Apteka Pod Gryfem, Bialystok 15-281, Legionowa Street 30/3, Poland.
Department of Organic Chemistry, Medical University, Bialystok 15-222, Mickiewicza Street 2c, Poland.
Mini Rev Med Chem. 2019;19(2):98-113. doi: 10.2174/1389557518666181009143203.
The DNA as the depository of genetic information is a natural target for chemotherapy. A lot of anticancer and antimicrobial agents derive their biological activity from their selective interaction with DNA in the minor groove and from their ability to interfere with biological processes such as enzyme catalysis, replication and transcription. The discovery of the details of minor groove binding drugs, such as netropsin and distamycin A, oligoamides built of 4-amino-1-methylpyrrole-2-carboxylic acid residues, allowed to develop various DNA sequence-reading molecules, named lexitropsins, capable of interacting with DNA precisely, strongly and with a high specificity, and at the same time exhibiting significant cytotoxic potential. Among such compounds, lexitropsins built of carbocyclic sixmembered aromatic rings occupy a quite prominent place in drug research. This work is an attempt to present current findings in the study of carbocyclic lexitropins, their structures, syntheses and biological investigations such as DNA-binding and antiproliferative activity.
DNA 作为遗传信息的储存库是化疗的天然靶标。许多抗癌和抗菌药物的生物活性来自于它们与 DNA 小沟的选择性相互作用，以及它们干扰酶催化、复制和转录等生物过程的能力。对诸如 netropsin 和 distamycin A 等小沟结合药物细节的发现，以及由 4-氨基-1-甲基吡咯-2-羧酸残基构建的寡聚酰胺，使得能够开发各种 DNA 序列读取分子，称为利妥昔单抗，能够精确、强烈和高度特异性地与 DNA 相互作用，同时具有显著的细胞毒性潜力。在这些化合物中，由碳环六元芳环构建的利妥昔单抗在药物研究中占据相当突出的地位。这项工作试图介绍碳环利妥昔单抗的研究现状，包括它们的结构、合成以及 DNA 结合和抗增殖活性等生物研究。
