BO-0742, a derivative of AHMA and N-mustard, has selective toxicity to drug sensitive and drug resistant leukemia cells and solid tumors

  • Cancer Lett. 2009 Apr 18;276(2):204-11. doi: 10.1016/j.canlet.2008.11.006.
Chien-Hsin Lee  1 ,  Ting-Chao Chou ,  Tsann-Long Su ,  John Yu ,  Li-En Shao ,  Alice L Yu
Affiliations
  • 1. Cellular and Molecular Medicine, Genomics Research Center, 128 Academia Sinica, Section 2, Taipei, Taiwan.
PMID: 19108949 DOI: 10.1016/j.canlet.2008.11.006
Abstract

This is a preclinical study of BO-0742, a derivative of 3-(9-acridinylamino)-5-hydroxymethyl-aniline (AHMA) and N-mustard, as an anti-cancer agent. MTS assays revealed a broad spectrum of anti-cancer activities in vitro, with the greatest cytotoxicity against leukemia and neuroblastoma including those with drug resistant characteristics, and a good therapeutic index with leukemia being 10-40 times more sensitive to BO-0742 than hematopoietic progenitors. Administration of BO-0742 at an optimal dose schedule based on its pharmacokinetics significantly suppressed the growth of xenografts of human breast and ovarian cancers in mice. Thus, BO-0742 is a potent anti-cancer agent worthy of further clinical development.

Products