吲哚——查耳酮杂合体的抗肿瘤活性

Therapeutic Potential of Indole-chalcone Hybrids as Anticancer Agents

癌症是一种异质性疾病,具有细胞分化和增殖异常、生长失去控制、浸润性和转移性等生物学特征。在世界范围内,癌症的发病率和死亡率不断攀升。目前,癌症已成为全世界最主要的致死原因之一。随着抗癌新药的不断问世,绝大多的癌症已能被治愈或缓解症状。然而,抗癌药物的毒副作用和耐药性已成为治疗癌症的主要障碍。因此,迫切需要开发新型抗癌药物。吲哚和查耳酮类化合物广泛存在于自然界,具有毒副作用低和生物活性谱广等诸多优点,是寻找抗癌药物的常见结构。值得一提的是,吲哚—查耳酮杂合体可同时作用于肿瘤细胞的多个靶点,具有提高抗肿瘤活性和克服耐药性的潜力。本文将总结近十年来所发展的具有抗肿瘤活性的吲哚—查耳酮杂合体,并探讨其构—效关系和作用机制。

Cancer, a heterogeneous disease and has the biological characteristics of abnormal cell differentiation and proliferation, uncontrolled growth, invasion and metastasis. The morbidity and mortality of cancer increased greatly in recent years across the world, and at present, cancer is one of the foremost causes of death globally. With the advent of new drugs, most cancers can be cured or relieved. However, the side effects and drug resistance of anticancer drugs have become the main obstacles for the effective therapy, creating an urgent demand to develop novel anticancer agents. Indoles and chalcones, ubiquitous in nature, possess many advantages, such as low side effects and broad biological activity spectrum, and are useful scaffolds for the development of novel anticancer agents. In particular,indole-chalcone hybrids could act on multiple targets in cancer cells simultaneously and have the potential to enhance anticancer activity and conquer drug resistance. This review will focus on the anticancer potential of indole-chalcone hybrids developed in recent decade, with special emphasis on the structure-activity relationships and mode of action.