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ANANBIOANAL - 2010
Pharmaceutical R & D Summit
doi:10.4172/2155-9872.1000059
Lead Molecules for Molecular Medicine and Omic Studies
S. V. Eswaran
St. Stephen’s College (University of Delhi), Delhi, India
I
n this paper, new compounds synthesised during the last three and a half decades
will be presented. These molecules have become intertwined with omic studies
and could serve as leads for molecular medicine. Six such compound classes will
be discussed here.
• Methoxyisoxazole quinones prepared have been shown to be potent
radiosensitisers in vitro for human cancer / tumour cells, which had stopped taking
up further radiation.
• New nitrophenyl azides prepared have been shown to exhibit inhibitory activity
against Crotalaria juncea (Jute) and E. coli. In the former, these showed ‘2, 4-D’
like activity. The corresponding amines were used to synthesise biologically
interesting 9-Aryl-9H-Purine-6-amines. This work has been cited in a recent
patent.
• 5, 6- Dimethoxybenzofuroxan, which exists in two rapidly equilibrating degenerate
forms has been shown to possess antifungal activity against Candida albicans
and other fungi. Based on this benzofuroxan, a new indoloquinoxaline dioxide has
been synthesised which could show antibacterial activity.
• A short synthesis of Pyrroloquinoline quinone, P. Q. Q. (Methoxatin) has been
developed. This compound is considered to be a new vitamin to prevent heart
attacks and strokes.
• New homo and hetero bifunctional crosslinkers have been developed. Similar
reagents could be designed based on P.Q.Q., which will be employed for
proteomics. Cholesterol /steroid photolabels are also being prepared for lipidomics.
• Dehydrodivanillin, a natural product has been used to prepare antifungal 1, 2,
3-triazoles using the Click reaction.
In vivo and in vitro studies are being undertaken for all the above compounds to
unravel the underlying biological mechanisms. This has a great potential in the area
of omic studies and for developing better diagnostic tools for molecular medicine.
ANALBIOANAL-2010
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