Abstract

RECENT ADVANCES IN THIENOPYRIMIDINE CHEMISTRY: SYNTHESIS AND THERAPEUTIC EXPLORATION OF THEIR DERIVATIVES (2018-2025)

Priya A.*, Dr. Shachindra L. Nargund and Mahesh Kumar N.

Abstract

Thienopyrimidines are fused bicyclic heterocyclic ring systems composed of a 6-membered Pyrimidine ring and a 5-membered thiophene ring, respectively. They possess substantial therapeutic relevance in the realm of drug discovery. The thienopyrimidine scaffold has served as a starting point for the development of a multitude of clinically validated or under investigation drugs, such as Relugolix (TAK-385), Sufugolix (TAK-013), Pictilisib (GDC-0941), Olmutinib (IKo), Apitolisib, DDP-225, SNS-314, PF-03758309, PRX- 08066, GNE-490, GNE-493, Fimepinostat, and Tepotinib. Due to the extensive therapeutic applications, thienopyrimidine and its derivatives are currently a major focus in drug discovery research. The current review highlights the latest developments in bioactive thienopyrimidine hybrids from 2018 to 2025, underscoring the significant advantages of incorporating thienopyrimidines into drug development. Also, this review presents an in-depth exploration of recent progress in the synthesis and therapeutic potential of thienopyrimidines, serving as a key reference for researchers and professionals in the dynamic field of medicinal chemistry.

Keywords: Drug development, Heterocyclic system, Synthesis, Therapeutic applications, Thienopyrimidine Scaffold.