Synthesis and Anti-Proliferative Effects of Mono- and Bis-Purinomimetics Targeting Kinases

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ID: 50540
2017
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Abstract
A series of mono-pyrrolo[2,3-d]pyrimidines 4a–4k, unsymmetrical bis-purine isosteres 5a–5e and symmetrical bis-pyrrolo[2,3-d]pyrimidines 6a and 6b connected via di(1,2,3-triazolyl)phenyl linker were synthesized by click chemistry. Whereas mono- 4g and bis-pseudopurine 5e showed selective inhibitory activities on cervical carcinoma (HeLa) cells, bis-pyrrolo[2,3-d]pyrimidine 6b exhibited potent and selective anti-proliferative effect in the nanomolar range on pancreatic carcinoma (CFPAC-1) cells. Among these, compound 6b induced a significant reduction in the expression level of CDK9 (cyclin-dependent kinase 9)/cyclin T1 in CFPAC-1 cells concomitant with attenuation of proliferative signaling mediated by c-Raf (rapidly accelerated fibrosarcoma) and p38 MAP (mitogen-activated protein) kinases. Our findings encourage further development of novel structurally related analog of 6b to obtain more selective anticancer agent for treating pancreatic cancer.
Reference Key
bistrovic2017synthesisinternational Use this key to autocite in the manuscript while using SciMatic Manuscript Manager or Thesis Manager
Authors Bistrović, Andrea;Harej, Anja;Grbčić, Petra;Sedić, Mirela;Pavelić, Sandra Kraljević;Cetina, Mario;Raić-Malić, Silvana;
Journal International journal of molecular sciences
Year 2017
DOI
DOI not found
URL
https://www.mdpi.com/1422-0067/18/11/2292
Keywords
chemistry Organic Chemistry Pharmacy and materia medica Biology (General) Science (General)

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