An update on late-stage functionalization in today’s drug discovery

Montgomery, Andrew P.; Joyce, Jack M; Danon, Jonathan J.; Kassiou, Michael

doi:10.1080/17460441.2023.2205635

Cited by 9 publications

(4 citation statements)

References 92 publications

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“…Given that the late-stage transformation of natural product or drug is a significant way for drug discovery 19 as well as encouraged by the good functional group compatibility of this protocol, the decarboxylation [2 + 2 + 2] annulation with 3-iodochromone 7 derived from estrone was further probed under the standard conditions, delivering the nonacyclic estrone derivative 8 in 53% yield (Scheme 4).…”

Section: Resultsmentioning

confidence: 99%

Palladium-catalyzed decarboxylation [2 + 2 + 2] annulation approach to chromone-containing polycyclic compounds

et al. 2023

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Section: Resultsmentioning

confidence: 99%

Palladium-catalyzed decarboxylation [2 + 2 + 2] annulation approach to chromone-containing polycyclic compounds

et al. 2023

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“…Beyond machine learning and artificial intelligence methods, quantum computing is another significant advance in technology in generative chemistry and drug discovery processes, which researchers may exploit in the case of amygdalin [ 90 ]. Late-stage functionalization also presents novel challenges for the introduction of new chemical moiety groups, such as amygdalin and its future potential synthetic analogues, toward the end of a synthetic sequence, which means that new molecules that could be rapidly accessed without laborious de novo chemical synthesis [ 91 ]. This specific approach may offer benefits such as efficient access to diverse libraries to explore structure–activity relationships and the improvement of physicochemical and pharmacokinetic properties [ 91 ].…”

Section: Discussionmentioning

confidence: 99%

Amygdalin as a Promising Anticancer Agent: Molecular Mechanisms and Future Perspectives for the Development of New Nanoformulations for Its Delivery

Spanoudaki,

Stoumpou,

Papadopoulou

et al. 2023

IJMS

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Cancer rates are increasing, and cancer is one of the main causes of death worldwide. Amygdalin, also known as vitamin B17 (and laetrile, a synthetic compound), is a cyanogenic glycoside compound that is mainly found in the kernels and pulps of fruits. This compound has been proposed for decades as a promising naturally occurring substance which may provide anticancer effects. This is a comprehensive review which critically summarizes and scrutinizes the available studies exploring the anticancer effect of amygdalin, highlighting its potential anticancer molecular mechanisms as well as the need for a nontoxic formulation of this substance. In-depth research was performed using the most accurate scientific databases, e.g., PubMed, Cochrane, Embase, Medline, Scopus, and Web of Science, applying effective, characteristic, and relevant keywords. There are several pieces of evidence to support the idea that amygdalin can exert anticancer effects against lung, breast, prostate, colorectal, cervical, and gastrointestinal cancers. Amygdalin has been reported to induce apoptosis of cancer cells, inhibiting cancer cells’ proliferation and slowing down tumor metastatic spread. However, only a few studies have been performed in in vivo animal models, while clinical studies remain even more scarce. The current evidence cannot support a recommendation of the use of nutritional supplements with amygdalin due to its cyano-moiety which exerts adverse side effects. Preliminary data have shown that the use of nanoparticles may be a promising alternative to enhance the anticancer effects of amygdalin while simultaneously reducing its adverse side effects. Amygdalin seems to be a promising naturally occurring agent against cancer disease development and progression. However, there is a strong demand for in vivo animal studies as well as human clinical studies to explore the potential prevention and/or treatment efficiency of amygdalin against cancer. Moreover, amygdalin could be used as a lead compound by effectively applying recent developments in drug discovery processes.

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“…Functional group tolerance and mild conditions allows access to new molecules not easily accessible by conventional approaches without the need for laborious de novo chemical synthesis. Number of literature reports suggest that the late-stage derivatization/transformation is an attractive approach for the facile synthesis of complex molecules like natural product analogs, immuniosuppressive drug and drug metabolites [ 34 – 37 ]. In view of the above discussion, the present work comprises development of a facile synthesis and characterization of a unique secondary metabolite of fenofibrate.…”

Section: Introductionmentioning

confidence: 99%

A facile synthesis of 2-(4-((4-chlorophenyl)(hydroxy)methyl) phenoxy)-2-methylpropanoic acid: Metabolite of anti-hyperlipidemic drug Fenofibrate

Majethia,

Haq,

Balendiran

2024

Results in Chemistry

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An update on late-stage functionalization in today’s drug discovery

Cited by 9 publications

References 92 publications

Palladium-catalyzed decarboxylation [2 + 2 + 2] annulation approach to chromone-containing polycyclic compounds

Palladium-catalyzed decarboxylation [2 + 2 + 2] annulation approach to chromone-containing polycyclic compounds

Amygdalin as a Promising Anticancer Agent: Molecular Mechanisms and Future Perspectives for the Development of New Nanoformulations for Its Delivery

A facile synthesis of 2-(4-((4-chlorophenyl)(hydroxy)methyl) phenoxy)-2-methylpropanoic acid: Metabolite of anti-hyperlipidemic drug Fenofibrate

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