Synthesis and cytotoxicity evaluation of novel 1,4-disubstituted 1,2,3-triazoles via CuI catalysed 1,3-dipolar cycloaddition.
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.
Vantikommu
Jyothi
J
Department of Chemistry, Nizam College, Osmania University, Hyderabad 500006, Andhra Pradesh, India.
Palle
Sadanandam
S
Reddy
Punganuru Surendra
PS
Ramanatham
Vinodkumar
V
Khagga
Mukkanti
M
Pallapothula
Venkateswara Rao
VR
D002384:Catalysis; D045744:Cell Line, Tumor; D003300:Copper / Q000737:chemistry*; D003500:Cyclization; D004353:Drug Evaluation, Preclinical; D006801:Humans; D014230:Triazoles / Q000138:chemical synthesis* / Q000494:pharmacology*
D014230:Triazoles; D003300:Copper