Department of Chemistry, Amity School of Applied Sciences, Amity University, Lucknow Campus, 226028, India.
Department of Pharmaceutical Chemistry, GIPER, Kashipur, Uttarakhand, 244713, India.
Curr Protein Pept Sci. 2023;24(10):783-804. doi: 10.2174/1389203724666230227115305.
The cancer is still a major cause of death worldwide. Among different targets to design anticancer agents, caspase-3 is an important target as its cleavage and activation lead to apoptosis and finally, cancer cell death. Apart from some naturally occurring molecules, many small molecules have been reported as caspase-3 activators.
In view of the above, the objective has been to review the published work on small molecules reported as caspase-3 activators and their anticancer activity to get some novel lead molecules for designing novel molecules of improved cancer therapeutic.
Literature search has been carried out using different search engines like google, Elsevier, Science direct, RSC, . for the publications of small molecules as caspase-3 activators inducing apoptosis in cancer cells.
In this review, the small molecules showing caspase-3 cleavage and activation have been discussed under different broad chemical classes so as to provide some insight into the structural features responsible for caspase-3 activation leading to anticancer activity. The review also encompasses the established drugs, novel organometallics showing caspase-3 activation and anticancer activity.
A large number of small molecules including some established drugs and organometallics have shown cleavage and activation of caspase-3 leading to apoptosis and anticancer activity. Many reported potent molecules of different chemical classes may be useful as lead molecules for optimization of anticancer activity as well as they may provide an insight of structural features which may be useful in designing novel caspase-3 activators as anticancer agents for drug development.
癌症仍然是全球主要的死亡原因。在设计抗癌药物的不同靶点中，Caspase-3 是一个重要的靶点，因为其切割和激活导致细胞凋亡，最终导致癌细胞死亡。除了一些天然存在的分子外，许多小分子已被报道为 Caspase-3 激活剂。
鉴于上述情况，本研究旨在综述已发表的关于 Caspase-3 激活剂的小分子及其抗癌活性的研究工作，以期为设计新型抗癌治疗药物提供一些新的先导分子。
使用不同的搜索引擎（如 Google、Elsevier、Science Direct、RSC 等）对 Caspase-3 激活剂诱导癌细胞凋亡的小分子出版物进行了文献检索。
在本综述中，根据不同的化学类别讨论了显示 Caspase-3 切割和激活的小分子，以便深入了解导致抗癌活性的 Caspase-3 激活的结构特征。该综述还包括已上市药物、具有 Caspase-3 激活和抗癌活性的新型有机金属化合物。
大量的小分子，包括一些已上市药物和有机金属化合物，已显示出 Caspase-3 的切割和激活，从而导致细胞凋亡和抗癌活性。不同化学类别报道的许多有效分子可能作为优化抗癌活性的先导分子有用，并且它们可能为设计新型 Caspase-3 激活剂作为抗癌药物提供结构特征的见解。
