Multicomponent synthesis of stereogenic-at-boron fluorophores (BOSPYR) from boronic acids, salicylaldehydes, and 2-formylpyrrole hydrazones.

This work describes one-step syntheses of various stereogenic-at-boron fluorochromes (BOSPYR) multicomponent reactions involving readily accessible boronic acids, salicylaldehydes, and 2-formylpyrrole hydrazones. The dyes absorb and emit in the visible region of the electromagnetic radiation, and are characterized by large Stokes shifts (2850-4930 cm) with weak fluorescence emissions (: 1.5-9.

Synthesis and photooxygenation of 3-(-substituted phenyl)-3a,8a-dihydro--cyclohepta[d]isoxazoles: facial selectivity.

Two 3-(-substituted phenyl)-3a,8a-dihydro-4-cyclohepta[d]isoxazoles were synthesized by 1,3-dipolar cycloaddition of the corresponding nitrile oxides with cycloheptatriene. Two endoperoxides were synthesized as facially selective and single products in high yields (93%-95%) from the reactions of isoxazole derivatives with singlet oxygen. The exact configurations of the endoperoxide with a methyl group in the phenyl ring and the diol synthesized from it were confirmed by X-ray analysis.

Comparison of Physicochemical Properties, Antioxidants, and Aroma Profiles of Water- and Sodium-Hydroxide-Treated Natural Cocoa Powder.

Cocoa powder alkalization is an essential process in chocolate manufacturing, and traditionally, this process involves the use of alkaline agents, such as sodium hydroxide (NaOH), potassium hydroxide (KOH), and potassium carbonate (KCO). However, these methods involve harsh chemicals and energy-intensive procedures, raising significant environmental concerns. Water (HO) has emerged as a promising alternative due to its safety, minimally harmful byproducts, and accessibility.

Unusual Rearrangements in Cyclohex-3-ene-1-carboxamide Derivatives: Pathway to Bicyclic Lactones.

The synthesis of new bicyclic lactone derivatives was carried out starting from 2-methyl/phenyl-3,4,7,7-tetrahydro-1-isoindole-1,3(2)-dione. 6-(Hydroxymethyl)--methyl/phenylcyclohex-3-ene-1-carboxamide derivatives were obtained from the reduction of tetrahydro-1-isoindole-1,3(2)-diones with NaBH. Bromination and epoxidation reactions of both compounds were examined, and the structures of the resulting products were determined by spectroscopic methods.

Lu-PSMA-617 Radioligand Treatment in Elderly Patients with Metastatic Castration-resistant Prostate Cancer: Therapeutic Efficacy and Safety Assessment.

Objective: This study aimed to evaluate the therapeutic efficacy and safety of Lutetium-Prostate Specific Membrane Antigen (Lu-PSMA-617) radioligand treatment (RLT) in metastatic castration-resistant prostate cancer (mCRPC) patients with aged older than 75 years.

Methods: A total of 37 patients with mCRPC aged older than 75 years treated with Lu- PSMA-617 were included in this study. Pre-therapy and post-therapy biochemical, metabolic, and clinical response results and Hb, TLC, platelet, serum creatinine and bilirubin levels were checked to evaluate the therapeutic efficacy and toxicity profile.

Bromination and conversion of tetrahydro-1H-indene to bisoxirane with a new approach: synthesis, structural characterization by spectroscopic and theoretical methods, and biological analysis supported by DFT and docking.

In this study, a new method for synthesizing diepoxides is proposed. Tetrahydroindene was brominated with NBS in the presence of LiClO and acetic acid, resulting in the formation of dibromodiacetate derivatives and . Treatment of compounds and with NaOH in methanol produced a mixture of diepoxides and .

Ga-FAPI PET/CT as an Alternative to F-FDG PET/CT in the Imaging of Invasive Lobular Breast Carcinoma.

Accurate staging of invasive lobular carcinoma (ILC), a subtype of breast cancer, is vital for effective clinical management. Although F-FDG PET/CT is a commonly used tool, its efficacy varies across different histologic subtypes. To mitigate this challenge, our investigation delves into the potential utility of Ga-fibroblast activation protein inhibitor (FAPI) PET/CT as an alternative for staging ILC, aiming to address a significant research gap using a more expansive patient cohort than the smaller samples commonly found in the existing literature.

The synthesis, carbonic anhydrase and acetylcholinesterase inhibition effects of sulfonyl chloride moiety containing oxazolidinones using an intramolecular aza-Michael addition.

Oxazolidinones are used as various potent antibiotics, in organisms it acts as a protein synthesis inhibitor, focusing on an initial stage that encompasses the tRNA binding process. Novel intramolecular aza-Michael reactions devoid of metal catalysts have been introduced in an oxazolidone synthesis pathway, different from α,β-unsaturated ketones. Oxazolidinone derivatives were tested against acetylcholinesterase (AChE), carbonic anhydrase I and II (hCA I and hCA II) enzymes.

Lutetium-177-PSMA-617 radioligand therapy in patients with high volume metastatic prostate cancer prior to chemotherapy and new generation androgen deprivation therapy: Clinical Experience.

Objective: We aimed to evaluate the efficacy oflutetium-177-prostate-specific membrane antigen-617 (Lu-PSMA-617) with the luteinizing hormone releasing hormone (LHRH) analogues in the first or in the second-line setting formetastatic castration sensitive patients and metastatic castration resistance after progression with LHRH analogues.

Subjects And Methods: Sixteen consecutive patients with high volume metastatic prostate cancer undergone Lu-PSMA-617 therapy who were refused chemotherapy and were unable to use new generation anti-androgen drugs because of unavailibility of reimbursement, were included in this retrospective study. Prostate specific antigen (PSA) response (>50% decrease), disease control rate (DCR: complete or partial response), progression-free survival (PFS) and overall survival (OS) were calculated to evaluate according to the clinicopathological features of the patients.

Comparison of Ga-FAPI-04 and F-FDG PET/CT for diagnosis of metastatic lesions in patients with recurrent papillary thyroid carcinoma.

Objective: We aimed to evaluate the gallium-68-labeled fibroblast-activation protein inhibitor (Ga-FAPI) positron emission tomography/computed tomography (PET/CT) in localizing papillary thyroid carcinoma (PTC) foci in patients with biochemical relapse. Papillary thyroid carcinoma has achieved biochemical recovery after appropriate treatment and had biochemical relapse in the last follow-up were included in this retrospective study. Gallium-68-FAPI and fluorine-18-fluorodeoxyglucose (F-FDG) PET/CT were performed to detect recurrence foci.

Stereoselective synthesis of novel bis-homoinositols with bicyclo[4.2.0]octane motifs.

Starting from cyclooctatetraene, bis-homoconduritols with cis-inositol and allo-inositol (or bicyclo[4.2.0]octane motif) structures were synthesized.

A boron dipyrromethene chiral at boron and carbon with a bent geometry: synthesis, resolution and chiroptical properties.

We report a boron dipyrromethene that is chiral at boron and carbon (B*C*-BODIPY) and accessible through a two-pot, one-step synthesis-an interrupted Knoevenagel condensation. The electronic circular dichroism spectra of chiral high performance liquid chromatography-resolved enantiomers show clear Cotton effects (∣∣ ∼ 2.0 × 10) in the visible region, suggesting efficient chirality induction to the otherwise achiral BODIPY.

Comparison of Ga-FAPI PET/CT and FDG PET/CT Modalities in Gastrointestinal System Malignancies with Peritoneal Involvement.

Purpose: In this study, we aimed to investigate the utilization of Ga-FAPI PET/CT in comparison to FDG PET/CT to evaluate the peritoneal involvement of the gastrointestinal malignancies alongside primary lesions and other metastatic foci.

Procedures: A total of 37 patients with various gastrointestinal malignancies with accompanying peritoneal involvement who underwent Ga-FAPI PET/CT and FDG PET/CT imaging between September 2020 and June 2021 were included in this retrospective study. SUV values of Ga-FAPI and FDG were compared according to lesion locations.

Comparison of [68Ga]-FAPI PET/CT and [18F]-FDG PET/CT in Multiple Myeloma: Clinical Experience.

Objective: In this study, we aimed to compare [68Ga]FAPI PET/CT and [18F]FDG PET/CT imaging to detect lesions in multiple myeloma.

Methods: A total of 14 patients with multiple myeloma who underwent [68Ga]FAPI PET/CT and [18F]FDG PET/CT imaging were included in this retrospective study. SUV values of [68Ga]FAPI and [18F]FDG were compared according to lesion locations.

Lu-PSMA-617 RLT in mCRPC: A single center experience, the earlier could be the better.

Introduction: Radioligand therapy which targets the prostate specific membrane antigen (PSMA) has recently considered as option in the treatment of metastatic castration resistant prostate cancer (mCRPC). The aim of this study was to evaluate the biochemical, clinical and radiological data of patients received treatment with Lu-PSMA-617 RLT in our clinic following the diagnosis of mCRPC, and to investigate the relationship between treatment timing and metastasis region and survival.

Material And Methods: This is a retrospective, observational, single-center study from December 2016 to December 2019.

Superiority of Ga-FAPI PET/CT scan in detecting additional lesions compared to FDG PET/CT scan in breast cancer.

Purpose: We compared the ability of Ga-FAPI PET//CT with FDG PET/CT imaging techniques to detect additional lesions in breast cancer patients that may affect further chemotherapy options.

Methods: A total of 48 patients with breast cancer underwent concurrent Ga-FAPI-04 and FDG PET/CT regardless of whether they had received chemotherapy or not in the last month before imaging. Both modalities were compared according to various parameters: clinical/pathological features, number of lesions detected, activity uptake (SUV), and the effect on the evaluation of response to treatment in the post-chemotherapy group.

Comparison of Ga-DOTA-FAPI and FDG PET/CT imaging modalities in the detection of liver metastases in patients with gastrointestinal system cancer.

Purpose: We aimed to compare the diagnostic performance of PET/CT imaging performed with Ga-DOTA-FAPI and FDG in detection of liver metastases in patients with gastrointestinal system (GIS) cancer.

Methods: A total of 31 patients who underwent Ga-DOTA-FAPI and F-FDG PET/CT examinations and diagnosed with GIS cancer (15 colorectal, 9 pancreas, 4 stomach and 3 other cancers) were included in the study. The presence of liver metastasis was decided based on histopathologic diagnosis, PET/CT, other radiologic examinations or tumor biomarker findings, and both PET/CT imaging findings were compared on the patient and lesion basis.

The role of tumour biomarkers in choosing the appropriate positron emission tomography imaging in follow-up of medullary thyroid cancer.

Introduction: We aimed to demonstrate the importance of serum calcitonin (Ct) and carcinoembryonic-antigen (CEA) levels in the selection of appropriate positron emission tomography/computed tomography (PET/CT) modality in the follow-up of operated patients with medullary thyroid cancer.

Methods: Fourteen operated patients (8 Female, 6 Male) with MTC underwent PET/CT imaging with somatostatin ( Ga-DOTATATE) and glucose ( FDG) analogs due to elevated Ct or CEA at follow-up. Ct and CEA levels and both PET/CT findings were compared based on both patients and lesions.

Synthesis and antioxidant activities of phenol derivatives from 1,6-bis(dimethoxyphenyl)hexane-1,6-dione.

Starting from the compound (3,4-dimethoxyphenyl)(2-(3,4-dimethoxyphenyl)cyclopent-1-en-1-yl)methanone (4), two diols and three tetrol derivatives were synthesised. Morover, from the reactions of 1,3-dimethoxybenzene and 1,4-dimethoxybenzene with adipoyl chloride, fifteen new along with nine known compounds were obtained. For the characterizations of compounds, spectroscopic methods such as NMR including DEPT, COSY, HMQC and HMBC experiments and X-ray diffraction were used.

Efficacy of positron emission tomography and computed tomography in clinical staging of cutaneous malignant melanoma.

Accurate staging is very important for determining the prognosis and appropriate treatment for malignant melanoma (MM). The aim of this study is to determine the effectiveness of positron emission tomography and computed tomography (PET/CT) imaging in staging MM. Patients diagnosed with MM who then underwent PET/CT metastasis before treatment were assessed retrospectively.

Synthesis and biological evaluation of new chloro/acetoxy substituted isoindole analogues as new tyrosine kinase inhibitors.

We have developed a versatile synthetic approach for the synthesis of new isoindole derivatives via the cleavage of ethers from tricyclic imide skeleton compounds. An exo-cycloadduct prepared from the Diels-Alder reaction of furan and maleic anhydride furnished imide derivatives. The epoxide ring was opened with AcO or AcO/AcCl in the presence of a catalytic amount of HSO in order to yield new isoindole derivatives 8a-d and 9a-d.

Synthesis, biological evaluation and in silico modelling studies of 1,3,5-trisubstituted pyrazoles carrying benzenesulfonamide as potential anticancer agents and selective cancer-associated hCA IX isoenzyme inhibitors.

Inhibition of carbonic anhydrases (CAs, EC 4.2.1.

Synthesis and biological evaluation of bromophenol derivatives with cyclopropyl moiety: Ring opening of cyclopropane with monoester.

Trans-(1R*,2R*,3R*)-Ethyl 2-(3,4-dimethoxyphenyl)-3-methylcyclopropane-1-carboxylate (6) and its cis isomer 7 were obtained from the reaction of the methyl isoeugenol (5) with ethyl diazoacetate. The reduction and bromination reactions of the ester 6 and 7 together with the hydrolysis of all esters were carried out. Opening ring of cyclopropane was observed in the reaction of 7 with bromine.

An anomalous addition of chlorosulfonyl isocyanate to a carbonyl group: the synthesis of ((3a,7a,)-2-ethyl-3-oxo-2,3,3a,4,7,7a-hexahydro-1-isoindol-1-ylidene)sulfamoyl chloride.

In this study, we developed a new addition reaction of chlorosulfonyl isocyanate (CSI), starting from 2-ethyl-3a,4,7,7a-tetrahydro-1-isoindole-1,3(2)-dione. The addition reaction of CSI with 2-ethyl-3a,4,7,7a-tetrahydro-1-isoindole-1,3(2)-dione resulted in the formation of ylidenesulfamoyl chloride, whose exact configuration was determined by X-ray crystal analysis. We explain the mechanism of product formation supported by theoretical calculations.

Transferring the protective effect of remote ischemic preconditioning on skin flap among rats by blood serum.

The aim of this study was to show whether the protective effect of remote ischemic preconditioning (RIPC) on flaps can be transferred among different individuals with the transfusion of blood serum. Blood serum was taken from rats without any procedure (Group x), rats 1 hour (Group y) and 24 hours (Group z) after performing RIPC and the remaining rats were divided into six groups. While the random pattern skin flap was performed only in the back region in Group 1, and it was performed 1 hour (Group 2) and 24 hours (Group 3) after induction RIPC.