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Aim Our study aims to investigate the safety and effectiveness of sentinel lymph node biopsy using indocyanine green (ICG) for the surgical staging of early-stage endometrial cancer in comparison to technetium-99 m use. Methods We conducted an observational retrospective study with patients diagnosed of endometrial cancer and FIGO stages I-II. All participants were injected technetium-99m the day prior to the surgery and underwent lymphoscintigraphy along with single-photon emission computed tomography. In addition, all patients were administered intraoperatively ICG injection to detect sentinel lymph node biopsy. The surgical staging was then completed according to the European Society for Medical Oncology preoperative risk category. Data obtained from the analysis of technetium-99m detection was compared to ICG detection. Results A total of 53 women with endometrial cancer were included in the study, 49 (92.5%) of them showed drainage preoperatively in the single-photon emission computed tomography and/or lymphoscintigraphy. The intraoperative bilateral detection rate for technetium-99 m was 26 (49.1%) patients compared to 40 (75.5%) patients with ICG (p = 0.013). We observed a 42.5% increase in the mean number of lymph nodes retrieved by ICG compared to technetium-99m (2.85 vs 2,0 nodes; p = 0.002). We intraoperatively identified 164 lymph nodes, 104 (63.4%) located in both obturator areas and external iliac vessels. Conclusion The use of ICG for the performance of sentinel node biopsy in patients with endometrial cancer seems safe and could be superior to technetium-99 m, since it offers a higher bilateral detection rate and nodal retrieval, resulting in the possibility to perform safely less full staging lymphadenectomies.

Focused microwave irradiation of equimolecular mixtures of 9-chloroacridines, 4-chloroquinolines and 4-chloroquinazolines with amines in the presence of 2 equiv of phenol allows the general, fast and high-yielding synthesis of aminated heterocycles, with a very broad scope in terms of amine structure (aromatic, linear primary aliphatic, α-branched primary aliphatic, secondary aliphatic and diamines). Workup consisted of a simple washing with water and purification could be achieved by crystallization, avoiding the use of organic solvents in extraction and chromatographic purification steps. This protocol provides a solution to the long-standing synthetic problem of achieving a practical and efficient method for the amination of pi-deficient nitrogen heterocycles for medicinal chemistry applications.

Reinvestigation of the title natural product's structure (1) has shown the easy racemization of the Trp-stereocenter in some derivatives of cyclo-L-Trp-Gly. The here described synthesis of compound 2, a regioisomer of 1 with the N-methyl group on the nitrogen adjacent to the ethylidene side-chain, permits us to conclude that structure 1 was correct.

The enzymatic activity of α-chymotrypsin chemically modified with monomethoxypolyethylene glycol (α-CT-PEG) is discussed using as test reactions the hydrolysis of esters different from the natural substrates of the enzyme, and the peptidic synthesis. These reactions allowed the analysis of the dimensions of “ar”, “h”, “n” and “am” subsites of α-CT-PEG. Using 2-aminoethanol esters and derivatives of glycine we have proved that the depth of the “n” subsite of the chemically modified α-CT (α-CT-PEG) must be lower than 14.455 A because the synthesis of peptides is not observed using 2-aminoethanol octanoate as nucleophile. α-CT-PEG is chemoselective towards the aromatic esters because unnatural aliphatic esters are not hydrolyzed in the presence of N-benzoyl-L-Tyrosine ethyl ester. Unnatural aliphatic acyl-donors with a distance H-C……C=O smaller than 8.8 A are recognized by the chemically modified enzyme as acyl-donors. From these results we can conclude that the presence of N-acyl group in the acyl-donor molecule is not necessary to be recognised by α-CT-PEG. The presence of bulky alkyl chain both in the acyl donor and in the nucleophile, reduces the enzymatic activity of the biocatalyst both in the hydrolysis of esters and in the synthesis of peptides.

The reaction generates a C—C double bond in a very efficient manner with only AcOH as the side product.

Focused microwave irradiation promoted the very effi- cient synthesis of 2-styrylquinolines by reaction between quinaldi- nes and benzaldehydes or cinnamaldehydes in the presence of acetic anhydride.

Condensation of N1-methyl-cyclo-Trp-Gly and aldehydes in basic media was studied to confirm the structure of the natural product TDD (N-methyl-Tryptophan Dehydrobutyrine Diketopiperazine, 1) and to prepare analogues with potential activity as GST (Glutathione-S-Transferase) inhibitors. This strategy was successful for 1,4-diacetyl-cyclo-Trp-Gly but it did not work for N4-acetyl, N1-methyl-cyclo-Trp-Gly derivatives. Pyrolytic cyclization of N- Boc- l -Thr -N- methyl- l -Trp methyl ester gave the Z-isomer of N-methyltryptophan dehydrobutyrine diketopiperazine, which was previously supposed to be the natural product. However, by comparison of melting points and pectroscopic data with those of 1, we conclude that the proposed structure for TDD must be corrected.

An efficient and reproducible synthetic method is proposed for the preparation of 2-nitro-3,6-dimethoxybenzaldehyde.

An efficient method is proposed for the preparation of 3-substituted carbostyrilquinone derivatives, based on Friedlander synthesis of the 5,8-dialkoxyquinolines followed by cerium ammonium nitrate oxidative demethylation