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High-throughput Identification of Synergistic Drug Combinations by the Overlap2 Method
Published on: May 21, 2018
Harnessing Synergy: A Review on the Synthesis and Bioactivity of Artemisinin-Isatin Hybrid Molecules
Vishal Choudhary1, Aanya Saini1, Emmanuel F Freeman1
1Department of Chemistry, School of Applied and Life Sciences, Uttaranchal University, Dehradun, 248007, Uttarakhand, India.
Introduction:
To examine the design, synthesis, and pharmacological potential of novel artemisinin-isatin hybrid compounds as a strategy to overcome drug resistance and expand therapeutic applications beyond malaria.
Methods:
Researchers employed molecular hybridization techniques-specifically Cu-promoted azide-alkyne cycloaddition, etherification, and esterification-to covalently link modified isatin moieties to the artemisinin scaffold. These methods produced diverse series of triazole, two-carbon, and ester-tethered hybrids. The compounds were evaluated using MTT assays to determine biological activity against various cancer cell lines.
Results:
Pharmacological testing identified several potent hybrids: Hybrids 3c and 3d: Demonstrated efficacy against breast cancer lines comparable to the standard drug doxorubicin. Hybrid 5d: Showed significant anti-leukemic activity with an enhanced safety profile. SAR Analysis: Structure-activity relationship (SAR) data indicated that therapeutic effectiveness is highly dependent on the length of the alkyl linker (with two carbons being ideal) and specific modifications at the C-3 and C-5 positions.
Discussion:
The review discussed the preparation and biological activities of artemisinin and isatin hybrid molecules. It has been discussed that after the resistant reported against artemisinin, several approaches have been tried to improve the efficacy of drugs in the treatment of deadly diseases like malaria. It has been found that hybrids like artemisinin-1,2,3-triazole-isatin, dihydroartemisininisatin, two-carbon tethered artemisinin-isatin hybrids, ester tethered artemisinin-isatin hybrids, ester tethered artemisinin-isatin hybrids reported better efficacy. Also, the comparison between linkers showed that alkyl linkers provide more potency than 1,2,3- triazole linkers for artemisinin and isatin hybrids.
Conclusion:
Artemisinin-isatin hybrids represent a promising new class of pharmaceuticals that utilize synergy to target multiple cellular pathways. These hybrids offer a robust approach for treating complex diseases, including aggressive breast cancer and leukemia, while addressing the challenges of drug resistance.
