Pim2 inhibitors from the Papua New Guinean plant Cupaniopsis macropetala.
Bioassay-guided fractionation of an organic extract from the leaves of Cupaniopsis macropetala resulted in the isolation of a new alkaloid, galloyl tyramine ( 1), together with the known flavonoid glycoside quercitrin ( 2). The structure of 1 was determined following 1D and 2D NMR, IR, UV, and MS data analysis. Compounds 1 and 2 displayed IC 50 values of 161 and 25 microM, respectively, in a Pim2 enzyme assay.
Davis
Rohan A
RA
Eskitis Institute, Griffith University, Brisbane, Australia.
Simpson
Moana M
MM
Nugent
Ryan B
RB
Carroll
Anthony R
AR
Avery
Vicky M
VM
Rali
Topul
T
Chen
Huawei
H
Qurallo
Barbara
B
Quinn
Ronald J
RJ
D005707:Gallic Acid / Q000031:analogs & derivatives* / Q000737:chemistry / Q000302:isolation & purification; D006801:Humans; D015394:Molecular Structure; D010219:Papua New Guinea; D018515:Plant Leaves / Q000737:chemistry; D010946:Plants, Medicinal / Q000737:chemistry*; D017346:Protein Serine-Threonine Kinases / Q000037:antagonists & inhibitors*; D011518:Proto-Oncogene Proteins / Q000037:antagonists & inhibitors*; D011794:Quercetin / Q000031:analogs & derivatives* / Q000737:chemistry / Q000302:isolation & purification / Q000494:pharmacology; D029631:Sapindaceae / Q000737:chemistry*; D014439:Tyramine / Q000031:analogs & derivatives* / Q000737:chemistry / Q000302:isolation & purification
C490587:PIM2 protein, human; D011518:Proto-Oncogene Proteins; C529037:galloyl tyramine; C012526:quercitrin; D005707:Gallic Acid; D011794:Quercetin; D017346:Protein Serine-Threonine Kinases; D014439:Tyramine