Click inspired synthesis of piperazine-triazolyl sugar-conjugates as potent anti-Hela activity

Carbohydr Res. 2023 Jul:529:108846. doi: 10.1016/j.carres.2023.108846. Epub 2023 May 22.

Abstract

To imbibe the aim of synthesizing water-soluble and biocompatible motif, a click-inspired piperazine glycoconjugate has been devised up. In this report, we present a focused approach to design and synthesis of versatile sugar-appended triazoles through 'Click Chemistry' along with their pharmacological studies on cyclin-dependent kinases (CDKs) and cell cytotoxicity on cancer cells using in silico and in vitro approaches, respectively. The study has inclusively recognized the galactose- and mannose-derived piperazine conjugates as the promising motifs. The findings suggested that the galactosyl bis-triazolyl piperazine analogue 10b is the most CDK interactive derivative and also possess significant anticancer activity.

Keywords: Anticancer activity; Click chemistry; Docking study; Glycoconjugate; Piperazine.

MeSH terms

  • Antineoplastic Agents* / pharmacology
  • Click Chemistry
  • Galactose
  • Glycoconjugates
  • Piperazine / pharmacology
  • Sugars*

Substances

  • Piperazine
  • Sugars
  • Glycoconjugates
  • Galactose
  • Antineoplastic Agents