2D-QSAR study of some 2,5-diaminobenzophenone farnesyltransferase inhibitors by different chemometric methods

Ghanbarzadeh, Saeed; Ghasemi, Saeed; Shayanfar, Ali; Ebrahimi‐Najafabadi, Heshmatollah

doi:10.17179/excli2015-177

EXCLI Journal; 14:Doc484; ISSN 1611-2156 2015

DOI: 10.17179/excli2015-177

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2D-QSAR study of some 2,5-diaminobenzophenone farnesyltransferase inhibitors by different chemometric methods

Saeed Ghanbarzadeh

Saeed Ghasemi

Ali Shayanfar

et al.

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Cited by 2 publications

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Antioxidant and Larvicidal Activity of Areal Parts of Scrophularia striata against Malaria Vector Anopheles stephensi

Yousefbeyk¹,

Vatandoost²,

Golfakhrabadi³

et al. 2018

JAD

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Background:Scrophularia striata is a perennial plant which is native in all parts of Iran, Turkey, and Azerbaijan. In this study, the total phenol content, antioxidant and larvicidal activities of total extract and different fractions of this plant were evaluated.Methods:The aerial parts of S. striata were collected from Boli village, Illam Province, western Iran in Apr 2013. The total phenol content of total extract and different fractions were evaluated by Folin-Ciocalteu method. Moreover, antioxidant activity was tested by DPPH and FRAPS assays. Larvicidal activity was investigated according to standard method described by WHO.Results:Ethyl acetate fraction (EF) had the highest content of total phenol (75.9±0.06mg Gallic acid equivalent/g dry extract). Furthermore, among the tested extract, methanol-water fraction (MWF), total methanol extract (TME) and water fraction (WF) showed the highest antioxidant activity in the DPPH assay (IC50= 226.8, 283.66 and 299.4 μg.ml−1, respectively). In FRAP assay MWF and WF and TME had the highest antioxidant activities (664.4±0.002, 565.3±0.003, 519.5±0.003mmol FeII/g dry extract, respectively). Ethyl acetate fraction had maximum larvicidal activity (LC50 49.1ppm) followed by TME (LC50 64.26ppm) and hexane fraction (HF) (LC50 89.69).Conclusion:Scrophularia striata collected from west of Iran illustrated considerable antioxidant and larvicidal effects and further in vitro and in vivo experimental models for investigation would be required.

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Antioxidant and Larvicidal Activity of Areal Parts of Scrophularia striata against Malaria Vector Anopheles stephensi

Yousefbeyk¹,

Vatandoost²,

Golfakhrabadi³

et al. 2018

JAD

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Design, Synthesis and Biological Evaluation of Novel Piperazinone Derivatives as Cytotoxic Agents

2020

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Purpose : In this study, a series of piperazin-2-one derivatives were prepared through bioisosteric substitution of the imidazole ring of L-778,123 (imidazole-containing FTase inhibitor) and rearrangement of groups based on the tipifarnib structure. Final compounds were evaluated for their cytotoxic activities on cancer and normal cell lines by MTT assay. Methods: Methyl α-bromophenylacetic acid and 1-(3-chlorophenyl) piperazin-2-one were synthesized using previously described methods. Methyl 2-(4-chlorophenyl)-2-(4-(3- chlorophenyl)-3-oxopiperazin-1-yl) acetate was prepared by reaction between these two compounds in presence of potassium carbonate. Finally, methoxy group of ester was substituted by various amines such as guanidine, thiourea, urea and hydrazide. The synthesized compounds were tested for their cytotoxicity against colon cancer (HT-29) and lung cancer (A549) cell lines as well as MRC-5 (normal fetal lung fibroblasts) cells as a healthy cell line using MTT colorimetric assay method. Results: Replacement of imidazole moiety with guanidine, thiourea, and hydrazide could increase cytotoxicity toward all three cell lines. Some substituents, such as amine, urea, and hydroxylamine exhibited significant cytotoxicity (<500 µM) but lower than L-778,123 as standard compound. Hydroxyl and methoxy substituents did not show significant cytotoxicity. Imidazole substituent group revealed cytotoxicity similar to L-778,123 All compounds showed lower cytotoxic activity against normal cell lines compared with cancer cell lines. Conclusion: It seems the electron density of substituted groups and rearrangement of groups may significantly increase cytotoxic activity

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2D-QSAR study of some 2,5-diaminobenzophenone farnesyltransferase inhibitors by different chemometric methods

Cited by 2 publications

References 34 publications

Antioxidant and Larvicidal Activity of Areal Parts of Scrophularia striata against Malaria Vector Anopheles stephensi

Antioxidant and Larvicidal Activity of Areal Parts of Scrophularia striata against Malaria Vector Anopheles stephensi

Design, Synthesis and Biological Evaluation of Novel Piperazinone Derivatives as Cytotoxic Agents

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