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Volumn 20, Issue 20, 2010, Pages 6020-6023

Exploration of piperidine-4-yl-aminopyrimidines as HIV-1 reverse transcriptase inhibitors. N-Phenyl derivatives with broad potency against resistant mutant viruses

Author keywords

HIV 1; Non nucleoside reverse transcriptase; Non nucleoside reverse transcriptase inhibitor (NNRTI)

Indexed keywords

BENZENE DERIVATIVE; NONNUCLEOSIDE REVERSE TRANSCRIPTASE INHIBITOR; PIPERIDINE 4 YL AMINOPYRIMIDINE DERIVATIVE; PIPERIDINE DERIVATIVE; PYRIMIDINE DERIVATIVE; RNA DIRECTED DNA POLYMERASE INHIBITOR; UNCLASSIFIED DRUG;

EID: 77956908369     PISSN: 0960894X     EISSN: None     Source Type: Journal    
DOI: 10.1016/j.bmcl.2010.08.068     Document Type: Article
Times cited : (38)

References (17)
  • 11
    • 77956926629 scopus 로고    scopus 로고
    • note
    • For a more detailed description of these syntheses see: Kertesz, D. J.; Brotherton-Pleiss, C.; Yang, M. US 2008/0146595.
  • 12
    • 77956927844 scopus 로고    scopus 로고
    • note
    • 50 values were obtained from a SPA heteropolymeric assay. RNA-dependent DNA polymerase activity was measured using a biotinylated primer oligonucleotide and tritiated dNTP substrate. Newly synthesized DNA was quantified by capturing the biotinylated primer molecules on streptavidin coated Scintillation Proximity Assay (SPA) beads (Amersham). Each value represents the average of at least two independent assays.
  • 14
    • 0023277417 scopus 로고
    • 50 values were obtained following incubation of compound with infected MT4 cells in the presence of 10% fetal bovine serum. The assay assesses the reduction in the cytopathic effect of HIV-1 on MT4 cells in the presence of HIV-RT inhibitors. Each value represents the average of at least two independent assays. For a detailed description of the antiviral assay see
    • 50 values were obtained following incubation of compound with infected MT4 cells in the presence of 10% fetal bovine serum. The assay assesses the reduction in the cytopathic effect of HIV-1 on MT4 cells in the presence of HIV-RT inhibitors. Each value represents the average of at least two independent assays. For a detailed description of the antiviral assay see: Pauwels, R.; De, C. E.; Desmyter, J.; Balzarini, J.; Goubau, P.; Herdewijn, P.; Vanderhaeghe, H.; Vandeputte, M. J. Virol. Methods, 1987, 16, 171.
    • (1987) J. Virol. Methods , vol.16 , pp. 171
    • Pauwels, R.1    De, C.E.2    Desmyter, J.3    Balzarini, J.4    Goubau, P.5    Herdewijn, P.6    Vanderhaeghe, H.7    Vandeputte, M.8
  • 15
    • 77956899191 scopus 로고    scopus 로고
    • note
    • Determination of potency versus wild type virus was repeated in the presence of 40% human serum (HS) for these compounds. The resulting 'protein shifted potency' as compared to the result with 10% FBS (see Ref. 14) is considered an indicator of potential for in vivo activity.
  • 17
    • 77956941499 scopus 로고    scopus 로고
    • note
    • Atomic coordinates for the structure of 11 bound to HIV-RT were deposited with the RCSB Protein Data Bank (PDB) under the access code 3 NBP.


* 이 정보는 Elsevier사의 SCOPUS DB에서 KISTI가 분석하여 추출한 것입니다.