草药被用作现代医学的补充,用于治疗癌症、炎症和糖尿病等人类疾病。香兰素等食品中的营养成分产生抗氧化和抗癌活性,其中许多对人体产生的副作用很小。因此,结合草药和营养成分的策略可以产生毒性降低的化合物。最近,我们开发了 GZ16.007,它是一种组合的洋甘菊碱和姜黄素,目前正在进行癌症治疗的临床评估。与姜黄素的利用相反,我们在此报告了一种新型支架的合成,该支架利用哈马林和香草醛作为营养成分来形成新发现的抗癌支架。确定包含两个哈马林分子和一个当量的香草醛产生了对各种人类癌细胞系具有活性的二聚体产物。本文讨论了二聚体支架的合成、评估和初步 SAR 研究。
The first Fe-catalysed alkylation of 2-methyl and 4-methyl-azaarenes with a series of alkyl and hetero-aryl alcohols is reported (>39 examples and up to 95% yield). Multi-functionalisation of pyrazines and synthesis of anti-malarial drug (±) Angustureine significantly broaden the scope of this methodology. Preliminary mechanistic investigation, deuterium labeling and kinetic experiments including trapping
Novel fused tricyclic or bicyclic dimers, such as β-carboline and quinoline moieties with a central linker, exhibit anti-cancer activities against a variety of human cancer cell lines. The dimer compounds can be used in anti-cancer therapeutic compositions useful in the treatment of human cancers.
Novel fused tricyclic or bicyclic dimers, such as β-carboline and quinoline moieties with a central linker, exhibit anti-cancer activities against a variety of human cancer cell lines. The dimer compounds can be used in anti-cancer therapeutic compositions useful in the treatment of human cancers.