Thiophene derivatives: A potent multitargeted pharmacological scaffold

Abstract

Despite a significant work that has been done on thiophene, continuous efforts are still being made by the researchers to identify novel heterocyclic compounds with potential bioactivities. Thiophene nucleus has been extensively utilized by the researchers across the globe for the development of diverse bioactive heterocycles for hitting a wide range of biological targets. This review throws light on synthetic approaches that have been used for the synthesis of potential thiophene derivatives followed by the depth analysis of them with respect to their pharmacological significance. This review can help the medicinal chemists and researchers to develop novel leads having thiophene nucleus with high efficacy and reduced side effects.

H2O2:HCl Catalyzed Synthesis of 5-(3-Substituted-Thiophene) Pyrimidine Derivatives and Evaluation for Their Pharmacological Effects

“…5. The Kb values of compounds (3a-d) are found to be 1.1216X10 7 , 1.4072X10 7 , 1.0634X10 7 and 3.4872X10 7 respectively appear in Table 6. These Kb values conforms all the synthesized compounds interacted strongly with CT-DNA.…”

“…Current chemotherapies suffers major limitation of side effect and drug resistance, therefore continued search for novel and safer anticancer drugs remains as important [5]. Pyrimidine and thiophene have been recognized as key scaffolds due to its biological significances such as antiviral, antibacterial, antifungal, anticancer, antiinflammatory, anti-diabetic, anti-tubercular, antioxidant, anti-parasitic, anti-convulsants, antidepressant, analgesic, antitumor, gastro protectors and kinase inhibitors [6,7].…”

Convenient synthesis and anticancer evaluation of novel pyrazolyl‐thiophene, thieno[3,2‐b]pyridine, pyrazolo[3,4‐d]thieno[3,2‐b]pyridine and pyrano[2,3‐d]thieno[3,2‐b]pyridine derivatives

“…Substituted thiophenes have been utilized as key structural units in significant bioactive pharmacophores, [1,2] and also as important building blocks in organic and medicinal chemistry. [3][4][5] Several thiophene-based compounds have been synthesized to screen their biological activities such as antimicrobial, [6][7][8] cytotoxic, [9,10] antiinflammatory, [11] anti-arrhythmic, [12] and antidepressant [13] agents. Many thiophene derivatives like ISO-930, Raloxifene, and Raltitrexed (Figure 1) have been marketed as anticancer agents.…”

Synthesis and Bioactivity Evaluation of Indole-Thiophene polymer with Molecular Docking Studies

“…Several studies revealed that the solubility of active pharmaceutical ingredients can be increased by the preparation of nanoparticles and by optimization of physicochemical properties [9,10,11]. Besides, indole and thiophene derivatives have wide range of pharmacological activity including anticancer, antimicrobial and antiinflammatory [12,13,14,15,16,17,18,19].…”