Abstract
Isatin-based derivatives are important organic molecules that use isatin (1H-indole-2,3-dione) as a backbone/scaffold; manipulation of key groups on the isatin backbone allows for synthesis of a wide range of derivatives of different classes which possess varied biological effects. These compounds have been found to act as ligands/antagonists of key receptors which regulate cancer signal transduction and metabolism in different cancer types. During thorough literature survey, we stumbled upon potent anticancer isatin derivatives of different kinds. These compounds have been synthesized, purified, characterized (using a range of biophysical techniques), and explored for prospective anticancer activity with the aid of in silico, in vitro, and in vivo methodologies. This chapter presents some of the representative anticancer isatin derivatives with potent anticancer activities. Since isatin is a naturally occurring compound in both plants and animals, utilization of this backbone for substitution reactions yields diverse pharmacophores with low toxicity and higher affinity for key cancer target receptors. Hence, these molecules may be safer for human chemotherapeutic interventions when compared to some routinely used anticancer chemotherapeutic agents which are organometallic complexes like cisplatin. A review of isatin-based derivatives is presented, and an attempt is made to encapsulate the rich structural and functional diversities of a few biologically active (and particularly, anticancer and redox active) isatin derivatives which may have potential to clear clinical trials and develop into standard chemotherapeutic agents.
Abbreviations
- Akt:
-
Serine/Threonine protein kinase (Protein Kinase B)
- BAX:
-
BCL-2 Associated X Apoptosis Receptor
- BCL-2:
-
B-cell Lymphoma 2
- CDK 1/CDK2:
-
Cyclin-Dependent Kinase 1 or 2
- CLK:
-
CDC2-Like Kinase
- EGFR:
-
Epidermal Growth Factor Receptor
- EPR:
-
Electron Paramagnetic Resonance
- ERB:
-
Estrogen Receptor Beta
- FITC:
-
Fluorescein isothiocyanate
- FTIR:
-
Fourier Transform Infrared Spectroscopy
- GSK3β:
-
Glycogen Synthase Kinase3
- HGF:
-
Hepatocyte growth factor
- HRMS:
-
High-Resolution Mass Spectroscopy
- IBD:
-
Isatin-Based derivatives
- JAK/STAT:
-
Janus Kinase/Signal Transducer and Activity of Transcription
- JNK3:
-
c- Jun NH2 Terminal Kinase
- MAPK:
-
Mitogen-Activated Protein Kinase
- MDR:
-
Multiple Drug Resistance
- mTOR:
-
Mechanistic Target of Rapamycin
- OxPhos:
-
Oxidative Phosphorylation
- PDGFR:
-
Platelet-Derived Growth Factor Receptor
- PI3K:
-
Phosphoinositide 3-Kinase
- QSAR:
-
Quantitative Structure Activity Relationship
- RCS:
-
Reactive Carbon Species
- RHS:
-
Reactive Halogen Species
- RNS:
-
Reactive Nitrogen Species
- ROS:
-
Reactive Oxygen Species
- RSS:
-
Reactive Sulphur Species
- RTK:
-
Receptor Tyrosine Kinase
- SRC:
-
Proto-Oncogene Tyrosine Protein Kinase
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Gideon, D.A., Annadurai, P., Nirusimhan, V., Parashar, A., James, J., Dhayabaran, V.V. (2022). Evaluation of the Anticancer Activities of Isatin-Based Derivatives. In: Chakraborti, S. (eds) Handbook of Oxidative Stress in Cancer: Therapeutic Aspects. Springer, Singapore. https://doi.org/10.1007/978-981-16-5422-0_51
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