- Tytuł:
- Synthesis and anti-HIV properties of novel 6-phenylselenenyl-5-propyluracils
- Autorzy:
-
Miazga, Agnieszka
Felczak, Krzysztof
Siwecka, Maria
Lipniacki, Andrzej
Piasek, Andrzej
Kulikowski, Tadeusz - Powiązania:
- https://bibliotekanauki.pl/articles/1040887.pdf
- Data publikacji:
- 2007
- Wydawca:
- Polskie Towarzystwo Biochemiczne
- Tematy:
-
HIV reverse transcriptase
HIV-1
inhibitors - Opis:
- Novel 6-phenylselenenyl-5-propyluracils were synthesized from 5-propyluracil with the use of regioselective synthesis to give 1-[(2-hydroxyethoxy)-methyl]-6-phenylselenenyl-5-propyluracil (6), 1-ethoxymethyl-6-phenylselenenyl-5-propyluracil (9) and 1-benzyloxymethyl-6-phenylselenenyl-5-propyluracil (10). Interaction of these compounds with recombinant HIV-1 reverse transcriptase (RT) was evaluated using a non-isotopic colorimetric method. Compounds 9 and 10 exerted potent HIV RT inhibition (IC50 0.06 and 0.05 µM respectively) while compound 6 showed moderate inhibition (IC50 = 3.5 µM). Potent anti-HIV-1 activity in MT-2 cells inoculated by a syncythia-inducing HIV-1 (cat #3 strain) laboratory isolate was exerted by compounds 9 and 10 (EC50 0.62 µM and 0.025 µM, respectively), while compound 6 showed only moderate activity (IC50 = 4.1 µM). In addition, compound 10 showed very good in vitro therapeutic index (TI > 2046), indicating that it is a potential anti-HIV/AIDS drug.
- Źródło:
-
Acta Biochimica Polonica; 2007, 54, 4; 863-868
0001-527X - Pojawia się w:
- Acta Biochimica Polonica
- Dostawca treści:
- Biblioteka Nauki
Artykuł