肿瘤是危害人类健康的重大疾病，不仅给病人造成难以忍受的痛苦，而且还会给家庭带来经济损失，给国家和社会造成沉重的负担。如何预防和治疗肿瘤是世界各国医药科研工作者的一项重要课题。真核细胞翻译起始因子4E（eIF4E）是极具吸引力的治疗肿瘤疾病的新靶点，我们前期研究发现多个靶向eIF4E溴酚杂合体。本项目将综合集成分子杂合、多样性导向合成、“点击”化学和计算机辅助药物设计等各种方法技术优势，将溴酚与上市抗肿瘤药物分子的优势药效基团进行合理组合构建靶向eIF4E溴酚杂合体组合库，进行抗肿瘤活性及构效关系研究，明晰高活性化合物抗肿瘤作用机制并对其成药前景进行初步评价，为将溴酚类化合物开发成具有独立知识产权的新型抗肿瘤海洋药物提供理论科学依据和物质基础。

Cancer is one of the most serious diseases, which not only cause pain to the patient, but also bring economic loss to the patient's family and heaven burden for the society. How to prevent and therapy cancer is the important subject for the medicinal researchers in the world. With evidence implicating the eIF4E complex in tumorigenesis, the development of eIF4E-specific anticancer therapies has begun to attract attention. This project will be construct novel molecular hybrids libraries of bromophenols containing the advantages of the pharmacophore active fragments of bromophenols with other anti-tumor drug molecules based on our previous study results by employing diversity-oriented synthesis (DOS), “click” chemistry and computer-aided drug design (CADD) methods. The structure-activity relationships of bromophenol hybrids will be discussed when the antitumor activities screening were finished. The mechanisms of lead compound will be explored along with its primary pharmaceutical parameters in order to developing it as novel anticancer drugs targeting eIF4E. This research would provide scientific basis for the developing bromophenols as novel anticancer drugs of marine with independent intellectual property right and be significant for prevention and chemotherapy of cancer.