Synthesis, antileukemic and antiplatelet activities of 2,3-diaryl-6,7-dihydro-5H-1,4-diazepines

R Ramajayam; Rajani Giridhar; M R Yadav; R Balaraman; Hakim Djaballah; David Shum; Constantin Radu

doi:10.1016/j.ejmech.2007.11.023

Synthesis, antileukemic and antiplatelet activities of 2,3-diaryl-6,7-dihydro-5H-1,4-diazepines

Eur J Med Chem. 2008 Sep;43(9):2004-10. doi: 10.1016/j.ejmech.2007.11.023. Epub 2007 Dec 7.

Authors

R Ramajayam¹, Rajani Giridhar, M R Yadav, R Balaraman, Hakim Djaballah, David Shum, Constantin Radu

Affiliation

¹ Pharmacy Department, Faculty of Technology and Engineering, The M.S University of Baroda, Kalabhavan, Vadodara 390 001, India.

PMID: 18191304
DOI: 10.1016/j.ejmech.2007.11.023

Abstract

The synthesis, antileukemic and antiplatelet activity evaluation of 2,3-diaryl-6,7-dihydro-5H-1,4-diazepines are described. In general, it was found that compound 17o showed moderate antileukemic activity against MOLT3 human leukemic cancer cell lines. An arachidonic acid induced platelet aggregation effect on washed rat platelets was studied. Compound 17i was found to be the most potent. The antiplatelet properties may be mediated by interference with the arachidonic acid pathway.

Publication types

Research Support, Non-U.S. Gov't

MeSH terms

Animals
Antineoplastic Agents / chemical synthesis*
Antineoplastic Agents / chemistry
Antineoplastic Agents / pharmacology*
Azepines / chemical synthesis*
Azepines / chemistry
Azepines / pharmacology*
Cell Line, Tumor
Cell Proliferation / drug effects
Female
Humans
Inhibitory Concentration 50
Platelet Aggregation / drug effects
Platelet Aggregation Inhibitors / chemical synthesis*
Platelet Aggregation Inhibitors / chemistry
Platelet Aggregation Inhibitors / pharmacology*
Rats

Substances

Antineoplastic Agents
Azepines
Platelet Aggregation Inhibitors