中文摘要：

本文评价了5个二甲苯酮类非核苷类逆转录酶抑制剂（DY1203、DY1204、DY1119、DY1208和DY1209）的体外抗HIV-1药效学。采用MTT法检测了5个化合物对人T淋巴细胞系（C8166、MT-4、H9）和PBMC的毒性作用;p24抗原ELISA方法测定了化合物对1株HIV-1实验株、4株耐药株和3株临床株的抗病毒活性;HIV逆转录酶试剂盒检测了化合物体外对HIV-1重组逆转录酶的抑制活性。结果表明,5个化合物中,DY1203和DY1204对不同细胞的毒性均很小（CC50〉200μg·m L^-1）。DY1119、DY1208和DY1209具有显著的抗病毒活性,对实验株HIV-1IIIB、NRTI耐药株HIV-174V、PI耐药株HIV-1RF/V82F/184V、FI耐药株HIV-1NL4-3 gp41（36G）N42S和临床分离株（HIV-1KM018、HIV-1TC-1、HIV-1Wan）均有很强的抑制作用,而NNRTI耐药株HIV-1A17对其有不同程度耐药。5个化合物对HIV-1重组逆转录酶有不同程度的抑制效应,其中DY1208有显著的抗HIV-1活性和较高的治疗指数,安全性高,有望成为新的抗HIV-1先导化合物。

英文摘要：

o evaluate the anti-HIV-1 activities of 5 benzophenones non-nucleoside reverse transcriptase inhibitors （NNRTIs） such as DY1203, DY1204, DY1119, DY1208 and DY1209 in vitro, the cytotoxicity of 5 compounds were tested on C8166, MT-4, H9 and PBMC with the MTT assay. The anti-HIV-1 activities of compounds were evaluated on laboratory-adapted strain, drug-resistant strains and primary isolated strains by p24 antigen expression ELISA. The inhibition of HIV-1 recombinant reverse transcriptase activity was assessed by ELISA assay. Among 5 compounds, DY1203 and DY1204 showed low cytotoxicities with CC50 greater than 200 μg·mL^-1. DY1119, DY1208 and DY1209 showed strong anti-HIV-1 activities against HIV-1IIIB, HIV-174V, HIV-1RF/V82F/184V, HIV-1NL4-3 gp41（36G） N42S, HIV-1KM018, HIV-1TC-1 and HIV-1Wan. However, NNRTIs drug-resistant strain HIV-1A17 showed different resistance to these compounds. The 5 compounds proved active against HIV-1 recombinant reverse transcriptase. DY1208 is expected to become a new lead compound for its high therapeutic index. The results can provide new information for HIV-1 drug research and promote the development of new HIV-1 drugs.