents pollution at a molecular level.

Niosomal formulation of mefenamic acid for enhanced cancer targeting; preparation, characterization and biodistribution study using radiolabeling technique.

Background: This work aimed to prepare niosomal formulations of an anticancer agent [mefenamic acid (MEF)] to enhance its cancer targeting. I was utilized as a radiolabeling isotope to study the radio-kinetics of MEF niosomes.

Methods: niosomal formulations were prepared by the ether injection method and assessed for entrapment efficiency (EE%), zeta potential (ZP), polydispersity index (PDI) and particle size (PS).

Green synthesis of highly functionalized heterocyclic bearing pyrazole moiety for cancer-targeted chemo/radioisotope therapy.

New derivatives of heterocyclic bearing pyrazole moiety were synthesized (eight new compounds from 2 to 9) via green synthesis methods (microwave-assisted and grinding techniques). 4,6-Diamino-1,3-diphenyl-1H-pyrazolo[3,4-b]pyridine-5-carbonitrile (2) shows high anti-cancer activity against both HepG2 and HCT-116 with IC of 9.2 ± 2.

Cod liver oil nano-structured lipid carriers (Cod-NLCs) as a promising platform for nose to brain delivery: Preparation, optimization, cytotoxicity & biodistribution utilizing radioiodinated zopiclone.

Nano-structured lipid carriers containing zopiclone were prepared as a targeted drug delivery system to convey zopiclone directly to brain nasal route. Nano-structured lipid carriers were constructed adopting hot emulsification-ultrasonication method using palmitic acid in place of the solid lipid, cod liver oil as liquid lipid, and poloxamer 407 as a surfactant. A three-factor three-level central composite face-centered design was used to optimize the formulated nano-structured lipid carriers.

New 5-Aryl-1,3,4-Thiadiazole-Based Anticancer Agents: Design, Synthesis, In Vitro Biological Evaluation and In Vivo Radioactive Tracing Studies.

A new series of 5-(4-chlorophenyl)-1,3,4-thiadiazole-based compounds featuring pyridinium (), substituted piperazines (), benzyl piperidine (), and aryl aminothiazoles () heterocycles were synthesized. Evaluation of the cytotoxicity potential of the new compounds against MCF-7 and HepG2 cancer cell lines indicated that compounds and displayed the highest activity toward the tested cancer cells. A selectivity study demonstrated the high selective cytotoxicity of and towards cancerous cells over normal mammalian Vero cells.

Radioiodinated acemetacin loaded niosomes as a dual anticancer therapy.

A niosomal formula of acemetacin was developed to improve its tumor targeting and radio-kinetic evaluation was performed using I. Niosomes were prepared by ether injection method and characterized for particle size (PS), polydispersity index (PDI), zeta potential (ZP), entrapment efficiency (EE%) and in vitro drug release. Factors affecting radiolabeling with I were studied and optimized.

Conventional and microwave-assisted synthesis, anticancer evaluation, Tc-coupling and In-vivo study of some novel pyrazolone derivatives.

New pyrazolone derivatives were successfully synthesized by both microwave-assisted and conventional techniques. Compound 3 (3-(3-Methyl-5-oxo-4,5-dihydro-1H-pyrazol-1-yl)-3-oxopropanehydrazide) displayed remarkable anti-cancer activity (IC obtained at 8.71 and 10.

Bone targeted new zoledronate derivative: design, synthesis, Tc-coupling, study and preclinical evaluation for promising osteosarcoma therapy.

Zoledronate suppresses human sarcomas by blocking the formation of geranylgeranyl diphosphate (GGPP) inhibiting GGPP synthase. Designing of new derivative of dronic acid (1-hydroxy-2-(4-nitro-1H-imidazol-1-yl)ethan-1,1-diyl)bis phosphonic acid), structurally related to zoledronate to be used for osteosarcoma therapy. 1-hydroxy-2-(4-nitro-1H-imidazol-1-yl)ethan-1,1-diyl)bis(phosphonic acid) was synthesized in one pot reaction with a yield of 65 ± 4%.

Preparation and preliminary evaluation study of [I]iodocolchicine-gallic-AuNPs: a potential scintigraphic agent for inflammation detection.

Background: Nanomedicine offers great potential for scintigraphic diagnostic imaging with lower risk and higher quality compared to other traditional techniques.

Objectives: This work aimed to develop and evaluate gold nanoparticles combined with gallic acid (gallic-AuNPs) and [I]iodocolchicine as a scintigraphic probe for inflammation.

Methods: [I]iodocolchicine-gallic-AuNPs were synthesized via chemical reduction method where gallic acid was used as reducing agent and [I]iodocolchicine was used as stabilizing agent.

Extraction, purification and radioiodination of Khellin as cancer theranostic agent.

Khellin was successfully extracted from Ammi visnaga fruits with a recovery percent of 96.15%. Next radio-iodination of Khellin was successfully achieved with a high yield.

Novel thiobarbiturates as potent urease inhibitors with potential antibacterial activity: Design, synthesis, radiolabeling and biodistribution study.

Urease enzyme is a virulence factor that helps in colonization and maintenance of highly pathogenic bacteria in human. Hence, the inhibition of urease enzymes is well-established to be a promising approach for preventing deleterious effects of ureolytic bacterial infections. In this work, novel thiobarbiturate derivatives were synthesized and evaluated for their urease inhibitory activity.

Synergistic Cytotoxicity Of Shikonin-Silver Nanoparticles As An Opportunity For Lung Cancer.

The combined action of shikonin and silver nanoparticles (AgNPs) for apoptosis in human cancer cells has not been elucidated. Hence, we investigated the synergistic combinatorial effect of shikonin and AgNPs in human lung cancer cells. Shikonin was used as a reducing and capping agent for AgNPs synthesis as a green method avoiding the hazards of chemical methods.

Dioximes: Synthesis and biomedical applications.

The selective properties of dioxime compounds were discovered and outlined in the beginning of 20th century by Tschugaeff [L.Z. Tschugaeff, Z.

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.