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

Mehany, Marwa M.; Hammam, Olfat A.; Selim, Adli A.; Sayed, Galal H.; Anwer, Kurls E.

doi:10.1038/s41598-024-53228-4

Cited by 3 publications

(1 citation statement)

References 60 publications

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“…The synthesized compounds were investigated for their potential to impede the proliferation of HepG2 cells [ 25 , 26 ]. Analysis of the data presented in Table 5 and Figure 6 reveals that both compound 3 and compound 3e significantly reduce cell viability in HepG2 cells after 24 h, exhibiting a concentration-dependent relationship where higher concentrations correlate with decreased cell survival rates.…”

Section: Resultsmentioning

confidence: 99%

Clindamycin Derivatives: Unveiling New Prospects as Potential Antitumor Agents

Jia,

Zhang,

Zhu

2024

Pharmaceuticals

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This study delves into the exploration of Clindamycin derivatives, specifically compounds 3 and 3e, to unveil their antitumor potential by employing a multidisciplinary approach. Screening a repertoire of 200 Clindamycin-associated targets pinpointed the Family A G-protein-coupled receptor as a prominent antitumor candidate. Subsequent analyses unearthed 16 pertinent antitumor proteins, with compound 3 exhibiting robust affinity towards a specific protein via stable hydrogen bonding. Molecular dynamics simulations underscored the adrenergic receptor β as a pivotal target, primarily situated in the plasma membrane and endoplasmic reticulum. These revelations hint towards compound 3’s potential to bolster natural defense mechanisms against tumors by modulating immune responses within the tumor microenvironment, thus paving the way for novel avenues in antitumor drug development. Furthermore, employing the MTT assay, we evaluated the anti-HepG2 cell activity of compounds 3 and 3e, with 5-fluorouracil serving as the control drug. Results revealed that compound 3 exhibited significant differences (p < 0.01) across all concentrations (2.5, 5, 10 μg/mL) compared to the control group, paralleled by the pronounced differences (p < 0.01) observed with 5-fluorouracil.

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Section: Resultsmentioning

confidence: 99%

Clindamycin Derivatives: Unveiling New Prospects as Potential Antitumor Agents

Jia,

Zhang,

Zhu

2024

Pharmaceuticals

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Efficient synthetic strategies for fused pyrimidine and pyridine derivatives: A review

Anjirwala,

Patel

2024

Journal of Heterocyclic Chem

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Pyrimidine and its derivatives play a paramount role in drug discovery as privileged pharmacophores with considerable chemical and biological significance and its presence in genes. This review aims to assemble a systematic evaluation of synthetic tactics of various fused pyrimidine derivatives containing nitrogen heterocycles such as pyridopyridines, pyridopyrimidines, and pyrimidopyrimidine from a pharmacological point of view and deliver an overview of methodologies presenting the chemistry of fused pyrimidine derivatives. The review details the importance of various catalysts and ring substitution using various electrophilic and nucleophilic reagents. These synthetic strategies were elaborated based on the different synthetic routes that lead to the specific type of pyrimidine and pyridine fused derivatives. The literature accumulates various developments in one‐pot condensation, the Knoevenagel–Michael addition mechanism, microwave and ultrasound irradiation, intramolecular cyclization, nano‐catalytic reactions, and so forth. Short reaction times, catalyst reusability, solvent‐free conditions, excellent yields, and stereo‐selectivity are some of the benefits of certain synthetic approaches.

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Research on the corrosion inhibition performance and mechanism of pyrimidine quaternary ammonium salt

Shao,

Fang,

Cheng

et al. 2024

ACMM

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Purpose At present, research on the preparation of corrosion inhibitors using modified pyrimidine derivatives is still blank. The purpose of this study is to synthesize a new cationic mercaptopyrimidine derivative quaternary ammonium salt, known as DTEBTAC, that can be used as a corrosion inhibitor to slow down the metal corrosion problems encountered in oil and gas extraction processes. Design/methodology/approach A new corrosion inhibitor was synthesized by the reaction of anti-Markovnikov addition and nucleophilic substitution. The weight loss method was used to study the corrosion inhibition characteristics of synthetic corrosion inhibitors. Electrochemical and surface topography analyses were used to determine the type of inhibitor and the adsorption state formed on the surface of N80 steel. Molecular dynamics simulations and quantum chemistry calculations were used to investigate the synthetic corrosion inhibitor’s molecular structure and corrosion inhibition mechanisms. Findings The results of the weight loss method show that when the dosage of DTEBTAC is 1%, the corrosion rate of N80 steel in hydrochloric acid solution at 90? is 3.3325 g m-2 h-1. Electrochemical and surface morphology analysis show that DTEBTAC can form a protective layer on the surface of N80 steel, and is a hybrid corrosion inhibitor that can inhibit the main anode. Quantum chemical parameter calculation shows that DTEBTAC has a better corrosion inhibition effect than DTP. The molecular dynamics simulation results show that DTEBTAC has stronger binding energy than DTP, and forms a network packing structure through hydrogen bonding, and the adsorption stability is enhanced. Originality/value A novel cationic mercaptopyrimidine derivative quaternium-ammonium salt corrosion inhibitor was designed and provided. Compared with the prior art, the preparation method of the synthesized mercaptopyrimidine derivative quaternary ammonium salt corrosion inhibitor is simple, and the presence of nitrogen-positive ions, sulfur atoms and nitrogen-rich atoms has an obvious corrosion inhibition effect, which can be used to inhibit metal corrosion during oil and gas field exploitation. It not only expands the application field of new materials but also provides a new idea for the research and development of new corrosion inhibitors.

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

Cited by 3 publications

References 60 publications

Clindamycin Derivatives: Unveiling New Prospects as Potential Antitumor Agents

Clindamycin Derivatives: Unveiling New Prospects as Potential Antitumor Agents

Efficient synthetic strategies for fused pyrimidine and pyridine derivatives: A review

Research on the corrosion inhibition performance and mechanism of pyrimidine quaternary ammonium salt

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