1594
J. Nat. Prod. 2002, 65, 1594-1597
Anti-HIV Agents Derived from the ent-Kaurane Diterpenoid Linearol Maurizio Bruno,*,† Sergio Rosselli,† Ivana Pibiri,† Nicole Kilgore,‡ and Kuo-Hsiung Lee§ Dipartimento di Chimica Organica, Universita` di Palermo, Viale delle Scienze, 90128 Palermo, Italy, Panacos Pharmaceuticals, Inc., 209 Perry Parkway, Gaithersburg, Maryland 20879, and Natural Products Laboratory, School of Pharmacy, University of North Carolina, Chapel Hill, North Carolina 27599 Received January 28, 2002
Twenty-six semisynthetic ent-kaurane derivatives of linearol (1) have been investigated for their antiHIV effects. Five compounds (4, 7, 11, 25, and 26) showed significant activity against HIV replication in H9 lymphocyte cells with EC50 values in the range 100 >100 20.6 >100 22.2 16.0 1.8 2.2 2.0 1.9 10.8 21.4 >100 >100 5.4 6.0 5.3 59.8 57.7 41.1 54.0 60.1 5.3 50.6 52.5 5.6
N.S. N.S. N.S. 163 N.S. N.S. 6.10 N.S. N.S. N.S. >19.2 3.49 N.S. N.S. N.S. N.S. N.S. N.S. N.S. N.S. N.S. N.S. N.S. N.S. 184 50.1 N.S.
a
N.S. N.S. 0.13 N.S. N.S. 2.63 N.S. N.S. N.S.
