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N-(Hydroxymethyl) melamines

H M Coley1

  • 1CRC Center for Cancer Therapeutics, Institute of Cancer Research, Belmont, Sutton, Surrey, UK.

General Pharmacology
|February 1, 1997
PubMed
Summary
This summary is machine-generated.

N-(hydroxymethyl) melamines, like CB7646, show promise as antitumor agents. These compounds do not require bioactivation and are effective against drug-resistant cancers, with CB7646 advancing to clinical trials.

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Area of Science:

  • Oncology
  • Medicinal Chemistry

Background:

  • Hexamethylmelamine (HMM) analogs, N-(hydroxymethyl) melamines, exhibit antitumor activity without bioactivation.
  • Trimelamol (TM) is a water-soluble analog developed for intravenous administration, showing promise in ovarian cancer but facing formulation challenges.

Purpose of the Study:

  • To develop stable N-(hydroxymethyl) melamine analogs overcoming TM's formulation issues.
  • To evaluate the in vitro and in vivo antitumor efficacy of these stable analogs.

Main Methods:

  • Synthesis of stable N-(hydroxymethyl) melamine analogs.
  • In vitro cytotoxicity assays in tumor cell lines.
  • In vivo studies using human ovarian and breast cancer xenograft models, including carboplatin-resistant models.

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Main Results:

  • Stable analogs demonstrated good in vitro cytotoxicity.
  • CB7646 exhibited in vivo antitumor activity comparable to TM.
  • Both TM and CB7646 were curative in xenograft models, including those resistant to carboplatin.
  • CB7646 shows superior stability and favorable formulation characteristics.

Conclusions:

  • CB7646 is a promising stable analog of TM with significant in vivo antitumor activity.
  • N-(hydroxymethyl) melamines can overcome drug resistance, offering potential for treating refractory tumors.
  • CB7646 is advancing to Phase I clinical trials due to its favorable properties.