Design, synthesis and evaluation of cyclic peptide analogues of Carnosine as anticancer agents

چکیده مقاله

Carnosine (β-alanyl-L-histidine) is a naturally occurring dipeptide in the muscle and nervous tissues. In the present perspective, a possible use of Carnosine as an anti-neoplastic therapeutic, especially for the treatment of other cell lines and its toxicity against Hep G2, HT-29 and A549 using 3-(4,5-Dimethylthiazol-2-yl)-2,5-diphenyltetrazoliumbromide (MTT assay) are discussed. In this work, two analogues of cyclic penta peptide Carnosine have shown good toxicity against cell lines of HepG2 (human liver cancer cell line), HT-29 (human colorectal adenocarcinoma cell line) and A549 (adenocarcinomic human alveolar basal epithelial cells) using MTT assay. 2-chlorotritylchloride resin (2-CTC) was used as solid support and a suitable resin. Macrocyclization of linear (N-Trt) Carnosine analogues were done by coupling reagent and then the final deprotection were done on cyclic (N-Trt) Carnosine analogues by treatment of trifluoroacetic acid 95%. The synthesized cyclic Carnosine analogues were characterized by using different methods such as, LC-MS and FT-IR.