Anti-AIDS agents. Part 58: synthesis and anti-HIV activity of 1-thia-di-O-(-)-camphanoyl-(+)-cis-khellactone (1-thia-DCK) analogues.
Two 1-thia-DCK analogues (9a and 9b) were synthesized and evaluated for inhibition of HIV-1 replication in H9 lymphocytes. Compound 9a showed excellent anti-HIV activity with an EC(50) value of 0.00012 microM and therapeutic index of 1408000. Compound 9b was less active with EC(50) and TI values of 3.11 microM and 62.3, respectively. The bioassay results indicated that thia-DCK analogues merit attention as potential HIV-1 inhibitors.
Xia
Peng
P
Department of Medicinal Chemistry, School of Pharmacy, Fudan University, Shanghai 200032, China. pxia@shmu.edu.cn
Yin
Zhi-Jian
ZJ
Chen
Ying
Y
Zhang
Qian
Q
Zhang
Beina
B
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; D002164:Camphor / Q000031:analogs & derivatives* / Q000138:chemical synthesis* / Q000494:pharmacology; D002460:Cell Line; D015497:HIV-1 / Q000187:drug effects* / Q000502:physiology; D006801:Humans; D007783:Lactones / Q000138:chemical synthesis* / Q000494:pharmacology; D013601:T-Lymphocytes / Q000187:drug effects / Q000821:virology; D014779:Virus Replication / Q000187:drug effects
C479985:3'R,4'R-di-O-(-)-camphanoyl-(+)-cis-khellactone; D019380:Anti-HIV Agents; D007783:Lactones; D002164:Camphor