mr-molecular-imaging-prostate-cancer-with-small-molecular-clt1

MR Molecular Imaging of Prostate Cancer with a Small Molecular CLT1 Peptide Targeted Contrast Agent

Tumor extracellular  matrix has abundance of cancer related proteins that can be used as biomarkers  for cancer molecular imaging. In this work,  we ...

Case Western Reserve University 

A series of novel 2-arylphenyl ether-3-(1H-1,2,4-triazol-1-yl)propan-2-ol derivatives were designed and synthesized as candidate fungicides. The new compounds were identified by (1)H NMR spectroscopy and element analysis. Their antifungal activities were evaluated. They exhibited excellent antifungal activities against five common pathogens in comparison with the commercial fungicides tebuconazole and difenoconazole. The antifungal activities of three new triazole alcohol compounds were compared with those of tebuconazole and difenoconazole at a concentration of 1 mug/mL.

Synthesis and fungicidal evaluation of 2-arylphenyl ether-3-(1H-1,2,4-triazol-1-yl)propan-2-ol derivatives.

In the crystal structure of the title compound, C(8)H(5)N(3)O(3), inter-molecular N-Hâ‹¯O hydrogen bonds link mol-ecules into centrosymmetric dimers. These dimers are, in turn, linked though weak inter-molecular C-Hâ‹¯O and C-Hâ‹¯N hydrogen bonds and Ï€-Ï€ stacking inter-actions, with centroid-centroid distances of 3.678â€…(3)â€…Ã…, into a three-dimensional network.

7-Nitro-quinazolin-4(3H)-one.

The crystal packing of the title compound, C(11)H(13)NO(3)S, exhibits weak inter-molecular C-Hâ‹¯O hydrogen bonding, which links mol-ecules related by translation along the b axis into chains, and Ï€-Ï€ inter-actions [centroid-centroid distance of 3.778â€…(2)â€…Ã… between benzene rings].

2-n-Butyl-1,2-benzisothia-zol-3(2H)-one 1,1-dioxide.

Tumor extracellular matrix has an abundance of cancer related proteins that can be used as biomarkers for cancer molecular imaging. Innovative design and development of safe and effective targeted contrast agents to these biomarkers would allow effective MR cancer molecular imaging with high spatial resolution. In this study, we synthesized a low molecular weight CLT1 peptide targeted Gd(III) chelate CLT1-dL-(Gd-DOTA)(4) specific to clotted plasma proteins in tumor stroma for cancer MR molecular imaging. CLT1-dL-(Gd-DOTA)(4) was synthesized by conjugating four Gd-DOTA monoamide chelates to a CLT1 peptide via generation 1 lysine dendrimer. The T(1) relaxivity of CLT1-dL-(Gd-DOTA)(4) was 40.4 mM(-1) s(-1) per molecule (10.1 mM(-1) s(-1) per Gd) at 37 Â°C and 1.5 T. Fluorescence imaging showed high binding specificity of CLT1 to orthotopic PC3 prostate tumor in mice. The contrast agent resulted in improved tumor contrast enhancement in male athymic nude mice bearing orthotopic PC3 prostate tumor xenograft at a dose of 0.03 mmol Gd/kg. The peptide targeted MRI contrast agent is promising for high-resolution MR molecular imaging of prostate tumor.

Article	Year
Synthesis and fungicidal evaluation of 2-arylphenyl ether-3-(1H-1,2,4-triazol-1-yl)propan-2-ol derivatives. Journal of agricultural and food chemistry\| PubMed ID: 19422214	2009
7-Nitro-quinazolin-4(3H)-one. Acta crystallographica. Section E, Structure reports online\| PubMed ID: 21201454	2008
2-n-Butyl-1,2-benzisothia-zol-3(2H)-one 1,1-dioxide. Acta crystallographica. Section E, Structure reports online\| PubMed ID: 21202296	2008
Synthesis and evaluation of a peptide targeted small molecular Gd-DOTA monoamide conjugate for MR molecular imaging of prostate cancer. Bioconjugate chemistry\| PubMed ID: 22812444	2012

Guan-Ping Yu

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