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Khalid Mohammed Khan

Publications and source records attributed to Khalid Mohammed Khan.

2 recordsLinked to original sources

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.

q-bio.BM↗

Free Radical Scavenging and Cytotoxic Activities of Substituted Pyrimidines

A library of substituted pyrimidines was synthesized and evaluated for free radical scavenging, and in vitro cytotoxic activity in 3T3 cells. All compounds showed good free radical scavenging activity with IC50 values in the range of 42.9 + 0.31 to 438.3 3.3 μM as compared to the standard butylated hydroxytoluene having IC50 value of 128.83 2. 1 μM. The structure activity-relationship was also established. Selected analogues 1, 2, 3, 5, 6, 7, 8, 9, 10, 12, 13, 15, 19, 20, 21, 24, 25, 26 and 28 were tested for cytotoxicity in mouse fibroblast 3T3 cell line using MTT assay, and most of the analogues showed cytotoxicity. This study has identified a number of cytotoxic novel substituted pyrimidines having free radical scavenging activities that can be used as inhibitory compounds for those cancer cells whose growth is mediated by reactive oxygen species.

q-bio.BM↗