Antitumor Activity of 3-Indolylmethanamines 31B and PS121912.
Year: 2015
Type: article
Abstract: 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. (13)C-Nuclear 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.
Source: PubMed
Language: English
Subfield: Organic Chemistry
Field: Chemistry
Domain: Physical Sciences
Open Access status: green
Awards: Small molecule inhibitors of the vitamin D receptor-coactivator interaction, Vitamin D Receptor Coactivators in Keratinocytes, Synthesis of Alpha2/Alpha3 GABA Agonists to Treat Neuropathic Pain, Development of new drugs for asthma by targeting GABA(A) receptors in the lung, Design of New Therapeutic Agents to Treat Schizophrenia
OpenAlex ID: W1888197883