Department of Forensic Chemistry and Toxicology, Government Institute of Forensic Science, Aurangabad 431 004, (MS), India.
Department of Chemistry, Biochemistry and Forensic Science, Amity School of Applied Sciences, Amity University, Haryana 122413, India.
Anticancer Agents Med Chem. 2022 Aug 4;22(16):2852-2875. doi: 10.2174/1871520622666220217161346.
Cancer is the most lethal disease that may be found anywhere globally. Approximately 10% of individuals die due to cancer of various types, with 19.3 million new cancer cases and 10 million deaths reported in 2020. More than 100 medications are commercially available for the treatment of cancer, but only a few candidates have high specificity, resulting in several side effects. The scientific community has spent the past decades focusing on drug discovery. Natural resources are used to isolate pharmaceutically active candidates, which are then synthesized in laboratories. More than 60% of all prescribed drugs are made from natural ingredients. Unique five-membered heteroaromatic center motifs with sulfur, oxygen and nitrogen atoms are found in heterocyclic compounds, such as indazole, thiazole, triazole, triazole, and oxazole, and are used as a core scaffold in many medicinally important therapies. Triazole possesses a wide range of pharmacological activities, including anticancer, antibacterial, antifungal, antibiotic, antiviral, analgesic, anti-inflammatory, anti-HIV, antidiabetic, and antiprotozoal activities. Novel triazole motifs with a variety of biological characteristics have been successfully synthesized using versatile synthetic methods. We intend here to facilitate the rational design and development of innovative triazole-based anti-cancer medicines with increased selectivity for various cancer cell lines by providing insight into various ligand-receptor interactions.
癌症是全球范围内最致命的疾病之一。全球每年约有 10%的人死于各种癌症，2020 年全球有 1930 万例新癌症病例和 1000 万人死亡。目前有超过 100 种药物可用于治疗癌症，但只有少数候选药物具有高特异性，导致多种副作用。科学界过去几十年来一直专注于药物发现。利用自然资源分离具有药用活性的候选药物，然后在实验室中进行合成。超过 60%的处方药都来自天然成分。杂环化合物中存在具有硫、氧和氮原子的独特五元杂芳环中心基序，如吲唑、噻唑、三唑、噻吩和噁唑，它们被用作许多具有重要医学意义的疗法的核心支架。三唑具有广泛的药理活性，包括抗癌、抗菌、抗真菌、抗生素、抗病毒、镇痛、抗炎、抗 HIV、抗糖尿病和抗原生动物活性。通过各种配体-受体相互作用的深入了解，利用多种通用的合成方法成功合成了具有各种生物学特性的新型三唑基序。我们旨在通过提供各种配体-受体相互作用的深入了解，促进具有创新性的基于三唑的抗癌药物的合理设计和开发，以提高对各种癌细胞系的选择性。
