Synthesis and serotonin transporter activity of 1,3-bis(aryl)-2-nitro-1-propenes as a new class of anticancer agents.

Structural derivatives of 4-MTA, an illegal amphetamine analogue have been previously shown to have anticancer effects in vitro. In this study we report the synthesis of a series of novel 1,3-bis(aryl)-2-nitro-1-propene derivatives related in structure to 4-MTA. A number of these compounds containing a classic nitrostyrene structure are shown to have antiproliferative activities in vitro in a range of malignant cell lines, particularly against Burkitt's lymphoma derived cell lines, whilst having no effect on 'normal' peripheral blood mononuclear cells. Such effects appear to be independent of the serotonin transporter, a high affinity target for amphetamines and independent of protein tyrosine phosphatases and tubulin dynamics both of which have been previously associated with nitrostyrene-induced cell death. We demonstrate that a number of these compounds induce caspase activation, PARP cleavage, chromatin condensation and membrane blebbing in a Burkitt's lymphoma derived cell line, consistent with these compounds inducing apoptosis in vitro. Although no specific target has yet been identified for the action of these compounds, the cell death elicited is potent, selective and worthy of further investigation.

Description of the final instar larva of Acrogomphus jubilaris Lieftinck, 1964 (Odonata, Gomphidae), with information on the distribution of Acrogomphus in Borneo.

The final instar larva of Acrogomphus jubilaris Lieftinck, 1964, is described and figured for the first time based on exuviae from four male and one female larvae collected in Sarawak, Malaysian Borneo. The adults of A. jubilaris are very rarely encountered. The larvae, however, are surprisingly common in forest streams in Borneo. It is compared with A. malayanus Laidlaw, 1925 and A. walshae Lieftinck, 1935, and notes on behavior, distribution and habitat are included. A map including all known records of A. jubilaris is provided.

Description of the final instar larva of Orthetrum borneense Kimmins, 1936 (Odonata, Libellulidae), using rearing and molecular methods.

The final instar larva of Orthetrum borneense Kimmins, 1936, is described and figured for the first time based on exuviae from three male and six female larvae collected in Sarawak, Borneo (East Malaysia). It is compared with an early instar larva, which was matched to the adult O. borneense by DNA barcoding, and the known larvae of other species of this genus that occur in the region.

Synthesis and serotonin transporter activity of sulphur-substituted alpha-alkyl phenethylamines as a new class of anticancer agents.

The discovery that some serotonin reuptake transporter (SERT) ligands have the potential to act as pro-apoptotic agents in the treatment of cancer adds greatly to their diverse pharmacological application. 4-Methylthioamphetamine (MTA) is a selective ligand for SERT over other monoamine transporters. In this study, a novel library of structurally diverse 4-MTA analogues were synthesised with or without N-alkyl and/or C-alpha methyl or ethyl groups so that their potential SERT-dependent antiproliferative activity could be assessed. Many of the compounds displayed SERT-binding activity as well as cytotoxic activity. While there was no direct correlation between these two effects, a number of derivatives displayed anti-tumour effects in lymphoma, leukaemia and breast cancer cell lines, showing further potential to be developed as possible chemotherapeutic agents.