Six‐Membered Aromatic Nitrogen Heterocyclic Anti‐Tumor Agents: Synthesis and Applications

The Chemical Record, Год журнала: 2023, Номер 23(12)

Опубликована: Ноя. 27, 2023

Cancer stands as a serious malady, posing substantial risks to human well-being and survival. This underscores the paramount necessity explore investigate novel antitumor medications. Nitrogen-containing compounds, especially those derived from natural sources, form highly significant category of agents. Among these, agents with six-membered aromatic nitrogen heterocycles have consistently attracted attention chemists pharmacologists. Accordingly, we present comprehensive summary synthetic strategies clinical implications these compounds in this review. entails an in-depth analysis synthesis pathways for pyridine, quinoline, pyrimidine, quinazoline. Additionally, historical progression, targets, mechanisms action, effectiveness small molecule inhibitors possessing structural features.

Язык: Английский

---

Microwave assisted synthesis, biological assessment and in-silico studies of some new 5,5′-(phenylmethylene)bisuracil and dihydropyrido[2,3-d:6,5-d']dipyrimidine derivatives as selective COX-2 inhibitors with potential anti-inflammatory activities

Journal of Molecular Structure, Год журнала: 2025, Номер unknown, С. 141504 - 141504

Опубликована: Янв. 1, 2025

Язык: Английский

---

Design, Synthesis, Drug-Likeness, anti-Inflammatory, Antimicrobial Activity, and Molecular Docking Studies of Pyrimidine Analogs

Polycyclic aromatic compounds, Год журнала: 2024, Номер unknown, С. 1 - 13

Опубликована: Апрель 1, 2024

Grounded on medicinal significances of pyrimidines, herein we are reporting initially the design and synthesis 1-(2-benzylthiopyrimidin-4-yl)-benzimidazol-2-thioacetic acid/thioacetate 2(a, b), 1-(2-benzylthiopyrimidin-4-yl)-3,5 diaryl-2-pyrazoline (3) 1-(2-benzylthiopyrimidin-4-yl)-3,5-dimethylpyrazole (4). In silico screening such as molecular docking studies these compounds with inflammation-causing enzyme cyclooxagenase-2 (COX-2) suggests that only 2a has shown a strong affinity for COX-2 (−9.0 kcal/mol) forms three hydrogen bonds active amino acid residues in comparison standard anti-inflammatory drugs celecoxib (-8.8 indomethacin (-7.7 kcal/mol). However, vitro, activity reveals IC50 compound was 3.5 μM compared to 0.65 μM. Also, displayed comparable antibacterial drug gentamycin against E. coli MIC 6.5 Furthermore, drug-likeness potent studied using Swiss ADME Mol inspiration software. All showed optimum without violating Lipinski's rule five. With our best observation based comparative SAR analogs indomethacin, conclude could develop therapeutically agent.

Язык: Английский

---

Synthesis, Antimicrobial Activity, Drug-likeness, and Molecular Docking Studies of Novel 3-((2-(Benzylthio)-5-(phenylselanyl) pyrimidin-4-yl)amino)-2-(4-substituted phenyl)thiazolidin-4-ones

Organic Preparations and Procedures International, Год журнала: 2024, Номер unknown, С. 1 - 7

Опубликована: Июнь 5, 2024

Язык: Английский

---

Synthesis of 2-azido-4-chloro-6-phenylpyrimidine-5-carbaldehyde and its transformations in DMSO

Russian Chemical Bulletin, Год журнала: 2024, Номер 73(7), С. 2014 - 2022

Опубликована: Июль 1, 2024

Язык: Английский

---

Kinetic and thermodynamic characteristics of the azide-tetrazole rearrangement of 4,6-substituted 2-azidopyrimidines

Russian Chemical Bulletin, Год журнала: 2024, Номер 73(9), С. 2616 - 2623

Опубликована: Сен. 1, 2024

Язык: Английский

---