1. Academic Validation
  2. Synthesis of novel pyrazolo[3,4-d]pyrimidine derivatives as potential anti-breast cancer agents

Synthesis of novel pyrazolo[3,4-d]pyrimidine derivatives as potential anti-breast cancer agents

  • Eur J Med Chem. 2012 Nov:57:323-8. doi: 10.1016/j.ejmech.2012.09.031.
Mohammed K Abd El Hamid 1 Marko D Mihovilovic Hala B El-Nassan
Affiliations

Affiliation

  • 1 Pharmaceutical Organic Chemistry Department, Faculty of Pharmacy, Cairo University, 33 Kasr El-Aini Street, Cairo 11562, Egypt.
Abstract

A series of new 1-aryl-4-benzylidenehydrazinyl-3-methylsulphanyl-pyrazolo[3,4-d]pyrimidines 6a-p was synthesized. The cytotoxic activity of the newly synthesized compounds against human breast Cancer cell line, MCF7 was investigated. Most of the test compounds showed potent antitumor activity comparable to that of doxorubicin. The 1-phenyl series (6a-i) exhibited better antitumor activity than 1-(4-methoxyphenyl) series (6j-p). 4-[2-(4-Fluorobenzylidene)hydrazinyl]-3-(methylsulphanyl)-1-phenyl-1H-pyrazolo[3,4-d]pyrimidine (6d) was the most active compound in this study with IC(50) equal to 7.5 nM.

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