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  • Synthesis and cytotoxicity evaluation of novel 1,4-disubstituted 1,2,3-triazoles via CuI catalysed 1,3-dipolar cycloaddition.

Synthesis and cytotoxicity evaluation of novel 1,4-disubstituted 1,2,3-triazoles via CuI catalysed 1,3-dipolar cycloaddition.

European journal of medicinal chemistry (2010-09-14)
Jyothi Vantikommu, Sadanandam Palle, Punganuru Surendra Reddy, Vinodkumar Ramanatham, Mukkanti Khagga, Venkateswara Rao Pallapothula
ABSTRACT

A facile and highly efficient method for the regioselective synthesis of 1,4-disubstituted 1,2,3-triazoles (β-keto 1,2,3-triazoles) in good to excellent yields from in-situ generated β-ketoazides and terminal alkynes through Cu(I) catalyzed 1,3 dipolar cycloaddition is described. This reaction proceeds smoothly either in water or in a 1:1 mixture of water and acetone at room temperature without use of any additive. The synthesized compounds were screened for their cytotoxicity in A549 (Lung Cancer), HT-29 (Colon Cancer), He La (Cervical Cancer) using MTT assay that exhibited significant cytotoxicity at modest doses.

MATERIALS
Product Number
Brand
Product Description

Sigma-Aldrich
Podophyllotoxin
Sigma-Aldrich
Colchicine, ≥95% (HPLC), powder
Sigma-Aldrich
Colchicine, BioReagent, suitable for plant cell culture, ≥95% (HPLC)