Carbophilic 3‐Component Cascades: Access to Complex Bioactive Cyclopropyl Diindolylmethanes

Naturally occurring indole‐3‐carbinol and 3,3‐diindolylmethane show bioactivity in a number of disparate disease areas, including cancer, prompting substantial synthetic analogue activity. We describe a new approach to highly functionalised derivatives that starts from allene gas and proceeds via the combination of a three‐component Pd⁰‐catalysed cascade with a one‐pot, three‐component carbophilic Pt^II cascade linked to a stereoselective acid‐catalysed Mannich–Michael reaction that generates complex cyclopropyl diindolylmethanes which show selective activity against prostate cancer cell lines.     

New examples of Beauville surfaces

We find new mixed and unmixed Beauville structures for groups constructed as 2-quotients, i.e. quotients of 2-power order, of the fundamental group of a certain simplicial complex.     

Synthesis and anticancer properties of RGD peptides conjugated to nitric oxide releasing functional groups and abiraterone

A series of analogues of the integrin binding aspartic acid-glycine-arginine (RGD) peptide sequence were synthesised conjugated to nitric oxide (NO) donating functional groups. Also the cytotoxicity of abiraterone, a prostate cancer drug, was explored when it was conjugated in three part constructs to RGD sequences and NO releasing heterocycles. In general the analogues showed integrin binding affinity comparable to RGD reference compounds, and all released NO by the Griess test assay. Two analogues exhibited significant cytotoxic effects against PC3 and MCF7 cell lines.     

Enhanced coding for exponentially distributed signals using suprathreshold stochastic resonance

Our previous work on stochastic resonance (SR) in threshold based systems proved that the SR effect is dependent on the nature of the input signal distribution; more specifically, for certain types of signal distribution SR is not observed [Das A, Stocks NG, Nikitin A, Hines EL. Quantifying stochastic resonance in a single threshold detector for random aperiodic signals. Fluctuation Noise Lett 2004;4:L247–65]. Here we show that suprathreshold stochastic resonance (SSR) – a novel and distinct form of SR – removes this limitation and hence leads to the conclusion that SSR can probably enhance the transmission of signals of any distribution and amplitude. SSR effects are studied in a parallel array of identical nonlinear threshold based devices. A double exponential signal distribution is chosen because this distribution did not demonstrate conventional SR effects in a single threshold device [Das A, Stocks NG, Nikitin A., Hines EL. Quantifying Stochastic resonance in a single threshold detector for random aperiodic signals. Fluctuation and Noise Letters 2004;4:L247-L265.]. SSR as a possible mechanism for enhancing transmission of speech signals in the human ear is also discussed.