Soni Jay Prakash, Yeole Yogesh, Shankaraiah Nagula
Department of Medicinal Chemistry, National Institute of Pharmaceutical Education and Research (NIPER) Hyderabad 500037 India
RSC Med Chem. 2021 Mar 24;12(5):730-750. doi: 10.1039/d0md00422g. eCollection 2021 May 26.
Cancer is a huge burden on the healthcare system and is foremost cause of mortality across the globe. Among various therapeutic strategies, chemotherapy plays an enormous role in overcoming the challenges of treating cancer, especially in late stage detection. However, limitations such as extreme side/adverse effects and drug resistance associated with available drugs have impelled the development of novel chemotherapeutic agents. In this regard, we have reviewed the development of β-carboline-based chemotherapeutic agents reported in last five years. The review mainly emphasizes on the molecular hybrids of β-carbolines with various pharmacophores, their synthetic strategies, and anticancer evaluation. In addition, the mechanisms of action, studies, structural influence on the potency and selectivity among diverse cancer cell lines have been critically presented. The review updates readers on the diverse molecular hybrids prepared and the governing structural features of high potential molecules that can help in the future development of novel cytotoxic agents.
癌症是医疗保健系统的巨大负担,也是全球首要的死亡原因。在各种治疗策略中,化疗在克服癌症治疗挑战方面发挥着巨大作用,尤其是在晚期检测中。然而,现有药物存在的诸如极端副作用/不良反应和耐药性等局限性,推动了新型化疗药物的研发。在这方面,我们回顾了过去五年报道的基于β-咔啉的化疗药物的发展情况。该综述主要强调了β-咔啉与各种药效基团的分子杂化物、它们的合成策略以及抗癌评估。此外,还批判性地介绍了其作用机制、研究、结构对不同癌细胞系中效力和选择性的影响。该综述使读者了解所制备的各种分子杂化物以及高潜力分子的主导结构特征,这些有助于未来新型细胞毒性药物的开发。