The human mitotic kinesin Eg5 represents a novel mitotic spindle target for cancer chemotherapy. We previously identified S-trityl-l-cysteine (STLC) and related analogues as selective potent inhibitors of Eg5. We herein report on the development of a series of 4,4,4-triphenylbutan-1-amine inhibitors derived from the STLC scaffold. This new generation systematically improves on potency: the most...

For the first time we have been able to employ enantiopure 1,2-amino alcohols derived from abundant amino acids in C−C bond-forming hydrogen-borrowing alkylation reactions. These reactions are facilitated by use of aryl ketone Ph*COMe. Racemisation amine stereocentre during can be prevented sub-stoichiometric base and protection nitrogen with a sterically hindered triphenylmethane (trityl) or b...

The title compound, C(44)H(35)NS, is a derivative of amino-thio-phenol and possesses a protected S-triphenyl-methyl thio-ether and an N-triphenyl-methyl-amine functional group. The trityl groups show an anti orientation, with C-C-N-C and C-C-S-C torsion angles of -151.0 (3) and -105.3 (2)°, respectively. There is an intra-molecular N-H⋯S hydrogen bond.

Dynamical decoupling sequences detect spin system and solvent-induced decoherence contributions for nitroxides, trityl radicals gadolinium complexes in glassy water–glycerol.

We previously reported that the garlic-derived compound S-allylmercaptocysteine (SAMC) causes growth inhibition, mitotic arrest, and induction of apoptosis in SW480 human colon cancer cells by inducing microtubule depolymerization and c-Jun NH(2) terminus kinase-1 activation. In the present study, we compared the aforementioned effects of SAMC to those of a series of garlic-derived and other or...

In the last decade, carbohydrates have attracted great attention as renewable resources for the chemical industry. Carbohydrates are abundantly found in nature in the form of monomers, oligomers and polymers, or as components of biopolymers and other naturally occurring substances. As natural products, they play important roles in conferring certain physical, chemical, and biological properties...

Kinesin spindle protein (KSP), known as Hs Eg5, a member of the kinesin-5 family, plays an important role in the formation and maintenance of the bipolar spindle. We previously reported S-trityl-l-cysteine derivatives as selective KSP inhibitors. Here, we report further optimizations using docking modeling in the L5 allosteric binding site, which led to the discovery of several high affinity de...

Quartet states, generated after photoexcitation of chromophore–radical dyads, are promising for applications in quantum sensing. We demonstrate the potential trityl radicals improving their coherence properties and spectral addressability.