Wang Gangqiang, Sun Shaofa, Guo Hua
Hubei Key Laboratory of Radiation Chemistry and Functional Materials, Non-power Nuclear Technology Collaborative Innovation Center, School of Nuclear Technology and Chemistry & Biology, Hubei University of Science and Technology, Xianning, 437100, PR China; School of Pharmaceutical Sciences, South-Central University for Nationalities, Wuhan, 430074, PR China.
Hubei Key Laboratory of Radiation Chemistry and Functional Materials, Non-power Nuclear Technology Collaborative Innovation Center, School of Nuclear Technology and Chemistry & Biology, Hubei University of Science and Technology, Xianning, 437100, PR China.
Eur J Med Chem. 2022 Feb 5;229:113999. doi: 10.1016/j.ejmech.2021.113999. Epub 2021 Nov 20.
The drug resistance and low specificity of current available chemotherapeutics to cancer cells are the main reasons responsible for the failure of cancer chemotherapy and remain dramatic challenges for cancer therapy, creating an urgent need to develop novel anticancer agents. Carbazole nucleus, widely distributed in nature, is a predominant feature of a vast array of biologically active compounds. Carbazole derivatives exhibited potential antiproliferative activity against different cancer cell lines by diverse mechanisms, inclusive of arrest cell cycle and induce apoptosis, and several anticancer agents are carbazole-based compounds. Thus, carbazole derivatives represent a fertile source for discovery of novel anticancer therapeutic agents. Over the past several years, a variety of carbazole hybrids have been developed as potential anticancer agents. The present review focuses on the recent progress, from 2016 until now, in knowledge on anticancer properties, structure-activity relationships and mechanisms of action of carbazole hybrids to provide a basis for development of relevant therapeutic agents.
目前可用的化疗药物对癌细胞的耐药性和低特异性是癌症化疗失败的主要原因，并且仍然是癌症治疗面临的巨大挑战，这迫切需要开发新型抗癌药物。咔唑核在自然界中广泛分布，是大量生物活性化合物的主要特征。咔唑衍生物通过多种机制对不同癌细胞系表现出潜在的抗增殖活性，包括阻滞细胞周期和诱导凋亡，并且几种抗癌药物是以咔唑为基础的化合物。因此，咔唑衍生物是发现新型抗癌治疗药物的丰富来源。在过去几年中，已经开发了多种咔唑杂化物作为潜在的抗癌药物。本综述重点关注2016年至今咔唑杂化物抗癌特性、构效关系和作用机制方面的最新进展，为相关治疗药物的开发提供依据。
