Calicheamicins bind with DNA in the minor groove, wherein they then undergo a reaction analogous to the Bergman cyclization to generate a diradical species. This diradical, 1,4-didehydrobenzene, then abstracts hydrogen atoms from the deoxyribose (sugar) backbone of DNA, which ultimately leads to strand scission.
What is the mode of action of the anticancer agent calicheamicin?
Platform Technologies in Drug Discovery and Validation Calicheamicins are a group of potent antitumor antibiotics that cleave DNA in a site-specific, double-stranded manner. This antibiotic was originally isolated from the actinomycete Micromonospora echinospora found in a soil sample from Texas.
Is calicheamicin an alkyne?
[*] Calicheamicin is part of a class of toxic chemicals called Alkynes, which are generally not very useful as pharmaceuticals.23 Mar 2019