Structure-activity relationship of in vitro antiviral and cytotoxic activity of semisynthetic analogues of scopadulane diterpenes.
Fourteen semisynthetic compounds derived from the natural scopadulane-type diterpenes thyrsiflorin A (4), B (5), and C (6), including several precursors, have been examined in vitro for their antiherpetic activity against Herpes simplex virus type II (HSV-2) and cytotoxicity against two human tumor cell lines. Four of these compounds showed moderate antiherpetic activity, but none of them exhibited a significant cytotoxicity against the cell lines used. Some structure-activity relationships have been identified for the antiviral activity in these scopadulane derivatives as well as important structural features for the cytotoxic activity.
Betancur-Galvis
L
L
Grupo Inmunovirología-Biogénesis, Universidad de Antioquia, A.A1226, Medellín-Colombia, Spain. labeta@catios.udea.edu.co
Zuluaga
C
C
Arnó
M
M
González
M A
MA
Zaragozá
R J
RJ
D000818:Animals; D000972:Antineoplastic Agents, Phytogenic / Q000737:chemistry / Q000302:isolation & purification* / Q000494:pharmacology; D000998:Antiviral Agents / Q000737:chemistry / Q000302:isolation & purification* / Q000494:pharmacology; D016466:CHO Cells / Q000187:drug effects; D002417:Cattle; D002470:Cell Survival / Q000187:drug effects; D002478:Cells, Cultured / Q000187:drug effects; D002522:Chlorocebus aethiops; D006224:Cricetinae; D004224:Diterpenes / Q000737:chemistry / Q000302:isolation & purification* / Q000494:pharmacology; D004423:Ear; D005260:Female; D006367:HeLa Cells / Q000187:drug effects; D018258:Herpesvirus 2, Human / Q000187:drug effects; D006801:Humans; D020128:Inhibitory Concentration 50; D007668:Kidney; D007822:Laryngeal Neoplasms; D010053:Ovary; D010946:Plants, Medicinal / Q000737:chemistry*; D012867:Skin / Q000187:drug effects; D013329:Structure-Activity Relationship; D014407:Tumor Cells, Cultured / Q000187:drug effects; D002583:Uterine Cervical Neoplasms; D014709:Vero Cells / Q000187:drug effects
D000972:Antineoplastic Agents, Phytogenic; D000998:Antiviral Agents; D004224:Diterpenes; C440673:thyrsiflorin A; C440674:thyrsiflorin B; C415031:thyrsiflorin C