Evolution of 3-(4-hydroxyphenyl)indoline-2-one as a scaffold for potent and selective anticancer activity

Boudreau, Matthew W.; Hergenrother, Paul J.

doi:10.1039/d2md00110a

RSC Med. Chem.

2022

DOI: 10.1039/d2md00110a

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Evolution of 3-(4-hydroxyphenyl)indoline-2-one as a scaffold for potent and selective anticancer activity

Matthew W. Boudreau

Paul J. Hergenrother

Abstract: Development of targeted anticancer modalities has prompted a new era in cancer treatment that is notably different from the age of radical surgery and highly toxic chemotherapy. Behind each effective...

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2024

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Cited by 2 publications

References 115 publications

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Recent drug design strategies and identification of key heterocyclic scaffolds for promising anticancer targets

Mushtaq,

Wu,

Naseer

2024

Pharmacology & Therapeutics

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Recent drug design strategies and identification of key heterocyclic scaffolds for promising anticancer targets

Mushtaq,

Wu,

Naseer

2024

Pharmacology & Therapeutics

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Identification of 3-((4-Hydroxyphenyl)amino)propanoic Acid Derivatives as Anticancer Candidates with Promising Antioxidant Properties

Kavaliauskas,

Grybaitė,

Sapijanskaite-Banevič

et al. 2024

Molecules

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Various cancer-associated morbidities remain a growing global health challenge, resulting in a significant burden on healthcare systems worldwide due to high mortality rates and a frequent lack of novel therapeutic options for advanced and localized disease. Reactive oxygen species (ROS) play an important role in cancer pathogenesis and response to chemotherapeutics; therefore, it is crucial to develop novel compounds with both antioxidant and anticancer activity. In this study, a series of previously reported 3-((4-hydroxyphenyl)amino)propanoic acid derivatives (compounds 1–36) were evaluated for their anticancer and antioxidant activities. Compounds 12, 20–22, and 29 were able to reduce A549 cell viability by 50% and suppress A549 cell migration in vitro. These compounds also showed favorable cytotoxicity properties towards noncancerous Vero cells. The most promising candidate, compound 20, exhibited potent antioxidant properties in the DPPH radical scavenging assay. These results demonstrate that 3-((4-hydroxyphenyl)amino)propanoic acid could be further explored as an attractive scaffold for the development of novel anticancer and antioxidant candidates.

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Evolution of 3-(4-hydroxyphenyl)indoline-2-one as a scaffold for potent and selective anticancer activity

Abstract: Development of targeted anticancer modalities has prompted a new era in cancer treatment that is notably different from the age of radical surgery and highly toxic chemotherapy. Behind each effective...

Cited by 2 publications

References 115 publications

Recent drug design strategies and identification of key heterocyclic scaffolds for promising anticancer targets

Recent drug design strategies and identification of key heterocyclic scaffolds for promising anticancer targets

Identification of 3-((4-Hydroxyphenyl)amino)propanoic Acid Derivatives as Anticancer Candidates with Promising Antioxidant Properties

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