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2 results on '"Bagul, C."'

1. Topical advances in PIM kinases and their inhibitors: Medicinal chemistry perspectives.

Author

Walhekar V, Bagul C, Kumar D, Muthal A, Achaiah G, and Kulkarni R

Subjects
Chemistry, Pharmaceutical, Humans, Male, Protein Kinase Inhibitors pharmacology, Protein Kinase Inhibitors therapeutic use, Proto-Oncogene Proteins c-pim-1 chemistry, Antineoplastic Agents chemistry, Antineoplastic Agents pharmacology, Antineoplastic Agents therapeutic use, Neoplasms drug therapy
Abstract

Cytosolic PIM kinases are the members of serine/ threonine family play a crucial role in the cancer progression and development. Overexpression of PIM kinases is observed in various types of cancers including prostate, hematological, pancreatic, breast carcinoma and likewise. PIM kinases have now been considered as limelight target for the discovery of new molecules as novel anticancer agents as no drug is in the market targeting PIM kinases. In the last two decades, numerous PIM kinase inhibitors have been developed and few of them were in clinical trial phases but could not pass the pipeline of the clinical trials. The present comprehensive review intends to cover biological and the structural aspects of PIM kinases and also medicinal chemistry of PIM inhibitors developed in recent years., (Copyright © 2022 Elsevier B.V. All rights reserved.)

Published
2022
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2. Synthesis and biological evaluation of imidazopyridinyl-1,3,4-oxadiazole conjugates as apoptosis inducers and topoisomerase IIα inhibitors.

Author

Subba Rao AV, Vishnu Vardhan MV, Subba Reddy NV, Srinivasa Reddy T, Shaik SP, Bagul C, and Kamal A

Subjects
Antigens, Neoplasm metabolism, Antineoplastic Agents chemical synthesis, Antineoplastic Agents chemistry, Cell Line, Tumor, Cell Proliferation drug effects, DNA Topoisomerases, Type II metabolism, DNA-Binding Proteins metabolism, Dose-Response Relationship, Drug, Drug Screening Assays, Antitumor, Humans, Models, Molecular, Molecular Structure, Oxadiazoles chemical synthesis, Oxadiazoles chemistry, Pyridines chemical synthesis, Pyridines chemistry, Structure-Activity Relationship, Topoisomerase II Inhibitors chemical synthesis, Topoisomerase II Inhibitors chemistry, Antineoplastic Agents pharmacology, Apoptosis drug effects, DNA-Binding Proteins antagonists & inhibitors, Oxadiazoles pharmacology, Pyridines pharmacology, Topoisomerase II Inhibitors pharmacology
Abstract

A series of imidazopyridinyl-1,3,4-oxadiazole conjugates were synthesized and investigated for their cytotoxic activity and some compounds showed promising cytotoxic activity. Compound 8q (NSC: 763639) exhibited notable growth inhibition that satisfies threshold criteria at single dose (10μM) on all human cancer cell lines. This compound was further evaluated at five dose levels (0.01, 0.1, 1, 10 and 100μM) to obtain GI 50 values ranging from 1.30 to 5.64μM. Flow cytometric analysis revealed that compound 8q arrests the A549 cells in sub G1 phase followed by induction of apoptosis which was further confirmed by Annexin-V-FITC, Hoechst nuclear staining, caspase 3 activation, measurement of mitochondrial membrane potential and ROS generation. Topo II mediated DNA relaxation assay results showed that conjugate 8q could significantly inhibit the activity of topo II. Moreover, molecular docking studies also indicated binding to the topoisomerase enzyme (PDBID 1ZXN)., (Copyright © 2016 Elsevier Inc. All rights reserved.)

Published
2016
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