The Thiocarboxanilides UC-10 and UC-781 Have an Additive Inhibitory Effect against Human Immunodeficiency Virus Type 1 Reverse Transcriptase and Replication in Cell Culture When Combined with other Antiretroviral Drugs
作者： J Balzarini , E De Clercq
DOI: 10.1177/095632029700800303
关键词:
摘要: The thiocarboxanilides represent a structural class of potent and selective human immunodeficiency virus type 1 (HIV-1)-specific reverse transcriptase (RT) inhibitors. Combinations the clinical candidate UC-10 (oxime ether derivative) UC-781 (pentenyloxy with variety nucleoside RT inhibitors (NRTls) non-nucleoside (NNRTls), two HIV protease one fusion/uncoating inhibitor were evaluated for their inhibitory effects on HIV-1 activity replication in CEM cell cultures. NNRTls including UC-10, UC-781, nevirapine, BHAP, α-APA, 8-chloro-TIBO, MKC-442 quinoxaline HBY 097 against was highly dependent nature template/primer used reaction. However, fractionary concentration (FIC) indexes all drug concentrations combination experiments other fell within range 0.5-1.5. This points to predominantly additive effect inhibition RT. Similar FIC observed NRTI triphosphates AZT-TP, d4T-TP, ddCTP, ddATP 3TC-TP diphosphate PMEApp All these combinations showed similar culture. Also, or Ro31-8959/008 ABT 84538.0 bicyclam JM 3100 an (FIC 0.5-1.5 range). Thus, irrespective drugs, proved merely additive. In no case antagonistic anti-HIV increased cytotoxicity observed. conclusion, combined clinically agents result activity.
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