InCl3-catalysed synthesis of 2-aryl quinazolin-4(3H)-ones and 5-aryl pyrazolo[4,3-d]pyrimidin-7(6H)-ones and their evaluation as potential anticancer agents

  • Bioorg Med Chem Lett. 2012 Aug 1;22(15):5063-6. doi: 10.1016/j.bmcl.2012.06.003.
Naveen Mulakayala  1 ,  Bhaskar Kandagatla ,  Ismail ,  Rajesh Kumar Rapolu ,  Pallavi Rao ,  Chaitanya Mulakayala ,  Chitta Suresh Kumar ,  Javed Iqbal ,  Srinivas Oruganti
Affiliations
  • 1. Cosmic Discoveries, Institute of Life Sciences, University of Hyderabad Campus, Gachibowli, Hyderabad, India. [email protected]
PMID: 22749421 DOI: 10.1016/j.bmcl.2012.06.003
Abstract

A convenient and practical methodology for the synthesis of 2-aryl quinazolin-4(3H)-ones by the condensation of o-aminobenzamides with aromatic aldehydes under mild conditions using catalytic InCl(3) with good yields and high selectivities. This method has been extended for the synthesis of 5-aryl pyrazolo[4,3-d]pyrimidin-7(6H)-ones which have potential applications in medicinal chemistry. Many of these compounds were evaluated for their anti-proliferative properties in vitro against four Cancer cell lines and several compounds were found to be active. Further in vitro studies indicated that inhibition of sirtuins could be the possible mechanism of action of these molecules.