
Bioorganic and Medicinal Chemistry Letters p. 5086 - 5090 (2013)
Update date:2022-08-03
Topics:
Patel, Pradeepkumar
Hanawa, Emi
Yadav, Reeta
Samuni, Uri
Marzabadi, Cecilia
Sabatino, David
The synthesis and characterization of a new class of DNA binding molecule exhibiting potent and selective anti-leukemic activity is described. The synthesis of an aminoacyl nucleolipid was developed from an efficient EEDQ coupling strategy, in which a series of seven bioconjugates were synthesized in yields of 53-78%. Guanosine bioconjugate 7, was used as building block for the synthesis of a target aminoacyl nucleolipid 14. Its GRP78 DNA binding affinity was confirmed by gel shift assay, CD spectroscopy, Tm measurements and dynamic light scattering experiments. Moreover, in a single dose (10 μM) screen against a panel of 60 cancer cell lines, aminoacyl nucleolipid 14 was found to selectively trigger greater than 90% cell death in a SR human leukemia cancer cell line. The reported aminoacyl nucleolipid represents a useful model for a new class of DNA binding molecules for the development of potent and selective anti-cancer agents.
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Doi:10.1134/S1070428013080125
()Doi:10.1021/ol4021207
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(2013)