Author Archive

Review: Practical use of Minisci reactions

09 Sep 2011

In this MedChemComm review Matthew Duncton, Renovis Inc., highlights the attractive potential of Minisci reactions – addition of radicals to heteroaromatic bases – for medicinal and biological chemists.

These reactions can be used to introduce a broad-range of selective CH-functionalization groups, such as alkyls, cycloalkyls, sugars, esters and more. In many cases, these processes are highly chemo- and regio-selective, making them ideal for industrial applications, because complicating factors such as protecting group strategies can be avoided.

Graphical abstract: Minisci reactions: Versatile CH-functionalizations for medicinal chemists

Read this review now for specific examples and future developments of these useful reactions. It’s free to download for the next 4 weeks!

Minisci reactions: Versatile CH-functionalizations for medicinal chemists
Matthew A. J. Duncton, Med. Chem. Commun., 2011, DOI: 10.1039/C1MD00134E

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HOT Article: A step forward in the fight against cancer

01 Apr 2011

Novel water soluble bis(1,10-phenanthroline)octanedioate Cu2+ and Mn2+ complexes synthesised by researchers in Ireland and the US show extremely high cytotoxicity, encouraging cytoselectivity against cancer cells.

Mononuclear [Cu(phen)2(phthalate)] complexes have been shown to display excellent chemotherapeutic potential against colon, breast and prostate cancer lines, but their water solubility is poor making them difficult to deliver in the body. This inspired Andrew Kellett, Michael Devereux and colleagues to build upon the most active chemotherapeutic agents in this class of compounds and develop more potent water soluble versions.

Both complexes displayed greater in vivo drug tolerance compared to cisplatin, a commonly used chemotherapy drug, when examined using the insect Galleria mellonella.

Read more now in the MedChemComm article that is free to download!

Water-soluble bis(1,10-phenanthroline) octanedioate Cu2+ and Mn2+ complexes with unprecedented nano and picomolar in vitro cytotoxicity: promising leads for chemotherapeutic drug development
Andrew Kellett, Mark O’Connor, Malachy McCann, Orla Howe, Alan Casey, Pauraic McCarron, Kevin Kavanagh, Mary McNamara, Sean Kennedy, Donald D. May, Philip S. Skell, Denis O’Shea and Michael Devereux
Med. Chem. Commun., 2011, DOI: 10.1039/C0MD00266F

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New antibiotics repair faulty genes

19 Jan 2011

Many genetic diseases, such as cystic fibrosis and muscular dystrophy, are caused by DNA mutations that terminate protein synthesis in the mutant gene. Aminoglycoside based antibiotics have been shown to stop these mutations but are often toxic and cause unpleasant side-effects in patients.   

Now Timor Baasov and colleagues have designed and synthesised new aminoglycoside derivatives that show enhanced targeting and reduced cell toxicity, compared with the leading antibiotic gentamicin. Baasov’s compounds contain a chiral methyl group at the side-chain of the ribosamine ring, which they claim could be an essential feature responsible for the compound’s biological activity.

These findings could have immediate therapeutic applications for the treatment of many genetic diseases and could also aid treatment of several types of cancer caused by DNA mutations.

Download this paper for free now!

Repairing faulty genes by aminoglycosides: Identification of new pharacophore with enhanced suppression of disease-causing nonsense mutations.  
Jeyakumar Kandasamy, Dana Atia-Gilkin, Valery Belakhov and Timor Baasov 
Med.Chem. Commun, 2011, Advance Article, DOI: 10.1039/C0md00195c

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