Manyeruke Meloddy H, Olomola Temitope O, Majumder Swarup, Abrahams Shaakira, Isaacs Michelle, Mautsa Nicodemus, Mosebi Salerwe, Mnkandhla Dumisani, Hewer Raymond, Hoppe Heinrich C, Klein Rosalyn, Kaye Perry T
Bioorg Med Chem. 2015 Dec 15;23(24):7521-8. doi: 10.1016/j.bmc.2015.10.039.
Novel 3-hydroxy-3-phenylpropanoate ester-azidothymidine (AZT) conjugates have been prepared using Baylis-Hillman methodology, and their potential as dual-action HIV-1 Integrase and Reverse Transcriptase inhibitors has been explored using enzyme inhibition and computer modelling techniques; their activity and HeLa cell toxicity have been compared with those of their cinnamate ester analogues.
已采用贝利斯-希尔曼方法制备了新型3-羟基-3-苯基丙酸酯-叠氮胸苷（AZT）缀合物，并使用酶抑制和计算机建模技术探索了它们作为双作用HIV-1整合酶和逆转录酶抑制剂的潜力；已将它们的活性和对HeLa细胞的毒性与其肉桂酸酯类似物的活性和毒性进行了比较。
