Synthesis of novel ellipticine analogues and their inhibition of Moloney leukaemia reverse transcriptase

Bioorganic and Medicinal Chemistry Letters

Volumn 6, Issue 23, 1996, Pages 2831-2836

  Timári, Géza ^a   Soós, Tibor ^a   Hajós, György ^a   Messmer, András ^a   Nacsa, János ^b   Molnár, József ^b  

^a CTRL RES INSTITUTE FOR CHEMISTRY   (Hungary)

^b UNIVERSITY OF SZEGED   (Hungary)

Author keywords

[No Author keywords available]

Indexed keywords

ELLIPTICINE DERIVATIVE; RNA DIRECTED DNA POLYMERASE; ZIDOVUDINE;

ARTICLE; DOSE RESPONSE; DRUG SYNTHESIS; ENZYME INHIBITION; IN VITRO STUDY; MOLONEY LEUKEMIA ONCOVIRUS;

LEUKAEMIA VIRUS; MOLONEY MURINE LEUKEMIA VIRUS; ONCOVIRINAE;

EID: 0030568131     PISSN: 0960894X     EISSN: None     Source Type: Journal    
DOI: 10.1016/S0960-894X(96)00521-5     Document Type: Article

References (22)

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20. 2, 300 mM KCl, and 100 mM DTT. In all experiments the final volume of reaction assay was 20 μl This contained water, 2μl/10x buffer, 20 μg/ml template-primer, 5 μM dTTP precursor (New England BioLabs), 0,2 μCi triciated precursor, reverse transcriptase and the compounds tested which were administrated in the reaction medium for 10 minutes before adding the RT, in 20μl final volume. The assay was initiated by 5U reverse transcriptase followed by an incubation for 40 min at 37°C. 15 μl of the mixture was then transferred to a DE81 filter paper disc, washed and radioactivity measured by Packard Tri-Carb 4530 liquid scintillation counter. The residual enzymatic activities were calculated relative to the activity in percent when no drug was added.
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22. -7) which blocks the enzyme activity at the nucleoside binding site. We assume, however, that our ellipticine analogues are able to block the reverse transcriptase activity at the so called non nucleoside binding site of the enzyme due to sterical fitness.