Concepedia

Calicheamicin θ: A Rationally Designed Molecule with Extremely Potent and Selective DNA Cleaving Properties and Apoptosis Inducing Activity

K. C. Nicolaou, Tao Li, Masahisa Nakada, Conrad W. Hummel, Andrew Hiatt, Wolfgang Wrasidlo

Angewandte Chemie International Edition in English · 1994 · 55 citations · 21 references

DOI

Concepts

Abstract

The attack of a thiolate ion on the trisulfide unit of natural calicheamicin γ (1) activates it to form a diradical, which then attacks DNA. Thioacetate 2 is even more readily activated—under mildly basic conditions caused by OH- ions—and likewise exhibits extremely interesting biological properties.

References

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Calicheamicin γ <sub>1</sub> <sup>I</sup> : an Antitumor Antibiotic That Cleaves Double-Stranded DNA Site Specifically

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