Diverse Thiophenes as Scaffolds in Anti-cancer Drug Development: A Concise Review

Abstract

: Thiophenes are one among the abundantly found heterocyclic ring systems in many biologically active compounds. Moreover various substituted thiophenes exert numerous pharmacological actions on account of their isosteric resemblance with compounds of natural origin thus rendering them with diverse actions like antibacterial, antifungal, antiviral, anti-inflammatory, analgesic, antiallergic, hypotensives etc.. In this review we specifically explore the chemotherapeutic potential of variety of structures consisting of thiophene scaffolds as prospective anticancer agents.

Noncovalent Interactions between Aromatic Heterocycles and Carboxylic Acids: Rotational Spectroscopy of the Furan–Formic Acid and Thiophene–Formic Acid Complexes

“…Furan and thiophene, heteroaromatics widely occurring in plants, algae and microorganisms, are the important constitutional units of polymers, natural products, medicines, and functional materials. − Due to their amphoteric nature, the lone-pair (LP) electrons of the oxygen or sulfur atom and π-electron can act as proton acceptors while the hydrogen atoms of the ring act as proton donors, and both furan and thiophene have great flexibility in forming different kinds of HBs. In the complexes of furan with HF, − and NH 3 , the preferred docking site of the furan is the O atom.…”

Experimental and computational evidence for stabilising parallel, offset π[C(O)N(H)NC]⋯π(phenyl) interactions in acetohydrazide derivatives

“…29 Studies into the latter relate to anti-bacterial, 30 including antimycobacterial, 31 anti-inflammatory 32 and anti-cancer activities. 33 Continuation of previous work on the biological activities and structural chemistry of acetohydrazides [34][35][36] led to the investigation of such derivatives bearing thienyl residues. Thus, four series of 2-thienyl(CH 2 ) n C(O)N(R) NC(H)-Ar [n = 0 or 1; R = H or Me] were prepared and tested as tuberculostatic agents against Mycobacterium tuberculosis H37Rv (ATTC27294) 37,38 and against three cancer cell lines.…”

Synthesis, Biological Evaluation, and Docking Study of a New Series of Thiophene Derivatives Based on 3‐Oxobutanamidothiophene as an Anticancer Agent

“…[22,23] In light of the above considerations, a number of novel heterocyclic scaffolds with a thiophene moiety were created by reacting 3-oxobutanamidothiophene derivatives 2 a and 2 b with diverse nucleophiles in the presence of distinct bases. These compounds were then studied for their biological effects [24,25] as anti-cancer agents against two cancer cells: hepatocellular carcinoma and breast cancer.…”