Dithiocarbamate substituted phenothiazine derivatives: in silicoexperiments, synthesis,and biological evaluation
By: Kotha, Anusha
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Contributor(s): Muni Sireesha, S.
Publisher: M P Innovare Academic Sciences Pvt Ltd 2021Edition: Vol.13(10).Description: 25-30p.Subject(s): PHARMACEUTICSOnline resources: Click here
In:
International journal of pharmacy and pharmaceutical scienceSummary: Objective: The present study was designed to study the anticancer activity of a series of novel analogs of phenothiazine with dithiocarbamate as a side chain.Methods: A novel series of derivatives containing dithiocarbamate as a side chain at the tenth position of phenothiazine nucleus were synthesized, characterized by spectral analysis, and evaluated for their antimitotic and antioxidant activity using germinated Bengal gram seeds and 2,2-diphenyl-1-picrylhydrazyl (DPPH)method,respectively. A quantitative estimate of drug-likeness was also performed,which calculated the molecular properties and screenedthe molecules based on drug-likeness rules.Further, molecular docking study was performed for finding the binding affinity with tubulin protein to rationalize their anticancer activity.Results: The results revealed that the antioxidant activity of compounds3e, 3g, 3i, 3j andstandard Ascorbic acid were 10 mmol, 14 mmol, 16 mmol, 16 mmoland 35 mmol,respectively. Further compounds 3e, 3g, 3h and 3i have shown promising antimitotic activity. Compound 3i (-9 K. Cal/mol) showed the highest binding energies towards tubulin protein when compared to standard drug colchicine (-8.6 K. Cal/mol). Among all, compound 3i showed promising antimitoticand antioxidant activity, which correlated with insilico docking studies.Conclusion: Dithiocarbamate substituted phenothiazine derivatives proved to be encouraging leads as tubulin inhibitors.
| Item type | Current location | Call number | Status | Date due | Barcode | Item holds |
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Articles Abstract Database
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School of Pharmacy Archieval Section | Not for loan | 2022-0400 |
Objective: The present study was designed to study the anticancer activity of a series of novel analogs of phenothiazine with dithiocarbamate as a side chain.Methods: A novel series of derivatives containing dithiocarbamate as a side chain at the tenth position of phenothiazine nucleus were synthesized, characterized by spectral analysis, and evaluated for their antimitotic and antioxidant activity using germinated Bengal gram seeds and 2,2-diphenyl-1-picrylhydrazyl (DPPH)method,respectively. A quantitative estimate of drug-likeness was also performed,which calculated the molecular properties and screenedthe molecules based on drug-likeness rules.Further, molecular docking study was performed for finding the binding affinity with tubulin protein to rationalize their anticancer activity.Results: The results revealed that the antioxidant activity of compounds3e, 3g, 3i, 3j andstandard Ascorbic acid were 10 mmol, 14 mmol, 16 mmol, 16 mmoland 35 mmol,respectively. Further compounds 3e, 3g, 3h and 3i have shown promising antimitotic activity. Compound 3i (-9 K. Cal/mol) showed the highest binding energies towards tubulin protein when compared to standard drug colchicine (-8.6 K. Cal/mol). Among all, compound 3i showed promising antimitoticand antioxidant activity, which correlated with insilico docking studies.Conclusion: Dithiocarbamate substituted phenothiazine derivatives proved to be encouraging leads as tubulin inhibitors.
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