Fluorine in medicinal chemistry: A review of anti-cancer agents

Isanbor, Chukwuemeka; O’Hagan, David

doi:10.1016/j.jfluchem.2006.01.011

Cited by 1,032 publications

(359 citation statements)

References 153 publications

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“…Currently, many fluorinated compounds are synthesised routinely in pharmaceutical research and are widely used in the treatment of diseases. These include: anti-cancer agents [2], antidepressants, antiinflammatory agents, anaesthetics and central nervous system drugs [3], and a number of review articles on different therapeutic classes of fluorine-containing agents have been published in recent years [2 -6].…”

Section: Introductionmentioning

confidence: 99%

The role of fluorine in medicinal chemistry

Shah

Westwell

2007

Journal of Enzyme Inhibition and Medicinal Chemistry

614

392

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The small and highly electronegative fluorine atom can play a remarkable role in medicinal chemistry. Selective installation of fluorine into a therapeutic or diagnostic small molecule candidate can enhance a number of pharmacokinetic and physicochemical properties such as improved metabolic stability and enhanced membrane permeation. Increased binding affinity of fluorinated drug candidates to target protein has also been documented in a number of cases. A further emerging application of the fluorine atom is the use of 18 F as a radiolabel tracer atom in the exquisitely sensitive technique of Positron Emission Tomography (PET) imaging. This short review aims to bring together these various aspects of the use of fluorine in medicinal chemistry applications, citing selected examples from across a variety of therapeutic and diagnostic settings. The increasingly routine incorporation of fluorine atom(s) into drug candidates suggests a bright future for fluorine in drug discovery and development. A major challenge moving forward will be how and where to install fluorine in a rational sense to best optimise molecular properties.

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Section: Introductionmentioning

confidence: 99%

The role of fluorine in medicinal chemistry

Shah

Westwell

2007

Journal of Enzyme Inhibition and Medicinal Chemistry

614

392

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“…[2][3][4][5][6] Consequently, fluorine-containing drugs are now prevalent within the life science industries and a considerable number of blockbuster pharmaceuticals and agrochemicals now contain at least one fluorine atom. [7][8][9] In particular, fluorinated azaheterocycles are very important subunits within life science products and a growing number of pharmaceuticals that contain fluoroheteroaromatic motifs such as Voriconazole (antifungal, Pfizer), Capecitabine (anticancer, Roche) and Diclosulam (herbicide, Dow) have now reached the commercial market [10][11][12] with many others in clinical trials such as Abemaciclib (anticancer, Eli Lilly), Riociguat (heart failure, Bayer) and Verubecestat (Alzheimers, Merck).…”

Section: Introductionmentioning

confidence: 99%

Fluorination of pyrrole derivatives by Selectfluor™

Heeran

Sandford

2016

Tetrahedron

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“…[1][2][3][4] In general, fluoroalkylsubstituted 2-aminothiazoles are regarded as privileged structure motifs in medicinal chemistry due to its presence in antimicrobial or antiviral agents, anticancer agents, etc. (Figure 1).…”

Section: Introductionmentioning

confidence: 99%

A One-Pot Domino Synthesis of 5-(Trifluoromethyl)-2-thiazolamine

Bao¹,

Qiao²,

Hou³

et al. 2016

Journal of the Brazilian Chemical Society

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5-(Trifluoromethyl)-2-thiazolamine is a key intermediate for manufacturing numerous pharmaceuticals and chemicals. Here, a low-cost, one-pot multicomponent domino synthetic route has been reported for the synthesis of 5-(trifluoromethyl)-2-thiazolamine, which was successfully prepared from 3-bromo-1,1,1-trifluoro-2-propanone, phosphorus pentasulfide and cyanamide in the presence of sodium carbonate with the yield of 56%.

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Fluorine in medicinal chemistry: A review of anti-cancer agents

Cited by 1,032 publications

References 153 publications

The role of fluorine in medicinal chemistry

The role of fluorine in medicinal chemistry

Fluorination of pyrrole derivatives by Selectfluor™

A One-Pot Domino Synthesis of 5-(Trifluoromethyl)-2-thiazolamine

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