New small-molecule tubulin inhibitors
New small-molecule tubulin inhibitors
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DOI：
10.1351/pac200173091459
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发表时间：
2001-09-01
影响因子：
1.8
通讯作者：
Nickel, B
中科院分区：
文献类型：
--
作者：
Bacher, G;Beckers, T;Nickel, B
针对微管蛋白系统的生物制剂的种类超过了作用于DNA的生物制剂，使其成为癌症化疗的重要靶点。然而，复杂的化学结构和难以获得的自然资源，再加上耐药性的发展，限制了第一代天然产物的发展。在寻找和合成新的合成化合物（如小分子微管蛋白抑制剂）方面所做的大量努力，为新的潜在/有前途的药物提供了途径。在这些物质中，两个系列的新颖的，容易获得的吲哚类被确定为微管蛋白不稳定剂。由于D-24851和D-64131的合成性质、体外和体内抗肿瘤活性以及对多药耐药（MDR）肿瘤的疗效，它们在癌症治疗中具有重要的潜力。
The variety of biological agents directed toward the tubulin system exceeds those acting on DNA, making it an important target for cancer chemotherapy. However, the complicated chemical structures and restricted access to the natural resources, in combination with the development of drug resistance, limit the first generation of natural products. Considerable efforts in the search and synthesis of new synthetic compounds, such as small molecular tubulin inhibitors, gave access to novel potential/promising drugs. Among these substances, two series of novel, easily accessible indole classes were identified as tubulin-destabilizing agents. Owing to the synthetic nature, potent in vitro and in vivo antitumoral activity, and efficacy against multidrug-resistant (MDR) tumors, D-24851 and D-64131 have significant potential in cancer treatment.