An efficient green diversity oriented synthesis of pyrimidinone and indole appended macrocyclic peptidomimetics
2019
Pathoor, Rajeena | Puthiyedath, Thasnim | Bahulayan, D.
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.
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