1-[2-(2-Methoxyphenylamino)ethylamino]-3-(naphthalene-1- yloxy)propan-2-ol may be a promising anticancer drug

Molecules. 2014 Dec 19;19(12):21462-72. doi: 10.3390/molecules191221462.

Abstract

We have originally synthesized the naftopidil analogue 1-[2-(2-methoxyphenylamino)ethylamino]-3-(naphthalene-1-yloxy)propan-2-ol (HUHS 1015) as a new anticancer drug. HUHS1015 induces cell death in a wide variety of human cancer cell lines originated from malignant pleural mesothelioma, lung cancer, hepatoma, gastric cancer, colorectal cancer, bladder cancer, prostate cancer, and renal cancer. HUHS1015-induced cell death includes necrosis (necroptosis) and apoptosis, and the underlying mechanism differs depending upon cancer cell types. HUHS1015 effectively suppresses tumor growth in mice inoculated with NCI-H2052, MKN45, or CW2 cells, with a potential similar to or higher than that of currently used anticancer drugs. Here we show how HUHS1015 might offer brilliant hope for cancer therapy.

MeSH terms

  • Aniline Compounds / chemical synthesis
  • Aniline Compounds / pharmacology*
  • Aniline Compounds / therapeutic use
  • Animals
  • Antineoplastic Agents / chemical synthesis
  • Antineoplastic Agents / pharmacology*
  • Antineoplastic Agents / therapeutic use
  • Apoptosis / drug effects
  • Apoptosis Regulatory Proteins / metabolism
  • Cell Line, Tumor
  • Humans
  • Mitochondrial Proteins / metabolism
  • Necrosis
  • Propanolamines / chemical synthesis
  • Propanolamines / pharmacology*
  • Propanolamines / therapeutic use
  • Xenograft Model Antitumor Assays

Substances

  • 1-(2-(2-methoxyphenylamino)ethylamino)-3-(naphthalene-1-yloxy)propan-2-ol
  • ferroptosis suppressor protein 1, human
  • Aniline Compounds
  • Antineoplastic Agents
  • Apoptosis Regulatory Proteins
  • Mitochondrial Proteins
  • Propanolamines