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 demonstrated effective MR cancer molecular imaging with a small molecular peptide targeted Gd-DOTA monoamide complex as a targeted MRI contrast agent specific to clotted plasma proteins in tumor stroma. We performed the experiment of evaluating the effectiveness of the agent for non-invasive detection of prostate tumor with MRI in a mouse orthotopic PC-3 prostate cancer model. The targeted contrast agent was effective to produce significant tumor contrast enhancement at a low dose of 0.03 mmol Gd/kg. The peptide targeted MRI contrast agent is promising for MR molecular imaging of prostate tumor.

Synthesis and evaluation of a peptide targeted small molecular Gd-DOTA monoamide conjugate for MR molecular imaging of prostate cancer.

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 °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.

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

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.

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

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

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

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