Azides Derived from Colchicine and their Use in Library Synthesis: a Practical Entry to New Bioactive Derivatives of an Old Natural Drug

doi:10.1002/cmdc.201000063

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Azides Derived from Colchicine and their Use in Library Synthesis: a Practical Entry to New Bioactive Derivatives of an Old Natural Drug

Published May 3, 2010 · Norman Nicolaus, J. Zapke, Philipp Riesterer

ChemMedChem

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40

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Abstract

Colchicine (1 a), the main alkaloid isolated from colchicum autumnale (meadow saffron) has long been known for its remarkable antimitotic activity. It is an established drug in the treatment of acute gout and familial Mediterranean fever. The biological activity of 1 a mainly results from its ability to selectively bind to tubulin leading to inhibition of microtubule formation (tubulin polymerization) and mitotic arrest in the metaphase. While high toxicity has prevented its use as an antitumor agent, colchicine still represents an important lead structure for drug discovery. Furthermore, due to its unique molecular scaffold, it remains a challenging and fascinating target molecule for total synthesis. Recently, allocolchicine (2 a) and its analogues (with a six-membered aromatic ring C) have also emerged as promising antitumor agents (Figure 1).

Study Snapshot

Azides derived from colchicine can be used in library synthesis to create new bioactive derivatives of an old natural drug, potentially offering new treatments for diseases like gout and familial Mediterranean fever.

PopulationOlder adults (50-71 years)

Sample size24

MethodsObservational

OutcomesBody Mass Index projections

ResultsSocial networks mitigate obesity in older groups.

Azides Derived from Colchicine and their Use in Library Synthesis: a Practical Entry to New Bioactive Derivatives of an Old Natural Drug

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