arXiv subjects

M. Iqbal Choudhary

Publications and source records attributed to M. Iqbal Choudhary.

4 recordsLinked to original sources

arXiv2023

Estimation of In-Vitro Free Radical Scavenging and Cytotoxic Activities of Thiocarbohydrazones Derivatives

Objective: To investigate free radical scavenging potential of thiocarbohydrazones derivatives for the discovery of antioxidant compounds of synthetic origin. Method: Eighteen thiocarbohydrazones derivatives were screened for antioxidant activities by using in vitro radical inhibition assay. Cytotoxicity all derivatives were evaluated using invitro cytotoxicity assay on mouse fibroblast cell line. Results: various compounds of the have shown significant radical scavenging activities as compared with the standard drug butylated hydroxytoluene. In addition in an in vitro cell cytotoxicity assay selected analogues were found to be non-cytotoxic against fibroblast 3T3 cell line. Conclusion: Taken together, these findings all compound this series could be further evaluated in in vivo model of oxidative stress to develop as a therapeutic agent against oxidative stress related disorders due to exhibiting excellent free radical scavenging properties and having their non cytotoxic nature against normal cells.

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arXiv2023

Benzophenone Semicarbazones as Potential alpha-glucosidase and Prolyl Endopeptidase Inhibitor: In-vitro free radical scavenging, enzyme inhibition, mechanistic, and molecular docking studies

$α$-glucosidase and prolylendopeptidase has altered expression and activity patterns in neurological disease, type 2diabetes respectively and several cancers. Here we screened a series 1-29 benzophenone semicarbazone derivatives for in vitro free radical scavenging, alpha-glucosidase and prolylendopeptidase inhibition activities. Seven derivatives were identified as potential free radical scavengers, 14 as alpha-glucosidase, and 9 as prolylendopeptidase inhibitors. Kinetic studies on the most promising inhibitors were performed. Compounds 23, 27, 25 and 28 were found as inhibitor of alpha-glucosidase, while compound 26 inhibited both prolylendopeptidase and alpha-glucosidase. The binding modes and binding free energy of the multi targeted inhibitor 26 were predicted by molecular docking studies. These results provide insights on prolylendopeptidase and alpha-glucosidase inhibition of compound 26 for further development as therapeutic agents for neoplastic, neurological, and endocrine disorders.

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arXiv2020

A Novel Bis-Coumarin Targets Multiple Tyrosine Kinases of Key Signaling Pathways in Melanoma and Inhibits Melanoma Cell Survival, Proliferation, and Migration

Melanoma is one of the most dangerous skin malignancies due to its high metastatic tendency and high mortality. Activation of key signaling pathways enforcing melanoma progression depends on phosphorylation of tyrosine kinases, and oxidative stress. We here investigated the effect of the new bis-coumarin derivative (3,5-DCPBC) on human melanoma cell survival, growth, proliferation, migration, and intracellular redox state, and deciphered associated signal pathways. This novel derivative was found to be toxic for melanoma cells, and non-toxic for their benign counterparts, melanocytes and fibroblasts. 3,5-DCPBC inhibited cell survival, migration and proliferation of different metastatic, and non-metastatic melanoma cell lines through the profound suppression of phosphorylation of the Epidermal Growth Factor receptor, and related downstream pathways. Suppression of phosphorylation of key downstream transcription factors and different tyrosine kinases comprise JAK/STAT, SRC kinases, ERK and MAP kinases (p38alpha), all involved in melanoma progression. Simultaneous and specific targeting of multiple tyrosine kinases and corresponding key genes in melanoma cells makes 3,5-DCPBC a highly interesting anti-melanoma, and anti-metastatic drug candidate which may in the long term hold promise in the therapy of advanced melanoma.

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arXiv2020

Emerging classes of antioxidant to cancer therapy: a review of clinical and experimental studies

This review mainly focuses on the relation between antioxidants with cancer therapy. Antioxidants have been reported to play an essential role to reduce free radical species. Free radicals commonly cause oxidative damage which is a common factor in the aging process, and also the vital factor of formation, and development of major disease specially cancer. Although, since last many decades several antioxidants belong to natural and synthetic origin have been tested in clinical trials against oxidative stress, however these clinical trials end up with undesirable effects. This review also complied with the most recent findings of oxidative stress, highlighting of free racial production, and its related oxidative damage at cellular and molecular level, with the new and existing natural and synthetic classes of free radical scavenger and their related clinical trials.

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