Synthesis and biological evaluation of conformationally flexible as well as restricted dimers of monastrol and related dihydropyrimidones

  • Eur J Med Chem. 2011 Aug;46(8):3274-81. doi: 10.1016/j.ejmech.2011.04.048.
Ahmed Kamal  1 ,  M Shaheer Malik ,  Shaik Bajee ,  Shaik Azeeza ,  Shaikh Faazil ,  Sistla Ramakrishna ,  V G M Naidu ,  M V P S Vishnuwardhan
Affiliations
  • 1. Division of Organic Chemistry, Indian Institute of Chemical Technology, Hyderabad 500 607, India. [email protected]
PMID: 21620531 DOI: 10.1016/j.ejmech.2011.04.048
Abstract

A series of conformationally flexible and restricted dimers of monastrol as well as related dihydropyrimidones have been synthesized by employing one-pot Biginelli multicomponent reaction. These dimers have been evaluated for cytotoxic potency against selected human Cancer cell lines and some of the compounds have exhibited more cytotoxic potency than the parent monastrol. Further, the DNA binding ability by thermal denaturation studies and antimicrobial activities of these compounds are also discussed.