Anti-AIDS agents. Part 56: Synthesis and anti-HIV activity of 7-thia-di-O-(-)-camphanoyl-(+)-cis-khellactone (7-thia-DCK) analogs.
Two thia-DCK analogs (3a,b) were synthesized and evaluated for inhibition of HIV-1 replication in H9 lymphocytes. Compound 3a showed potent anti-HIV activity with an EC50 value of 0.14 microM and a therapeutic index of 1110. However, the corresponding 6-tert-butyl-substituted compound (3b) showed no suppression. The bioassay results indicated that thia-DCK analogs merit attention as potential HIV-1 inhibitors.
Chen
Ying
Y
Department of Medicinal Chemistry, School of Pharmacy, Fudan University, Shanghai 200032, China.
Zhang
Qian
Q
Zhang
Beina
B
Xia
Peng
P
Xia
Yi
Y
Yang
Zheng-Yu
ZY
Kilgore
Nicole
N
Wild
Carl
C
Morris-Natschke
Susan L
SL
Lee
Kuo-Hsiung
KH
D019380:Anti-HIV Agents / Q000138:chemical synthesis* / Q000494:pharmacology; D002460:Cell Line; D006678:HIV / Q000187:drug effects; D006801:Humans; D020128:Inhibitory Concentration 50; D007783:Lactones / Q000138:chemical synthesis / Q000494:pharmacology; D008214:Lymphocytes / Q000821:virology; D013329:Structure-Activity Relationship; D013871:Thiones / Q000138:chemical synthesis / Q000494:pharmacology
D019380:Anti-HIV Agents; D007783:Lactones; D013871:Thiones