2. Academic Validation
  3. Synthesis and biological evaluation of 2,4-diaminoquinazoline derivatives as novel heat shock protein 90 inhibitors

Synthesis and biological evaluation of 2,4-diaminoquinazoline derivatives as novel heat shock protein 90 inhibitors

  • Bioorg Med Chem Lett. 2011 Mar 15;21(6):1593-7. doi: 10.1016/j.bmcl.2011.01.117.
Dhanaji Achyutrao Thorat 1,  Munikumar Reddy Doddareddy,  Seon Hee Seo,  Tae-Joon Hong,  Yong Seo Cho,  Ji-Sook Hahn,  Ae Nim Pae
Affiliations

Affiliation

  • 1 Neuro-Medicine Center, Korea Institute of Science and Technology, Seoul, Republic of Korea.
PMID: 21353544 DOI: 10.1016/j.bmcl.2011.01.117
Abstract

Novel 2,4-diaminoquinazoline derivatives originating from a virtual screening approach were designed, synthesized and their biological activities as heat shock protein 90 (HSP90) inhibitors were evaluated. The prepared compounds exhibited significant anti-proliferative activities against DU-145, HT-29, HCT-116, A375P and MCF-7 Cancer cell lines. The selected compounds were tested against Her2, a client protein of HSP90, and showed significant reduction in Her2 protein expression. Compound 6b was found the most potent, reduced Her2 protein expression levels and induced HSP70 protein expression levels significantly.

Figures