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- 저자 : Yogeeswari Perumal (검색결과 2 건)
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A Novel, Potent, Small Molecule AKT Inhibitor Exhibits Efficacy against Lung Cancer Cells In Vitro
Saketh S. Dinavahi,Rajagopalan Prasanna,Sriram Dharmarajan,Yogeeswari Perumal,Srikant Viswanadha 대한암학회 2015 Cancer Research and Treatment Vol.47 No.4
Purpose Anomalies of Akt regulation, including overexpression in lung cancer, impart resistance toconventional chemotherapy and radiation, thereby implicating this kinase as a therapeuticintervention point. A novel scaffold of Akt inhibitors was developed through virtual screeningof chemical databases available at Birla Institute of Technology and Science, Pilani, Hyderabad,based on docking studies using Maestro. A benzothienopyrimidine derivative (BIA-6)was identified as a potential lead molecule that inhibited Akt1 enzyme activity with an IC50of 256 nM. Materials and MethodsBIA-6 was tested for in vitro Akt1 inhibition using a fluorescence resonance energy transferkit. Anti-proliferative activity was tested in NCI-H460, A549, NCI-H1975, and NCI-H2170cell lines. The effect of the compound on p-Akt (S473) was estimated. ResultsBIA-6 allosterically caused a dose dependent reduction of growth of cell lines with a halfmaximal growth inhibition (GI50) range of 0.49 !M to 6.6 !M. Cell cycle analysis indicatedthat BIA-6 caused a G1 phase arrest at < 100 nM but led to apoptosis at higher doses. BIA-6 also exhibited synergism with standard chemotherapeutic agents. ConclusionBIA-6 is a novel, allosteric Akt inhibitor with potent anti-cancer activity in lung cancer celllines, that effectively blocks the phosphoinositide-3 kinase/Akt pathway with a high marginselectivity towards normal cells.
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Hajjaj H. M. Abdu-Allah,Bahaa G. M. Youssif,Mostafa H. Abdelrahman,Mohammed K. Abdel-Hamid,Rudraraju Srilakshmi Reshma,Perumal Yogeeswari,Tarek Aboul-Fadl,Dharmarajan Sriram 대한약학회 2017 Archives of Pharmacal Research Vol.40 No.2
The antitubercular drug; para-aminosalicylicacid (PAS) was used as the core scaffold for the design of aseries of 1H-1,2,3-triazolylsalicylhydrazones upon couplingwith triazole and arylhydrazone moietis to furnish asingle molecular architecture. The obtained derivativeswere screened against Mycobacterium tuberculosis H37Rvrevealing good to high activity for the active compounds(MIC values of 0.39–1.5 lg/mL) compared to the marketeddrugs isoniazid, rifampicin and ethambutol. Moreover, themost active analogue N-(1-(4-chlorobenzyl)-2-oxoindolin-3-ylidene)-2-hydroxy-4-(4-phenyl-1H-1,2,3-triazol-1-yl)-benzohydrazide (20) was found to be ten-fold more potentthan PAS and equipotent to rifampicin (MIC 0.39 lg/mL),while exhibiting low cytotoxicity with a selectivity indexof[128. In addition, this compound was shown to beactive against persistent forms of mycobacteria comparableto standard drugs in nutrient starvation model. Accordingly,we introduce compound 20 as a valuable lead forfurther development. A 3D-QSAR study was also conductedto help in explaining the observed activity and toserve as a tool for further development.
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