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  3. Thieno[2,3-d]pyrimidine as a promising scaffold in medicinal chemistry: Recent advances

Thieno[2,3-d]pyrimidine as a promising scaffold in medicinal chemistry: Recent advances

  • Bioorg Med Chem. 2019 Apr 1;27(7):1159-1194. doi: 10.1016/j.bmc.2019.02.044.
Eslam M H Ali 1,  Mohammed S Abdel-Maksoud 2,  Chang-Hyun Oh 3
Affiliations

Affiliations

  • 1 Center for Biomaterials, Korea Institute of Science & Technology (KIST), Seoul, Seongbuk-gu 02792, Republic of Korea; Department of Biomolecular Science, University of Science & Technology (UST), Daejeon, Yuseong-gu 34113, Republic of Korea.
  • 2 Medicinal & Pharmaceutical Chemistry Department, Pharmaceutical and Drug Industries Research Division, National Research Centre (NRC), Dokki, Giza 12622, Egypt.
  • 3 Center for Biomaterials, Korea Institute of Science & Technology (KIST), Seoul, Seongbuk-gu 02792, Republic of Korea; Department of Biomolecular Science, University of Science & Technology (UST), Daejeon, Yuseong-gu 34113, Republic of Korea. Electronic address: choh@kist.re.kr.
PMID: 30826188 DOI: 10.1016/j.bmc.2019.02.044
Abstract

Thienopyrimidine scaffold is a fused heterocyclic ring system that structurally can be considered as adenine, the purine base that is found in both DNA and RNA-bioisosteres. Thienopyrimidines exist in three distinct isomeric forms. The current review discusses thieno[2,3-d]pyrimidine as a one of the opulent heterocycles in drug discovery. Its broad range of medical applications such as Anticancer, anti-inflammatory, anti-microbial, and CNS protective agents has inspired us to study its structure-activity relationship (SAR), along with its relevant synthetic strategies. The present review briefly summarizes synthetic approaches for the preparation of thieno[2,3-d]pyrimidine derivatives. In addition, the promising biological activities of this scaffold are also illustrated with explanatory diagrams for their SAR studies.

Keywords

Anti-inflammatory; Anticancer; Antimicrobial; Antiviral; CNS protective agents; Thienopyrimidine.

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