Mónica Costa Cerqueira , Ana Silva , Sofia Martins Sousa , Filipa Pinto-Ribeiro , Fátima Baltazar , Julieta Afonso , Marta Freitas Costa
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引用次数: 0
Abstract
Renal (RC) and bladder cancers (BC) are common urological malignancies prevalent in the male population. Incidence and mortality rates are expected to increase in the near future. Drug toxicity and development of drug resistance in both diseases are major obstacles to achieve successful treatments. Chromenes are heterocyclic compounds constituted by a benzene ring fused to a pyran nucleus. Natural and synthetic chromene-based compounds have proven to be promising anticancer agents. Additionally, re-sensitization of cancer cells to classical treatments has also been demonstrated. Thus, the aim of this systematic review is to assess the potential of chromene-based compounds in the treatment of RC and BC. Study collection was performed in six different databases, to compile existing information on preclinical (in vitro and in vivo) and clinical studies developed to date. Overall, multiple chromene-based compounds showed potent anticancer effects, affecting several biological features such as reduction in cell viability, proliferation, migration and invasion in vitro, and induction of cell cycle arrest and cell death. Tumor volume and weight were generally decreased in vivo upon chromene-based treatment. Modest results have been obtained in two clinical trials, with reports of a partial response and two objective responses in RC patients. Thus, the chromene family can be considered an attractive chemical scaffold, harboring promising drug candidates for RC and BC therapeutics.
肾癌(RC)和膀胱癌(BC)是男性常见的泌尿系统恶性肿瘤。预计在不久的将来,这两种癌症的发病率和死亡率都将上升。这两种疾病的药物毒性和耐药性是成功治疗的主要障碍。色烯是由苯环与吡喃核融合而成的杂环化合物。天然和合成的色烯化合物已被证明是很有前途的抗癌剂。此外,癌细胞对传统疗法的再敏感性也已得到证实。因此,本系统综述旨在评估铬基化合物在治疗 RC 和 BC 方面的潜力。研究收集工作在六个不同的数据库中进行,以汇编迄今为止临床前(体外和体内)和临床研究的现有信息。总体而言,多种基于铬的化合物显示出了强大的抗癌作用,影响了多种生物学特征,如降低体外细胞活力、增殖、迁移和侵袭,诱导细胞周期停滞和细胞死亡。使用铬化物治疗后,体内肿瘤的体积和重量普遍减少。两项临床试验取得了适度的效果,RC 患者出现了部分反应和两次客观反应。因此,铬烯家族可被视为一种极具吸引力的化学支架,蕴藏着治疗 RC 和 BC 的候选药物。
期刊介绍:
Bioorganic Chemistry publishes research that addresses biological questions at the molecular level, using organic chemistry and principles of physical organic chemistry. The scope of the journal covers a range of topics at the organic chemistry-biology interface, including: enzyme catalysis, biotransformation and enzyme inhibition; nucleic acids chemistry; medicinal chemistry; natural product chemistry, natural product synthesis and natural product biosynthesis; antimicrobial agents; lipid and peptide chemistry; biophysical chemistry; biological probes; bio-orthogonal chemistry and biomimetic chemistry.
For manuscripts dealing with synthetic bioactive compounds, the Journal requires that the molecular target of the compounds described must be known, and must be demonstrated experimentally in the manuscript. For studies involving natural products, if the molecular target is unknown, some data beyond simple cell-based toxicity studies to provide insight into the mechanism of action is required. Studies supported by molecular docking are welcome, but must be supported by experimental data. The Journal does not consider manuscripts that are purely theoretical or computational in nature.
The Journal publishes regular articles, short communications and reviews. Reviews are normally invited by Editors or Editorial Board members. Authors of unsolicited reviews should first contact an Editor or Editorial Board member to determine whether the proposed article is within the scope of the Journal.