Morigi Rita, Locatelli Alessandra, Leoni Alberto, Rambaldi Mirella
Dipartimento di Farmacia e Biotecnologie FaBiT, Universita di Bologna, Via Belmeloro, 6. Bologna- 40126, Italy.
Recent Pat Anticancer Drug Discov. 2015;10(3):280-97. doi: 10.2174/1574892810666150708110432.
Cancer is a disease of remarkable importance in the world today and is projected to become the primary cause of death within the coming years, therefore the design and development of new antitumor agents is one of the most pressing research areas in medicinal chemistry. Considering the importance of thiazole ring as scaffold present in a wide range of therapeutic agents, the medicinal chemists have been encouraged to synthesize a large number of novel antitumors bearing this heterocycle, which furnish extensive synthetic possibilities due to the presence of several reaction sites. The present review describes the patents from 2008 to present concerning new thiazole compounds useful for the development of new drug molecules. It has been divided according to the molecular target and describes the pathways involved in the biological activities and the structure of the most potent compounds, together with the screening results.
癌症是当今世界极为重要的一种疾病，预计在未来几年将成为主要死因，因此新型抗肿瘤药物的设计与开发是药物化学中最紧迫的研究领域之一。鉴于噻唑环作为众多治疗药物中的骨架的重要性，药物化学家们受到鼓舞，合成了大量含有这种杂环的新型抗肿瘤药物，由于存在多个反应位点，这些药物提供了广泛的合成可能性。本综述描述了2008年至今有关可用于开发新药分子的新型噻唑化合物的专利。它根据分子靶点进行了划分，描述了生物活性所涉及的途径以及最有效化合物的结构，同时还介绍了筛选结果。
