2. Academic Validation
  3. Synthesis and preliminary cytotoxicity of nitrogen mustard derivatives of distamycin A

Synthesis and preliminary cytotoxicity of nitrogen mustard derivatives of distamycin A

  • Bioorg Med Chem Lett. 2003 Feb 10;13(3):459-61. doi: 10.1016/s0960-894x(02)00986-1.
Yuqiang Wang 1,  Susan C Wright,  James W Larrick
Affiliations

Affiliation

  • 1 Panorama Research, Inc., 2462 Wyandotte Street, Mountain View, CA 94043, USA. [email protected]
PMID: 12565950 DOI: 10.1016/s0960-894x(02)00986-1
Abstract

Distamycin and nitrogen mustard conjugates, in which the nitrogen mustard unit was coupled to the C-terminus of the pyrrole, were synthesized. The switching of the nitrogen mustard unit from the N-terminus to the C-terminus did not compromise the compound's cytotoxicity. Compound 3, bearing three pyrrole units, was highly toxic to human K562 leukemia cells in vitro with an IC(50) value of 0.03 microM. Addition of a trans double bond to the molecule had little effects on cytotoxicity.

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