恶性肿瘤的发生和发展是极其复杂的，涉及多种不同的病生理过程、多组基因、多条信号传导通路和多个生物分子靶点，单一的治疗方式很难达到令人满意的肿瘤治疗效果。联合治疗，尤其是光动力治疗和化疗的联合治疗，已成为恶性肿瘤高效精准治疗的重要方法。但目前光敏剂和化疗药物之间的联合方式未能最大限度地发挥二者的协同治疗效果。本项目拟以具有高光敏活性的酞菁锌作为光敏剂活性结构主体，以可被缺氧活化断裂的偶氮苯键作为连接链，修饰上集化疗活性和靶向功能为一体的小分子靶点药物酪氨酸激酶抑制剂，合成一系列在肿瘤缺氧条件下可控释放的靶向联合药物；通过对其光物理性质、缺氧活化释药效率、联合抗肿瘤效果和靶向性功能等参数进行系统表征，最后总结分析其构效关系，为今后发展高效精准的抗肿瘤药物提供依据，具有重大的科学意义和指导价值。

The occurrence and development of malignant tumor is extremely complex. It involves different pathological processes, multiple genes, signal transduction pathways and biological molecular targets. The attempts to treat malignant tumor with monotherapeutic approach are not always efficient. Therefore, combination therapy, especially the combinations of PDT and chemotherapy, is an important method in the efficient and precise treatment of malignant tumor. However, synergistic therapeutic effect has not been maximized. In this project, we choose zinc phthalocyanine as the photosensitizer, the azobenzene bone, which is cleaved under hypoxic tumor environment, as the linker; and then modify small molecule targeted drugs tyrosine kinase inhibitors which have anticancer activity and cancer targeting capability, to synthesize a series of targeted   combined drugs which can be activated under hypoxia in cancer. The parameters of photophysical properties, hypoxia activated drug released efficiency, combination therapy effect, and tumor targeted activity of the conjugates will be studied. Finally, the structure-activity relationship will be summarized and analyzed. Our study will provide the theoretical basis for developing efficient and precise anticancer drugs in future, and have great scientific significance and guiding values.