2 results match your criteria brostallicin presently

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Cytotoxic alpha-halogenoacrylic derivatives of distamycin A and congeners.

J Med Chem 2004 May;47(10):2611-23

Pharmacia Italia S.p.A., Discovery Research Oncology, Viale Pasteur 10, 20014 Nerviano, Milan, Italy.

The mechanism of action of many antitumor agents involves DNA damage, either by direct binding of the drug to DNA or to DNA-binding proteins. However, most of the DNA-interacting agents have only a limited degree of sequence specificity, which implies that they may hit all the cellular genes. DNA minor groove binders, among which the derivatives of distamycin A play an important role, could provide significant improvement in cancer management, increasing gene specificity, due to high selectivity of interaction with thymine-adenine (TA) rich sequences. Read More

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Brostallicin, a novel anticancer agent whose activity is enhanced upon binding to glutathione.

Cancer Res 2002 Apr;62(8):2332-6

Laboratory of Molecular Pharmacology, Department of Oncology, Mario Negri Institute of Pharmacological Research, via Eritrea 62, 20157 Milan, Italy.

Brostallicin (PNU-166196) is a synthetic alpha-bromoacrylic, second-generation DNA minor groove binder structurally related to distamycin A, presently in Phase II trials in Europe and the United States. The compound shows broad antitumor activity in preclinical models and dramatically reduced in vitro myelotoxicity in human hematopoietic progenitor cells compared with that of other minor groove binders. Brostallicin showed a 3-fold higher activity in melphalan-resistant L1210 murine leukemia cells than in the parental line (IC(50) = 0. Read More

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