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

Andrew Nortcliffe, Ian N. Fleming, Nigel P. Botting, David O'Hagan

Research output: Contribution to journal › Article

2 Citations (Scopus)

Abstract

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
Original languageEnglish
Pages (from-to)8343-8347
Number of pages5
JournalTetrahedron
Volume70
Issue number44
Early online date6 Sep 2014
DOIs
Publication statusPublished - 4 Nov 2014

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Functional groups
Nitric Oxide
Integrins
MCF-7 Cells
Cytotoxicity
Aspartic Acid
Glycine
Arginine
Assays
Prostatic Neoplasms
Cells
Cell Line
Pharmaceutical Preparations
abiraterone
arginyl-glycyl-aspartic acid

Keywords

  • anticancer
  • RGD peptide
  • nitric oxide
  • abiraterone

Cite this

Synthesis and anticancer properties of RGD peptides conjugated to nitric oxide releasing functional groups and abiraterone. / Nortcliffe, Andrew; Fleming, Ian N.; Botting, Nigel P.; O'Hagan, David.

In: Tetrahedron, Vol. 70, No. 44, 04.11.2014, p. 8343-8347.

Research output: Contribution to journal › Article

Nortcliffe, A, Fleming, IN, Botting, NP & O'Hagan, D 2014, 'Synthesis and anticancer properties of RGD peptides conjugated to nitric oxide releasing functional groups and abiraterone', Tetrahedron, vol. 70, no. 44, pp. 8343-8347. https://doi.org/10.1016/j.tet.2014.09.004
Nortcliffe A, Fleming IN, Botting NP, O'Hagan D. Synthesis and anticancer properties of RGD peptides conjugated to nitric oxide releasing functional groups and abiraterone. Tetrahedron. 2014 Nov 4;70(44):8343-8347. https://doi.org/10.1016/j.tet.2014.09.004
Nortcliffe, Andrew ; Fleming, Ian N. ; Botting, Nigel P. ; O'Hagan, David. / Synthesis and anticancer properties of RGD peptides conjugated to nitric oxide releasing functional groups and abiraterone. In: Tetrahedron. 2014 ; Vol. 70, No. 44. pp. 8343-8347.
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