Thieno[3,2-b]pyrrole as a privileged scaffold in medicinal chemistry: An exploration of synthetic strategies and anticancer attributes

Abstract

Heterocyclic structural frameworks are the backbone of chemistry, especially in material and medicinal chemistry. Concerning medicinal chemistry, more than 75 % of approved drugs under clinical utilization or clinical investigations possess heterocyclic structural fragments. Thieno[3,2-b]pyrrole is a privileged heterocyclic pharmacophore with fused pyrrole and thiophene rings. The recent advancements in the synthetic methodologies and broad opportunities for structural alteration, thieno[3,2-b]pyrrole as a synthon has accelerated the interest of medicinal chemists toward utilization of this structural fragment in pharmacophores for the development of new anticancer drug candidates possessing high efficiency and specificity to diverse targets. The current report emphasizes the innumerable synthetic methodologies reported for synthesizing thieno[3,2-b]pyrroles, along with recent advancements and applications. We have discussed thieno[3,2-b]pyrroles' biological potential, focusing on anticancer potential and their SAR studies. We have also compiled a list of recently granted patents on thieno[3,2-b]pyrroles to various research groups. This study will assist in recognizing thieno[3,2-b]pyrrole derivatives that have high potency and efficacy as anticancer ligands, which can be identified for further clinical investigations to develop new drug molecules.