Abstract |
L-N-MCd4T (1) has been synthesized as a potent anti-HIV agent starting from (R)- epichlorohydrin using tandem alkylation, chemoselective reduction of ester in the presence of lactone functional group, RCM reaction and Mitsunobu reaction as key steps and was found to be a very potent anti-HIV-1 (EC50 = 6.76 microg mL(-1)) agent without cytotoxicity up to 100 microg mL(-1), indicating that the anti-HIV-1 activity found is similar to that of ddI (EC50 = 4.95 microg mL(-1)), which is used clinically for the treatment of AIDS patients.
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Authors | Ah-Young Park, Hyung Ryong Moon, Kyung Ran Kim, Moon Woo Chun, Lak Shin Jeong |
Journal | Organic & biomolecular chemistry
(Org Biomol Chem)
Vol. 4
Issue 22
Pg. 4065-7
(Nov 21 2006)
ISSN: 1477-0520 [Print] England |
PMID | 17312958
(Publication Type: Journal Article, Research Support, Non-U.S. Gov't)
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Chemical References |
- 1-(5-(hydroxymethyl)bicyclo(3.1.0)hex-3-en-2-yl)-5-methyl-1,3-dihydropyrimidine-2,4-dione
- Anti-HIV Agents
- Bridged Bicyclo Compounds
- Thymidine
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Topics |
- Anti-HIV Agents
(chemical synthesis, chemistry, pharmacology)
- Bridged Bicyclo Compounds
(chemical synthesis, chemistry, pharmacology)
- HIV
(drug effects)
- Humans
- Lymphocytes
(drug effects)
- Microbial Sensitivity Tests
- Molecular Conformation
- Stereoisomerism
- Thymidine
(analogs & derivatives, chemical synthesis, chemistry, pharmacology)
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