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

• Published in: Bioorganic & medicinal chemistry 2019-04, Vol.27 (7), p.1159-1194
• Main Authors: Ali, Eslam M.H., Abdel-Maksoud, Mohammed S., Oh, Chang-Hyun
• Format: Article
• Language: English
• Subjects: Anti-Infective Agents - chemical synthesis; Anti-Infective Agents - chemistry; Anti-Infective Agents - pharmacology; Anti-inflammatory; Anti-Inflammatory Agents, Non-Steroidal - chemical synthesis; Anti-Inflammatory Agents, Non-Steroidal - chemistry; Anti-Inflammatory Agents, Non-Steroidal - pharmacology; Anticancer; Antimicrobial; Antineoplastic Agents - chemical synthesis; Antineoplastic Agents - chemistry; Antineoplastic Agents - pharmacology; Antiviral; Chemistry, Pharmaceutical; CNS protective agents; Humans; Inflammation - drug therapy; Neoplasms - drug therapy; Pyrimidines - chemical synthesis; Pyrimidines - chemistry; Pyrimidines - pharmacology; Structure-Activity Relationship; Thienopyrimidine
• ISSN: 0968-0896; 1464-3391
• DOI: 10.1016/j.bmc.2019.02.044

[Display omitted] •Comprehensive review on thieno[2,3-d]pyrimidine scaffold.•Detailed presentation of different synthetic pathways of Thieno[2,3-d]pyrimidines.•Anticancer activity and SAR of compounds containing thieno[2,3-d]pyrimidine.•Kinases inhibitory effect of thieno[2,3-d]pyrimidine derivatives.•Biological activities of thieno[2,3-d]pyrimidines were reported. 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.