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2000
Volume 21, Issue 9
  • ISSN: 1573-4072
  • E-ISSN: 1875-6646

Abstract

Introduction

A preliminary biological evaluation of ten synthesized analogs, {[5-(E)-benzylidene amino]-1,3,4-thiadiazol-2-yl} cyclohexane-1,2,3,5-tetrol, revealed promising results, positioning these compounds as potential lead candidates for further optimization and preclinical exploration in cancer therapy. Incorporating the 1,3,4-thiadiazol moiety into the structure of the produced analogs considerably improved their anticancer activities, revealing the compound's high potential for cancer treatment. Spectroscopic approaches and structural analysis, such as elemental analysis, IR, 1H NMR, 13C NMR, and MS, were crucial for properly establishing the molecular structures of these analogs and evaluating their anticancer activity. These methodologies laid a solid platform for rationally developing new anticancer medications with increased efficacy and fewer adverse effects. Furthermore, computational tools like molecular docking, ADMET prediction, and drug-likeness evaluation have accelerated the drug development by finding the most promising lead candidates for preclinical and clinical trials. This technique not only saves time and costs, but also raises the chances of producing successful anticancer drugs.

Methods

The main aim of the current study is to develop, synthesize, , potentials of {5-[()-benzylidene amino]-1,3,4-thiadiazol-2-yl} cyclohexane-1,2,3,5-tetrol for a possible anticancer drug to improve their efficiency and selectivity against cancer cells, computational approaches aided in the rational design of these chemicals. Spectroscopic methods verified the chemical structures of the target compounds. The structures show the presence of 1,3,4-thiadiazol also responsible for anticancer activity. The 10 analogs were synthesized and showed encouraging anticancer efficacy in preliminary biological evaluation, suggesting they might be suitable lead candidates for more optimization and preclinical exploration.

Results

{5-[()-benzylidene amino]-1,3,4-thiadiazol-2-yl} cyclohexane-1,2,3,5-tetrol derivatives showed optimum IC values in activity by SRB assay using MCF-7 as a strain, the few selected analogs.

Conclusion

The study synthesized cyclohexane-1,2,3,5-tetrol analogs and evaluated their potential for cancer therapy. The compounds showed promising cytotoxic activity against various cancer cell lines, with and showing the most potent anti-proliferative effects. These compounds induce apoptosis mitochondrial dysfunction and cell cycle arrest. Further preclinical investigations are needed to establish their therapeutic potential.

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2025-01-09
2025-10-21

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Synthesis and Biological Evaluation of Cyclohexane-1,2,3,5-Tetrol Analogs as Potential Lead Candidates for Cancer Therapy
Curr. Bioact. Compd. 21, e15734072337125 (2025); https://doi.org/10.2174/0115734072337125241228011338
/content/journals/cbc/10.2174/0115734072337125241228011338
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  • Article Type:     Research Article
Keyword(s): 1,3,4,5tetrahydroxycyclohexyl derivatives; Anticancer; cancer therapy; molecular docking; SRB assay; topoisomerase

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