Novel hybrids of drug with bioactive heterocycles for enhancing biological activity

A novel series of aceclofenac hybridised with 1,2,4-triazolo-[3,4-b]-1,3,4-thiadiazoles were designed using molecular hybridization approach and synthesised 6a – j . The structural integrity was confirmed by analytical methods. The hybrid molecules were subjected to in vitro cytotoxic studies agains...

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Bibliographic Details
Published in:Archives of pharmacal research 2016, 39(10), , pp.1382-1390
Main Authors: Valentina, Parthiban, Ilango, Kaliappan, Kathiravan, Muthu K.
Format: Article
Language:English
Subjects:
Antifungal Agents - chemistry
Antifungal Agents - pharmacology
Aspergillus niger - drug effects
Aspergillus niger - physiology
Biological Products - chemistry
Biological Products - pharmacology
Candida albicans - drug effects
Candida albicans - physiology
Heterocyclic Compounds - chemistry
Heterocyclic Compounds - pharmacology
Humans
MCF-7 Cells
Medicine
Pharmacology/Toxicology
Pharmacy
Research Article
Structure-Activity Relationship
Thiadiazoles - chemistry
Thiadiazoles - pharmacology
Triazoles - chemistry
Triazoles - pharmacology
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Summary:A novel series of aceclofenac hybridised with 1,2,4-triazolo-[3,4-b]-1,3,4-thiadiazoles were designed using molecular hybridization approach and synthesised 6a – j . The structural integrity was confirmed by analytical methods. The hybrid molecules were subjected to in vitro cytotoxic studies against four human cancer cell lines PA‐1, OAW‐42, T47-D and MCF‐7 by MTT assay method. The results indicate that the hybrid molecules bearing halogen on phenyl ring in 6th position of triazolo-thiadiazole exhibited significant cytotoxic activity. The test compounds were also screened for antifungal activity against two strains.
ISSN:0253-6269
1976-3786
DOI:10.1007/s12272-016-0797-6