1. Academic Validation
  2. Synthesis and apoptosis inducing ability of new anilino substituted pyrimidine sulfonamides as potential anticancer agents

Synthesis and apoptosis inducing ability of new anilino substituted pyrimidine sulfonamides as potential anticancer agents

  • Eur J Med Chem. 2011 Dec;46(12):5817-24. doi: 10.1016/j.ejmech.2011.09.039.
Ahmed Kamal 1 D Dastagiri M Janaki Ramaiah J Surendranadha Reddy E Vijaya Bharathi M Kashi Reddy M Victor Prem Sagar T Lakshminarayan Reddy S N C V L Pushpavalli Manika Pal-Bhadra
Affiliations

Affiliation

  • 1 Division of Organic Chemistry, Indian Institute of Chemical Technology, Tarnaka, Hyderabad 500 607, India. ahmedkamal@iict.res.in
Abstract

A series of anilino substituted pyrimidine sulfonamides were prepared and evaluated for their Anticancer activity. These sulfonamides showed promising activity with IC(50) values ranging from 5.6 to 12.3 μM. The detailed biological aspects of some of the promising compounds (3d, 3e and 3g) on the K562 cell line were studied. Interestingly, compounds induced G1 cell cycle arrest and down regulation of G1 phase cell cycle regulatory proteins such as cyclin D1, CDK4. These compounds also exhibited inhibition of NF-κB as well as its downstream target gene Akt1 and the phosphorylated form of Akt ser 474 proteins. One of the representative compound 3e could be considered as the potential lead for its development as a new Anticancer agent.

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