Xu Z Q, Buckheit R W, Stup T L, Flavin M T, Khilevich A, Rizzo J D, Lin L, Zembower D E
MediChem Research Inc., Lemont, IL 60439, USA.
Bioorg Med Chem Lett. 1998 Aug 18;8(16):2179-84. doi: 10.1016/s0960-894x(98)00380-1.
The three chromanone derivatives, (+)-, (-)-, and (+/-)-12-oxocalanolide A (2), were evaluated for in vitro antiviral activities against HIV and simian immunodeficiency virus (SIV). The compounds were determined to be inhibitors of HIV-1 reverse transcriptase (RT) and exhibited activity against a variety of viruses selected for resistance to other HIV-1 nonnucleoside RT inhibitors. They are the first reported calanolide analogues capable of inhibiting SIV.
对三种色满酮衍生物,即(+)-、(-)-和(+/-)-12-氧代卡拉诺内酯A(2)进行了抗HIV和猿猴免疫缺陷病毒(SIV)的体外抗病毒活性评估。这些化合物被确定为HIV-1逆转录酶(RT)抑制剂,并对多种对其他HIV-1非核苷RT抑制剂耐药的病毒表现出活性。它们是首次报道的能够抑制SIV的卡拉诺内酯类似物。