Imidazo[2,1-b] [1,3,4]thiadiazole: A Versatile Scaffold in Anticancer Drug Discovery - Impact of C-2, C-5, and C-6 Substitutions

Imidazo[2,1-b][1,3,4]thiadiazoles, a class of fused bicyclic heterocycles, have garnered significant interest in medicinal chemistry due to their diverse biological activities, particularly their anticancer properties. Over recent decades, extensive research has been conducted to explore and enhance their therapeutic potential. This comprehensive review spans six decades of research on the imidazo[2,1-b][1,3,4]thiadiazole scaffold, focusing on structural variations at C-2, C-5, and C-6 position on this scaffold and their implications for anticancer activity. Modifications at these positions have been shown to significantly impact the compound's efficacy against various cancer cell lines. Continuous exploration and optimization of these substitutions hold promise for the development of novel anticancer therapeutics.

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Publication Details

Journal
Mini-Reviews in Medicinal Chemistry
Published
2025-10-24
DOI
https://doi.org/10.2174/0113895575415617251007055129
Primary Topic
Synthesis and biological activity
Type
article
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article

Imidazo[2,1-b] [1,3,4]thiadiazole: A Versatile Scaffold in Anticancer Drug Discovery - Impact of C-2, C-5, and C-6 Substitutions

Fadzilah Adibah Abdul Majid, Dwi Hudiyanti, Wan Mohd Norsani Bin Wan
Mini-Reviews in Medicinal Chemistry
Synthesis and biological activity
article

Imidazo[2,1-b] [1,3,4]thiadiazole: A Versatile Scaffold in Anticancer Drug Discovery - Impact of C-2, C-5, and C-6 Substitutions

Fadzilah Adibah Abdul Majid, Dwi Hudiyanti, Wan Mohd Norsani Bin Wan
article en

Abstract

Imidazo[2,1-b][1,3,4]thiadiazoles, a class of fused bicyclic heterocycles, have garnered significant interest in medicinal chemistry due to their diverse biological activities, particularly their anticancer properties. Over recent decades, extensive research has been conducted to explore and enhance their therapeutic potential. This comprehensive review spans six decades of research on the imidazo[2,1-b][1,3,4]thiadiazole scaffold, focusing on structural variations at C-2, C-5, and C-6 position on this scaffold and their implications for anticancer activity. Modifications at these positions have been shown to significantly impact the compound's efficacy against various cancer cell lines. Continuous exploration and optimization of these substitutions hold promise for the development of novel anticancer therapeutics.

Mini-Reviews in Medicinal ChemistryVol. 25(21)
Diponegoro University (ID), Universiti Malaysia Terengganu (MY), Mangalore University (IN)
Openalex Percentile: Top 77%
Synthesis and biological activity
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Imidazo[2,1-b] [1,3,4]thiadiazole: A Versatile Scaffold in Anticancer Drug Discovery - Impact of C-2, C-5, and C-6 Substitutions — Fadzilah Adibah Abdul Majid, Dwi Hudiyanti, et al. · Mini-Reviews in Medicinal Chemistry (2025) | TGRS Research Map | TGRS