Antitumor activity of 3-indolylmethanamines 31b and ps121912

Margaret L. Guthrie, Preetpal S. Sidhu, Emily K. Hill, Timothy C. Horan, Premchendar Nandhikonda, Kelly A. Teske, Nina Y. Yuan, Marina Sidorko, Revathi Rodali, James M. Cook, Lanlan Han, Nicholas R. Silvaggi, Daniel D. Bikle, Richard G. Moore, Rakesh K. Singh, Leggy A. Arnold*

*Corresponding author for this work

Research output: Contribution to journalArticlepeer-review

7 Citations (Scopus)


Aim: To investigate the in vivo effects of 3-indolylmethanamines 31B and PS121912 in treating ovarian cancer and leukemia, respectively. Materials and Methods: Terminal deoxynucleotidyl transferase dUTP nick-end labeling (TUNEL) and western blotting were applied to demonstrate the induction of apoptosis. Xenografted mice were investigated to show the antitumor effects of 3-indolylmethanamines. 13CNuclear magnetic resource (NMR) and western blotting were used to demonstrate inhibition of glucose metabolism. Results: 31B inhibited ovarian cancer cell proliferation and activated caspase-3, cleaved poly (ADP-ribose) polymerase 1 (PARP1), and phosphorylated mitogen-activated protein kinases (MAPK), JUN N-terminal kinase/stress-activated protein kinase (JNK/SAPK) and p38. 31B reduced ovarian cancer xenograft tumor growth and PS121912 inhibited the growth of HL-60-derived xenografts without any sign of toxicity. Compound 31B inhibited de novo glycolysis and lipogenesis mediated by the reduction of fatty acid synthase and lactate dehydrogenase-A expression. Conclusion: 3-Indolylmethanamines represent a new class of antitumor agents. We have shown for the first time the in vivo anticancer effects of 3-indolylmethanamines 31B and PS121912.

Original languageEnglish
Pages (from-to)6001-6007
Number of pages7
JournalAnticancer Research
Issue number11
Publication statusPublished - Nov 2015
Externally publishedYes


  • 3-Indolylmethanamine
  • Leukemia
  • Ovarian cancer


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