4.7 Article

Sulfur and selenium derivatives of quinazoline and pyrido[2,3-d]pyrimidine: Synthesis and study of their potential cytotoxic activity in vitro

Journal

EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
Volume 47, Issue -, Pages 283-298

Publisher

ELSEVIER FRANCE-EDITIONS SCIENTIFIQUES MEDICALES ELSEVIER
DOI: 10.1016/j.ejmech.2011.10.056

Keywords

Cytotoxics; Antiproliferatives; Quinazolines; Pyridopyrimidines

Funding

  1. Ministerio de Educacion y Ciencia, Spain [SAF 2009-07744]
  2. CAN Foundation
  3. Department of Education of the Navarra Government

Ask authors/readers for more resources

The synthesis, cytotoxic activities and selectivities of 35 derivatives related to quinazoline and pyrido [2,3-d]pyrimidine are described. The synthesized compounds were screened in vitro against four tumoral cell lines leukemia (CCRF-CEM), colon (HT-29), lung (HTB-54) and breast (MCF-7) - and two cell lines derived from non-malignant cell lines, one mammary (18485) and one from bronchial epithelium (BEAS-2B). MCF-7 and HTB-54 were the most sensitive cell lines with GI(50) values below 10 mu M for eleven and ten compounds. respectively. Two compounds (2o and 3a) were identified that evoked a marked cytotoxic effect in all cell lines tested and one compound, 7h, was potent and selective against MCF-7. A preliminary study into the mechanism of the potent derivatives 2o, 3a and 7h indicated that the cytotoxic activities of these compounds might be mediated by inducing cell death without affecting cell cycle phases. (C) 2011 Elsevier Masson SAS. All rights reserved.

Authors

I am an author on this paper
Click your name to claim this paper and add it to your profile.

Reviews

Primary Rating

4.7
Not enough ratings

Secondary Ratings

Novelty
-
Significance
-
Scientific rigor
-
Rate this paper

Recommended

No Data Available
No Data Available