2. Academic Validation
  3. A novel achiral seco-cyclopropylpyrido[e]indolone (CPyI) analog of CC-1065 and the duocarmycins: synthesis, DNA interactions, in vivo anticancer and anti-parasitic evaluation

A novel achiral seco-cyclopropylpyrido[e]indolone (CPyI) analog of CC-1065 and the duocarmycins: synthesis, DNA interactions, in vivo anticancer and anti-parasitic evaluation

  • Bioorg Med Chem. 2010 Jul 15;18(14):5016-24. doi: 10.1016/j.bmc.2010.05.078.
Sameer Chavda 1,  Balaji Babu,  Stephanie K Yanow,  Armando Jardim,  Terry W Spithill,  Konstantinos Kiakos,  Jerome Kluza,  John A Hartley,  Moses Lee
Affiliations

Affiliation

  • 1 Division of Natural Sciences and Department of Chemistry, Hope College, 35 East 12th Street, Holland, MI 49423, USA.
PMID: 20579889 DOI: 10.1016/j.bmc.2010.05.078
Abstract

The synthesis of an achiral seco-hydroxy-aza-CBI-TMI analog (8) of the Duocarmycins is reported. Its specificity for the DNA minor groove of AT-rich sequences and covalent bonding to adenine-N3 was ascertained by a thermal cleavage assay. Compound 8 was found to be cytotoxic in the nanomolar range against murine and human Cancer cells. It was further demonstrated that compound 8 was active against murine melanoma (B16-F0) grown in C57BL/6 mice. Compound 8 was also shown to inhibit the growth of the protozoan parasites Leishmania donovani, Leishmania mexicana, Trypanosoma brucei, and Plasmodium falciparum in culture.

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