Pharmaceutical Organic Chemistry Department, Faculty of Pharmacy, Cairo University, 33 Kasr El-Aini Street, Cairo 11562, Egypt.
Eur J Med Chem. 2013 Apr;62:614-31. doi: 10.1016/j.ejmech.2013.01.031. Epub 2013 Feb 5.
Cancer is considered as one of the most serious health problems. Despite the presence of many effective chemotherapeutic agents, their severe side effects together with the appearance of mutant tumors limit the use of these drugs and increase the need for new anticancer agents. Eg5 represents an attractive target for medicinal chemists since Eg5 is overexpressed in many proliferative tissues while almost no Eg5 is detected in nonproliferative tissues. Many Eg5 inhibitors displayed potent anticancer activity against some of the mutant tumors with limited side effects. The present review provides an overview about the progress in the discovery of Eg5 inhibitors especially from 2009 to 2012 as well as the clinical trials conducted on some of these inhibitors.
癌症被认为是最严重的健康问题之一。尽管有许多有效的化疗药物，但它们的严重副作用以及突变肿瘤的出现限制了这些药物的使用，并增加了对新抗癌药物的需求。Eg5 是医学化学家的一个有吸引力的靶标，因为 Eg5 在许多增殖组织中过度表达，而在非增殖组织中几乎检测不到 Eg5。许多 Eg5 抑制剂对一些突变肿瘤表现出很强的抗癌活性，副作用有限。本综述概述了 Eg5 抑制剂的发现进展，特别是 2009 年至 2012 年的进展，以及对其中一些抑制剂进行的临床试验。
