Scabrosin esters and derivatives: chemical derivatization studies and biological evaluation.
Several derivatives of the natural scabrosin esters were synthesized in order to elucidate the structural features present, which are responsible for the biological activities. The studies demonstrate that full anti-proliferative activities of the scabrosin esters, both the carboskeleton core as well as the ability to form the dithiol and/or the disulfide linkage of the epidithiopiperazine-2,5-dione are required. The presence of the epoxide rings on the scabrosin esters do not contribute to the observed biological activities.
Chai
Christina L L
CL
Centre for the Study of Bioactive Molecules, Department of Chemistry, Australian National University, Canberra ACT 0200, Australia. christina.chai@anu.edu.au
Elix
John A
JA
Huleatt
Paul B
PB
Waring
Paul
P
D000818:Animals; D001685:Biological Factors / Q000737:chemistry* / Q000302:isolation & purification* / Q000494:pharmacology; D001688:Biological Products / Q000138:chemical synthesis / Q000494:pharmacology; D045744:Cell Line, Tumor; D004353:Drug Evaluation, Preclinical / Q000379:methods; D004952:Esters; D051379:Mice
D001685:Biological Factors; D001688:Biological Products; D004952:Esters