Oxaphosphinanes: New Therapeutic
Perspectives for
Glioblastoma
- Publication date
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Abstract
This paper reports the design and the synthesis of a
new family
of compounds, the phostines, belonging to the [1,2]oxaphosphinane
family. Twenty-six compounds have been screened for their antiproliferative
activity against a large panel of NCI cancer cell lines. Because of
its easy synthesis and low EC<sub>50</sub> value (500 nM against the
C6 rat glioma cell line), compound <b>3.1a</b> was selected
for further biological study. Moreover, the specific biological effect
of <b>3.1a</b> on the glioblastoma phylogenetic cluster from
the NCI is dependent on its stereochemistry. Within that cluster, <b>3.1a</b> has a higher antiproliferative activity than Temozolomide
and is more potent than paclitaxel for the SF295 and SNB75 cell lines.
In constrast with paclitaxel and vincristine, <b>3.1a</b> is
devoid of astrocyte toxicity. The original activity spectrum of <b>3.1a</b> on the NCI cancer cell line panel allows the development
of this family for use in association with existing drugs, opening
new therapeutic perspectives
