Anti-HIV agents derived from the ent-kaurane diterpenoid linearol.
Twenty-six semisynthetic ent-kaurane derivatives of linearol (1) have been investigated for their anti-HIV effects. Five compounds (4, 7, 11, 25, and 26) showed significant activity against HIV replication in H9 lymphocyte cells with EC(50) values in the range <0.1-3.11 microg/mL. With TI values of 163 and 184, compounds 4 and 25 are especially promising for further development as potential anti-HIV agents.
Bruno
Maurizio
M
Dipartimento di Chimica Organica, Università di Palermo, Viale delle Scienze, 90128 Palermo, Italy. bruno@dicpm.unipa.it
Rosselli
Sergio
S
Pibiri
Ivana
I
Kilgore
Nicole
N
Lee
Kuo-Hsiung
KH
D019380:Anti-HIV Agents / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology; D020650:Combinatorial Chemistry Techniques; D004224:Diterpenes / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology; D006678:HIV / Q000187:drug effects; D006801:Humans; D008214:Lymphocytes / Q000187:drug effects / Q000821:virology; D009682:Magnetic Resonance Spectroscopy; D015394:Molecular Structure; D031365:Sideritis / Q000737:chemistry*
D019380:Anti-HIV Agents; D004224:Diterpenes; C471495:linearol