Design, synthesis and biological evaluation of indole-2-carboxylic acid derivatives as novel HIV-1 integrase strand transfer inhibitors

Zhang, Rong-Hong; Chen, Guo-Qi; Wang, Weilin; Wang, Yu-Chan; Zhang, Wen-Li; Chen, Ting; Xiong, Qian-Qian; Zhao, Yong-Long; Liao, Shang-Gao; Li, Yong-Jun; Yan, Guo-Yi; Zhou, Meng

doi:10.1039/d3ra08320a

RSC Adv.

2024

DOI: 10.1039/d3ra08320a

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Design, synthesis and biological evaluation of indole-2-carboxylic acid derivatives as novel HIV-1 integrase strand transfer inhibitors

Rong-Hong Zhang,

Guo-Qi Chen,

Weilin Wang

et al.

Abstract: Integrase plays an important role in the life cycle of HIV-1, and indole-2-carboxylic acid derivative 17a can effectively inhibit the strand transfer of integrase.

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A mini-review on integrase inhibitors: The cornerstone of next-generation HIV treatment

Shalbi,

Ali

2024

European Journal of Medicinal Chemistry

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A mini-review on integrase inhibitors: The cornerstone of next-generation HIV treatment

Shalbi,

Ali

2024

European Journal of Medicinal Chemistry

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Discovery of a potent anticancer agent against pancreatic ductal adenocarcinoma targeting FAK with DFG-out state and JAK/Aurora kinases

Zhang,

Chen,

Xiong

et al. 2025

European Journal of Medicinal Chemistry

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Indole Derivatives: A Versatile Scaffold in Modern Drug Discovery—An Updated Review on Their Multifaceted Therapeutic Applications (2020–2024)

Mo,

Rao,

Kaur

et al. 2024

Molecules

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Indole derivatives have become an important class of compounds in medicinal chemistry, recognized for their wide-ranging biological activities and therapeutic potential. This review provides a comprehensive overview of recent advances in the evaluation of indole-based compounds in the last five years, highlighting their roles in cancer treatment, infectious disease management, anti-inflammatory therapies, metabolic disorder interventions, and neurodegenerative disease management. Indole derivatives have shown significant efficacy in targeting diverse biological pathways, making them valuable scaffolds in designing new drugs. Notably, these compounds have demonstrated the ability to combat drug-resistant cancer cells and pathogens, a significant breakthrough in the field, and offer promising therapeutic options for chronic diseases such as diabetes and hypertension. By summarizing recent key findings and exploring the underlying biological mechanisms, this review underscores the potential of indole derivatives in addressing major healthcare challenges, thereby instilling hope and optimism in the field of modern medicine.

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Design, synthesis and biological evaluation of indole-2-carboxylic acid derivatives as novel HIV-1 integrase strand transfer inhibitors

Abstract: Integrase plays an important role in the life cycle of HIV-1, and indole-2-carboxylic acid derivative 17a can effectively inhibit the strand transfer of integrase.

Cited by 3 publications

References 50 publications

A mini-review on integrase inhibitors: The cornerstone of next-generation HIV treatment

A mini-review on integrase inhibitors: The cornerstone of next-generation HIV treatment

Discovery of a potent anticancer agent against pancreatic ductal adenocarcinoma targeting FAK with DFG-out state and JAK/Aurora kinases

Indole Derivatives: A Versatile Scaffold in Modern Drug Discovery—An Updated Review on Their Multifaceted Therapeutic Applications (2020–2024)

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