Publications by authors named "Meshari A Alsharif"

4 Publications

  • Page 1 of 1

Medicinal Potential of Isoflavonoids: Polyphenols That May Cure Diabetes.

Molecules 2020 Nov 24;25(23). Epub 2020 Nov 24.

Department of Pharmaceutical and Medicinal Chemistry, Faculty of Pharmaceutical Sciences, Usmanu Danfodiyo University, P M B: 2436 Sokoto, Nigeria.

In recent years, there is emerging evidence that isoflavonoids, either dietary or obtained from traditional medicinal plants, could play an important role as a supplementary drug in the management of type 2 diabetes mellitus (T2DM) due to their reported pronounced biological effects in relation to multiple metabolic factors associated with diabetes. Hence, in this regard, we have comprehensively reviewed the potential biological effects of isoflavonoids, particularly biochanin A, genistein, daidzein, glycitein, and formononetin on metabolic disorders and long-term complications induced by T2DM in order to understand whether they can be future candidates as a safe antidiabetic agent. Based on in-depth in vitro and in vivo studies evaluations, isoflavonoids have been found to activate gene expression through the stimulation of peroxisome proliferator-activated receptors (PPARs) (α, γ), modulate carbohydrate metabolism, regulate hyperglycemia, induce dyslipidemia, lessen insulin resistance, and modify adipocyte differentiation and tissue metabolism. Moreover, these natural compounds have also been found to attenuate oxidative stress through the oxidative signaling process and inflammatory mechanism. Hence, isoflavonoids have been envisioned to be able to prevent and slow down the progression of long-term diabetes complications including cardiovascular disease, nephropathy, neuropathy, and retinopathy. Further thoroughgoing investigations in human clinical studies are strongly recommended to obtain the optimum and specific dose and regimen required for supplementation with isoflavonoids and derivatives in diabetic patients.
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http://dx.doi.org/10.3390/molecules25235491DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC7727648PMC
November 2020

Synthesis and Anti-Proliferative Evaluations of New Heterocyclic Derivatives Using 5,6,8,9-Tetrahydropyrazolo[5,1-b]quinazolin-7(3H)-one Derivatives Derived from Cyclohexa-1,4-dione.

Anticancer Agents Med Chem 2021 ;21(4):468-486

Department of Chemistry, Faculty of Science, Cairo University, Giza, Egypt.

Background: Recentlty, pyrazoloquinazoline derivatives acquired a special attention due to their wide range of pharmacological activities, especially therapeutic. Through the market, it was found that many pharmacological drugs containing the quinazoline nucleus were known.

Objective: The aim of this work is to synthesize target molecules possessing not only anti-tumor activities but also kinase inhibitors. The target molecules were obtained through the synthesis of a series of 5,6,8,9- tetrahydropyrazolo[5,1-b]quinazolin-7(3H)-one derivatives 4a-i using the multi-component reactions of cyclohexane- 1,4-dione (1), the 5-amino-4-(2-arylhydrazono)-4H-pyrazol-3-ol derivatives 2a-c, the aromatic aldehydes 3a-c, respectively. The synthesized compounds were evaluated against c-Met kinase, PC-3 cell line, and different kinds of cancer cell lines together with normal cell line, tyrosine kinases, and Pim-1 kinase.

Methods: Multi-component reactions were adopted using compound 1 to get different 5,6,8,9- tetrahydropyrazolo[5,1-b]quinazolin-7(3H)-one derivatives which underwent further heterocyclization reactions. The c-Met kinase activity of all compounds was evaluated using Homogeneous Time-Resolved Fluorescence (HTRF) assay, taking foretinib as the positive control. The anti-proliferative activity of all target compounds against the human prostatic cancer PC-3 cell line was measured using MTT assay using SGI-1776 as the reference drug. All the synthesized compounds were assessed for inhibitory activities against A549 (non-small cell lung cancer), H460 (human lung cancer), HT-29 (human colon cancer), and MKN-45 (human gastric cancer) cancer cell lines together with foretinib as the positive control by an MTT assay.

Results: Antiproliferative evaluations and c-Met kinase, Pim-1 kinase inhibitions were performed for the synthesized compounds, where the varieties of substituents through the aryl ring and the thiophene moiety afforded compounds with high activities.

Conclusion: The compounds with high antiproliferative activity were tested towards c-Met and the results showed that compounds 4e, 4f, 4g, 4i, 6i, 6k, 6l, 8f, 8i, 10d, 10e, 10f, 10h, 12e, 12f, 12g, 12h, 12i, 14f, 14g, 14h, and 14i were the most potent compounds. A further selection of compounds for the Pim-1 kinase inhibition activity showed that compounds 4f, 6i, 6l, 8h, 8i, 8g, 10d, 12i, and 14f were the most active compounds to inhibit Pim-1.
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http://dx.doi.org/10.2174/1871520620666200523162549DOI Listing
January 2021

One-pot synthesis of 1,5-diketones from 3-acetyl-4-hydroxycoumarin and effective cyclization to unexpected 3,4-dihydropyridines.

Org Biomol Chem 2018 05;16(18):3428-3437

Department of Chemistry, Indian Institute of Technology Roorkee, Roorkee-247667, Uttarakhand, India.

A facile synthesis of 1,5-diketones from 3-acetyl-4-hydroxycoumarin, aldehydes and cyclic-ketones via a one-pot aldol condensation and subsequent Michael addition reaction in the presence of a single catalyst of l-proline under mild reaction conditions has been developed. Novel 1,5-diketones were further cyclized to unexpected 3,4-dihydropyridines rather than generally formed pyridine analogues with ammonium acetate in acetic acid. One pot, high yields (72-92%) for novel 1,5-diketones and (70-90%) for the 3,4-dihydropyridine adducts, easy work-up and purification of products are the key advantages of this method.
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http://dx.doi.org/10.1039/c8ob00718gDOI Listing
May 2018

Retracted: Novel spiro-thiazolidin-4-one and thioether derivatives of benzylidene flavanones: New leads in cancer and microbial chemotherapy.

Arch Pharm (Weinheim) 2018 May 12;351(5):e1700397. Epub 2018 Mar 12.

Department of Interdisciplinary Biotechnology, Aligarh Muslim University, Aligarh, India.

The above article from Archiv der Pharmazie, published online on 12 March 2018 in Wiley Online Library (wileyonlinelibrary.com), has been retracted by agreement between the authors, the journal Editor-in-Chief, Prof. Holger Stark, and Wiley-VCH Verlag GmbH & Co. KGaA, Weinheim. The retraction has been agreed due to errors in the spectroscopic data of the investigated new compounds.

Reference To Retraction: S. Mukhtar, M. A. Alsharif, M. I. Alahmdi, H. Parveen, A. U. Khan, Arch. Pharm. Chem. Life Sci. 2018;1-12. DOI: 10.1002/ardp.201700397.
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http://dx.doi.org/10.1002/ardp.201700397DOI Listing
May 2018