2. Academic Validation
  3. Novel pyrazolo[3,4-d]pyrimidines as dual Src-Abl inhibitors active against mutant form of Abl and the leukemia K-562 cell line

Novel pyrazolo[3,4-d]pyrimidines as dual Src-Abl inhibitors active against mutant form of Abl and the leukemia K-562 cell line

  • Eur J Med Chem. 2016 Nov 10:123:1-13. doi: 10.1016/j.ejmech.2016.07.034.
Samir M El-Moghazy 1,  Riham F George 2,  Essam Eldin A Osman 1,  Ahmed A Elbatrawy 3,  Miroslava Kissova 4,  Ambra Colombo 4,  Emmanuele Crespan 4,  Giovanni Maga 4
Affiliations

Affiliations

  • 1 Pharmaceutical Chemistry Department, Faculty of Pharmacy, Cairo University, El-kasr Elaini Street, Cairo 11562, Egypt.
  • 2 Pharmaceutical Chemistry Department, Faculty of Pharmacy, Cairo University, El-kasr Elaini Street, Cairo 11562, Egypt. Electronic address: rihamfgeorge@yahoo.com.
  • 3 Pharmaceutical Chemistry Department, Faculty of Pharmacy, Nahda University, Beni Suef 62511, Egypt.
  • 4 Istituto di Genetica Molecolare, IGM-CNR, Via Abbiategrasso 207, I-27100 Pavia, Italy.
PMID: 27474918 DOI: 10.1016/j.ejmech.2016.07.034
Abstract

Some novel 6-substituted pyrazolo[3,4-d]pyrimidines 4, 5, 6a-d, 7a-c, 8 and pyrazolo[4,3-e][1,2,4]triazolo[4,3-a]pyrimidines 9a-c, 10a-c, 11, 12a,b, 13a-c and 14 were synthesized and characterized by spectral and elemental analyses. They were screened for their biological activity in vitro against Abl and Src kinases. Compounds 7a and 7b revealed the highest activity against both wild and mutant Abl kinases as well as the Src kinase and the leukemia K-562 cell line. They can be considered as new hits for further structural optimization to obtain better activity.

Keywords

Abl inhibition; K-562 cell line; Molecular modeling; Pyrazolo[3,4-d]pyrimidines; Src inhibition.

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