An efficient green diversity oriented synthesis of pyrimidinone and indole appended macrocyclic peptidomimetics

Abstract A concise protocol for the synthesis of pyrimidinone/indole functionalized hybrid peptide macrocycles with varying ring size is described. The precursors of the macrocycles were obtained from the post reaction modification of multicomponent reaction products and were cyclized via copper (I) catalyzed [3 + 2] azide-alkyne cycloaddition. The macrocycles showed excellent inhibitory property towards CDK2 protein which is responsible for a variety of cancers and were also showed excellent cytotoxicity against human breast cancer cell line MCF-7.

• Publication year

  2019

• Venue

  Tetrahedron Letters

• Publication date

  2019-01-01

• Fields of study

  Chemistry

• Identifiers
  DOI 10.1016/J.TETLET.2018.12.012
• External record

  Open on Semantic Scholar

• Source metadata

  Semantic Scholar

• No claims are published for this paper.

• No concepts are published for this paper.

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