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Farghaly AM, AboulWafa OM, Baghdadi HH, et al. New thieno[3,2-d]pyrimidine-based derivatives: Design, synthesis and biological evaluation as antiproliferative agents, EGFR and ARO inhibitors inducing apoptosis in breast cancer cells. Bioorg Chem. 2021;115:105208doi: 10.1016/j.bioorg.2021.105208.
Farghaly, A. M., AboulWafa, O. M., Baghdadi, H. H., Abd El Razik, H. A., Sedra, S. M. Y., & Shamaa, M. M. (2021). New thieno[3,2-d]pyrimidine-based derivatives: Design, synthesis and biological evaluation as antiproliferative agents, EGFR and ARO inhibitors inducing apoptosis in breast cancer cells. Bioorganic chemistry, 115105208. https://doi.org/10.1016/j.bioorg.2021.105208
Farghaly, Ahmed M, et al. "New thieno[3,2-d]pyrimidine-based derivatives: Design, synthesis and biological evaluation as antiproliferative agents, EGFR and ARO inhibitors inducing apoptosis in breast cancer cells." Bioorganic chemistry vol. 115 (2021): 105208. doi: https://doi.org/10.1016/j.bioorg.2021.105208
Farghaly AM, AboulWafa OM, Baghdadi HH, Abd El Razik HA, Sedra SMY, Shamaa MM. New thieno[3,2-d]pyrimidine-based derivatives: Design, synthesis and biological evaluation as antiproliferative agents, EGFR and ARO inhibitors inducing apoptosis in breast cancer cells. Bioorg Chem. 2021 Oct;115:105208. doi: 10.1016/j.bioorg.2021.105208. Epub 2021 Jul 26. PMID: 34365057.
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Bioorg Chem. 2021 Oct;115:105208. doi: 10.1016/j.bioorg.2021.105208. Epub 2021 Jul 26.

New thieno[3,2-d]pyrimidine-based derivatives: Design, synthesis and biological evaluation as antiproliferative agents, EGFR and ARO inhibitors inducing apoptosis in breast cancer cells.

Bioorganic chemistry

Ahmed M Farghaly, Omaima M AboulWafa, Hoda H Baghdadi, Heba A Abd El Razik, Samir M Y Sedra, Marium M Shamaa

Affiliations

  1. Department of Pharmaceutical Chemistry, Faculty of Pharmacy, Alexandria University, 21521 Alexandria, Egypt.
  2. Department of Environmental Studies, Institute of Graduate Studies and Research, Alexandria University, Alexandria, Egypt.
  3. Department of Pharmaceutical Chemistry, Faculty of Pharmacy, Alexandria University, 21521 Alexandria, Egypt. Electronic address: [email protected].
  4. Department of Pharmaceutical Chemistry, Faculty of Pharmacy, Pharos University in Alexandria, Alexandria, Egypt.
  5. Clinical and Biological Sciences (Biochemistry and Molecular Biology) Department, College of Pharmacy, Arab Academy for Science, Technology and Maritime Transport, Alexandria, Egypt.

PMID: 34365057 DOI: 10.1016/j.bioorg.2021.105208

Abstract

An array of newly synthesized thieno[3,2-d]pyrimidine-based derivatives and thienotriazolopyrimidines hybridized with some pharmacophoric anticancer fragments were designed, synthesized and assessed for their in vitro antiproliferative activity against MCF-7 and MDA-MB-231 breast cancer cell lines using erlotinib and pictilisib as reference standards in the MTT assay. In general, many compounds were endowed with considerable antiproliferative activity (IC

Copyright © 2021 Elsevier Inc. All rights reserved.

Keywords: ARO; Antiproliferative activity; Apoptosis; Caspase-9; Cell cycle analysis; Docking; Downstream signaling protein expression; EGFR; MCF-7 and MDA-MB-231 breast cancer cells; Thieno[3,2-d]pyrimidines

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