Anti-proliferative evaluation of monoterpene derivatives against leukemia

Eur J Med Chem. 2016 May 4:113:75-80. doi: 10.1016/j.ejmech.2016.02.034. Epub 2016 Feb 16.

Abstract

The cure rate of pediatric acute lymphoblastic leukemia (ALL) has significantly improved in the past thirty years, however not all patient cohorts respond well to current chemotherapy regimens. Among the high risk patient cohort is infants with MLL-rearranged (MLL-r) B-ALL, which remains dismal with an overall survival rate <35%. Our program is interested in identifying new molecular scaffolds to better understand the underlying mechanisms and ultimately provide new targeted treatments. Based on a phenotypic screen, phenolic natural products were identified as promising scaffolds for further chemical evaluation. Herein we disclose the effects of a potent anti-proliferative compound 31 against human ALL leukemia cellular models.

Keywords: Apoptosis; Bakuchiol; Leukemia; Monoterpene; Natural products.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Antineoplastic Agents, Phytogenic / chemical synthesis
  • Antineoplastic Agents, Phytogenic / chemistry
  • Antineoplastic Agents, Phytogenic / pharmacology*
  • Cell Proliferation / drug effects
  • Dose-Response Relationship, Drug
  • Drug Screening Assays, Antitumor
  • Humans
  • Molecular Structure
  • Monoterpenes / chemical synthesis
  • Monoterpenes / chemistry
  • Monoterpenes / pharmacology*
  • Precursor Cell Lymphoblastic Leukemia-Lymphoma / drug therapy*
  • Precursor Cell Lymphoblastic Leukemia-Lymphoma / pathology
  • Structure-Activity Relationship

Substances

  • Antineoplastic Agents, Phytogenic
  • Monoterpenes