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Enediynes
Enediynes are organic compounds containing two triple bonds and one double bond. Enediynes are most notable for their limited use as antitumor antibiotics (known as enediyne Chemotherapy, anticancer antibiotics). They are efficient at inducing apoptosis in Cell biology, cells, but cannot differentiate Cancer cell, cancerous cells from healthy cells. Consequently, research is being conducted to increase the specificity of enediyne toxicity. Structure and reactivity A nine- or ten-membered ring containing a double bond between two triple bonds is termed the warhead of the enediyne. In this state, the warhead is inactive. Enediynes are triggered into a chemically active state via Bergman cyclization, Bergman or Myers-Saito cyclization. The triggering mechanism can be attributed to an intramolecular nucleophilic attack initiated by one of the variable regions of the molecule. Triggering can also occur via attack by an external nucleophile. Bergman cyclization restructures the ened ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
C-1027
C-1027 or lidamycin is an antitumor antibiotic consisting of a complex of an enediyne chromophore and an apoenzyme, apoprotein. It shows antibiotic activity against most Gram-positive bacteria. It is one of the most potent cytotoxic molecules known, due to its induction of a higher ratio of DNA double-strand breaks than single-strand breaks. C-1027's chromophore contains a nine-membered enediyne that is responsible for most of the molecule's biological activity. Unlike other enediynes, this molecule contains no triggering mechanism. It is already primed to undergo the cycloaromatization reaction without external activation to produce the toxic 1,4-benzenoid diradical species. C-1027 can induce oxygen-independent interstrand DNA crosslinks in addition to the oxygen-dependent single- and double-stranded DNA breaks typically generated by other enediynes. This unique oxygen-independent mechanism suggests that C-1027 may be effective against Tumor hypoxia, hypoxic tumor cells. C-102 ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
