2. Academic Validation
  3. Synthesis and bioevaluation of new vascular-targeting and anti-angiogenic thieno[2,3-d]pyrimidin-4(3H)-ones

Synthesis and bioevaluation of new vascular-targeting and anti-angiogenic thieno[2,3-d]pyrimidin-4(3H)-ones

  • Eur J Med Chem. 2020 Mar 1:189:112060. doi: 10.1016/j.ejmech.2020.112060.
Madeleine Gold 1,  Leonhard Köhler 1,  Clarissa Lanzloth 1,  Ion Andronache 2,  Shrikant Anant 3,  Prasad Dandawate 3,  Bernhard Biersack 1,  Rainer Schobert 4
Affiliations

Affiliations

  • 1 Organic Chemistry Laboratory, University Bayreuth, Universitaetsstrasse 30, 95440, Bayreuth, Germany.
  • 2 Research Center for Integrated Analysis and Territorial Management, University of Bucharest, 4-12, Regina Elisabeta Avenue, Bucharest, 3rd District, 030018, Romania.
  • 3 Department of Cancer Biology, University of Kansas Medical Center, 3901 Rainbow Boulevard, Kansas City, KS, 66160, USA.
  • 4 Organic Chemistry Laboratory, University Bayreuth, Universitaetsstrasse 30, 95440, Bayreuth, Germany. Electronic address: Rainer.Schobert@uni-bayreuth.de.
PMID: 31958738 DOI: 10.1016/j.ejmech.2020.112060
Abstract

A series of forty-six 5,6-annulated 2-arylthieno [2,3-d]pyrimidin-4(3H)-ones were prepared as potentially pleiotropic Anticancer drugs with variance in the tubulin-binding trimethoxyphenyl motif at C-2 of a thieno [2,3-d]pyrimidine fragment, enlarged by additional rings of different size and substitution. By assessing their cytotoxicity against various Cancer cells, their influence on the polymerization of neat tubulin and the dynamics of microtubule and F-actin cytoskeletons, and their vascular-disrupting and anti-angiogenic activities in vitro and in vivo, structure-activity relations were identified which suggest the 3-iodo-4,5-dimethoxyphenyl substituted thienopyrimidine 2e as a promising Anticancer drug candidate for further research. 2020 Elsevier Ltd. All rights reserved.

Keywords

Anti-angiogenesis; Anticancer drugs; Microtubule binding agents; Thienopyrimidine; Vascular-disruptive agents.

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