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


Authors: Lee, C. H.; Chou, T. C.; Su, T. L.; Yu, J.; Shao, L. E.; Yu, A. L.
Article Title: BO-0742, a derivative of AHMA and N-mustard, has selective toxicity to drug sensitive and drug resistant leukemia cells and solid tumors
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. © 2008 Elsevier Ireland Ltd. All rights reserved.
Keywords: controlled study; human tissue; leukemia; unclassified drug; human cell; area under the curve; drug efficacy; liver cell carcinoma; nonhuman; antineoplastic agents; paclitaxel; antineoplastic agent; neoplasms; mouse; animals; mice; animal tissue; mus; ovary cancer; breast cancer; etoposide; animal experiment; antineoplastic activity; cancer cell culture; continuous infusion; cytotoxicity; in vitro study; drug resistance, neoplasm; xenograft model antitumor assays; cell line, tumor; cancer inhibition; human cell culture; drug distribution; neuroblastoma; hematopoietic stem cells; drug clearance; maximum plasma concentration; hematopoietic stem cell; 9 anilinoacridine derivative; aniline compounds; drug half life; drug sensitivity; acridines; bo-0742; n-mustard; pharmacokinetics; pre-clinical study; solid tumors; bo 0742; chlormethine derivative; mean residence time; plasma concentration-time curve; multidrug resistance-associated proteins; nitrogen mustard compounds; p-glycoprotein
Journal Title: Cancer Letters
Volume: 276
Issue: 2
ISSN: 0304-3835
Publisher: Elsevier Ireland Ltd.  
Date Published: 2009-04-18
Start Page: 204
End Page: 211
Language: English
DOI: 10.1016/j.canlet.2008.11.006
PUBMED: 19108949
PROVIDER: scopus
DOI/URL:
Notes: --- - "Cited By (since 1996): 1" - "Export Date: 30 November 2010" - "CODEN: CALED" - "Source: Scopus"
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  1. Ting-Chao Chou
    319 Chou