AIMS AND OBJECTIVES A one-pot synthesis of 2,3-dihydroquinazolin-4(1H)-one derivatives by threecomponent cyclo-condensation of isatoic anhydride, aldehydes and amine or ammonium acetate has been developed using 3,5-Bis(trifluoromethyl) phenylammonium triflate (BFPAT) as a new organocatalyst. MATERIALS AND METHODS All of the obtained products are known compounds and identified by IR, 1HNMR, 13CNMR and melting points. RESULTS A wide variety of structurally different aldehydes reacted easily and rapidly to result in the relating 2,3-dihydroquinazolin-4(1H)-ones in good to excellent yield. CONCLUSION We have demonstrated an extremely effective and new process for synthesizing 2,3- dihydroquinazolin-4(1H)-ones employing BFPAT as a novel organocatalyst in one-pot fashion. Copyright© Bentham Science Publishers; For any queries, please email at epub@benthamscience.net.BACKGROUND Quinoxaline 1,4-dioxides have a broad range of biological activity that causes a growing interest in their derivatives for drug discovery. Recent studies demonstrated that quinoxaline 1,4- dioxides have a promising anticancer activity and good hypoxia-selectivity. OBJECTIVE The preparation, isolation, structure characterization, and screening for anticancer activity of the first representatives of 6-substituted quinoxaline-2-carbonitrile 1,4-dioxides have been described. MATERIALS AND METHODS A series of 7- and 6-halogeno-3-phenylquinoxaline-2-carbonitrile 1,4-dioxides was synthesized by the Beirut reaction. The cytotoxicity was assessed by MTT test (72 h incubation) in normoxia (21% O2) and hypoxia (1% O2) conditions. RESULTS We found that during the Beirut reaction between a benzofuroxan bearing an electron withdrawing group and benzoylacetonitrile in the presence of triethylamine, in addition to well-known 7-substituted quinoxaline-2-carbonitrile 1,4-dioxides 7-11a, the 6-isomers 7-11b are formed. Moreover, the yield of the 6- isomers increased with the increase in the electron-withdrawing character of the substituent. For benzofuroxans with CO2Me and CF3 groups, 6-substituted quinoxaline-2-carbonitrile 1,4-dioxides 10-11b were the major products. Despite similarities in physicochemical and spectroscopic properties, the obtained isomers exhibit considerable differences in their anticancer activity and hypoxia selectivity. CONCLUSION Substituents and their electronic effects play a key role in the formation of 7- and 6-substituted quinoxaline-2-carbonitrile 1,4-dioxides in the Beirut reaction and in the cytotoxicity properties of the obtained isomers. Copyright© Bentham Science Publishers; For any queries, please email at epub@benthamscience.net.BACKGROUND AND OBJECTIVE The objective of our work was to establish a facile and scalable synthesis of imidazopyridone for further use in medicinal chemistry applications. NSC 13128 An easy synthesis of a core scaffold will enable the medicinal chemistry community to use imidazopyridone as a privileged scaffold in new chemical entity (NCE) synthesis. MATERIALS AND METHODS The synthesis was achieved from commercially available and cheap raw materials like amino acetonitrile hydrochloride or commercially available guanidine. RESULTS Simple transformation starting from amino acetonitrile hydrochloride leads to the synthesis of a versatile imidazo [1, 5-a] pyrimidine-2-(1H)-one core structure. Using suitable functionalized starting materials, a set of NCEs were synthesized to demonstrate the application of the developed synthetic scheme. Similarly, guanidine was also used to synthesize a regioisomer of imidazopyridone in moderate to good yields. CONCLUSION We demonstrate the synthesis of two different regio-isomers of imidazopyrimidinone using simple chemical transformations. Its application in synthesizing NCEs has also been exhibited in the present work. Copyright© Bentham Science Publishers; For any queries, please email at epub@benthamscience.net.BACKGROUND Onychine is a 4-azafluorenone alkaloid isolated from the Annonaceae family, in low concentrations. Onychine and its analogs exhibit a wide range of pharmacological activities such as antifungal, antibacterial, anticancer, and antimalarial. Because of the high bioactivity of some 4-azafluorenone derivatives, several synthetic methods have been developed for their procurement. OBJECTIVE Considering the importance of these alkaloids, we aim to present the main synthetic approaches to onychines and its derivatives and the biological activity of some 4-azafluorenones. METHODS The most prominent methodologies for the synthesis of onychines were reviewed. RESULTS In this work, we cover many synthetic approaches for the synthesis of onychine and 4-azafluorenone derivatives including intramolecular cyclizations, multicomponent reactions, microwave-assisted multicomponent reactions, Diels-alder reactions, among others. link2 Moreover, we also review the biological activity of 4-azafluorenones. CONCLUSION 4-azafluorenones have risen as prominent structures in medicinal chemistry; however, most of the time, access to new derivatives involves toxic catalysts, harsh reaction conditions, and long-step procedures. Therefore, the development of new synthetic routes with more operational simplicity, simple purification procedure, good yields, and low environmental impact, is desirable. Copyright© Bentham Science Publishers; For any queries, please email at epub@benthamscience.net.Aim We investigated publication rates and reported results for gene- and cell-based therapy trials. Materials & methods In a cohort of Institutional Review Board (IRB)-authorized trials during 2007-2017 in the Netherlands (n = 105), we examine publication rates and reported results in scientific papers and conference abstracts as well as associations with the occurrence of trial characteristics. Results The publication rate for scientific papers was 27% and 17% for conference abstracts (median survival time 1050 days). Academic hospitals published more in scientific papers whereas private sponsors published more in conference abstracts. Manufacturing protocols were underreported compared with clinical outcomes. Most publications reported positive results (78%). Conclusion Publication rates are currently suboptimal indicating a need for enhanced knowledge sharing to stimulate gene- and cell-based therapy development.Recent advancements in tissue engineering suggest that biomaterials, such as decellularized extracellular matrix (ECM), could serve to potentiate the localization and efficacy of regenerative therapies in the central nervous system. Still, what factors and which mechanisms are required from these ECM-based biomaterials to exert their effect is not entirely understood. In this study we use the brain as a novel model to test the effects of particular biochemical and structural properties by evaluating, for the first time, three different sections of the brain (i.e., cortex, cerebellum and remaining areas) side-by-side and their corresponding decellularized counterparts using mechanical (4-day) and chemical (1-day) decellularization protocols. The three different brain subregions had considerably different initial conditions in terms of cell number and growth factor content, and some of these differences were maintained after decellularization. Decellularized ECM from both protocols was used as a substrate or as soluble factor, in both cases showing good cell attachment and growth capabilities. Interestingly, the 1-day protocol was capable of promoting greater differentiation than the 4-day protocol, probably due to its capacity to remove a similar amount of cell nuclei while better conserving the biochemical and structural components of the cerebral ECM. Still, some limitations of this study include the need to evaluate the response in other biologically relevant cell types, as well as a more detailed characterization of the components in the decellularized ECM of the different brain subregions. In conclusion, our results show differences in neuronal maturation depending on the region of the brain used to produce the scaffolds. Complex organs like the brain have sub-regions with very different initial cellular and biochemical conditions that should be considered for decellularization to minimize exposure to immunogenic components, while retaining bioactive factors conducive to regeneration.Cell microencapsulation is a rapidly expanding field with broad potential for stem cell therapies and tissue engineering research. Traditional alginate microspheres suffer from poor biocompatibility, and microencapsulation of more advanced hydrogels is challenging due to their slower gelation rates. We have developed a novel, non-cytotoxic, non-emulsion based method to produce hydrogel microspheres compatible with a wide variety of materials, called Core-Shell Spherification (CSS). Fabrication of microspheres via CSS derived from two slow-hardening hydrogels hyaluronic acid (HA) and polyethylene glycol diacrylate (PEGDA) were characterized. HA microspheres were manufactured with two different crosslinking methods thiolation and methacrylation. Microspheres of methacrylated HA (MeHA) had the greatest swelling ratio, the largest average diameter and the lowest diffusion barrier. In contrast, PEGDA microspheres had the smallest diameters, the lowest swelling ratio and the highest diffusion barrier, while microspheres of thiolated HA (ThHA) had characteristics that were in between the other two groups. To test the ability of the hydrogels to protect cells while promoting function, diabetic NOD mice received intraperitoneal injections of PEGDA or MeHA microencapsulated canine islets. PEGDA microspheres reversed diabetes for the length of the study (up to 16 weeks). In contrast, islets encapsulated in MeHA microspheres at the same dose restored normoglycemia, but only transiently (3-4 weeks). link3 Non-encapsulated canine islet transplanted at the same dose did not restore normoglycemia for any length of time. In conclusion, CSS provides a non-toxic microencapsulation procedure compatible with various hydrogel types.BACKGROUND Endobronchial ultrasound-guided transbronchial needle aspiration (EBUS-TBNA) is a widely used, safe, and accurate technique for obtaining pathological specimens to be used in the diagnosis of diseases involving lung hilar and mediastinal lymph node (LN) enlargement. However, application of the suction technique during EBUS-TBNA remains controversial. In addition, the effectiveness of the slow-pull capillary technique for the diagnosis of pancreatic masses was recently reported. The aim of this study was to compare the diagnostic accuracy of EBUS-TBNA using these two techniques. METHODS The accuracy, sensitivity, specificity, negative predictive value (NPV), positive predictive value (PPV), and availability of tissue cores of the suction and slow-pull capillary techniques were studied retrospectively in patients who underwent EBUS-TBNA for the diagnosis of diseases involving lung hilar and mediastinal LN enlargement. RESULTS A total of 97 patients with hilar and mediastinal LN enlargement underwent acquisition of tissue core. The reviews of this paper are available via the supplemental material section.BACKGROUND Myelitis accompanied by a negative spinal cord MRI may lead to diagnostic uncertainty. OBJECTIVE AND METHODS We retrospectively investigated the frequency of negative spinal cord MRI (performed less then 6 weeks from onset) in Mayo Clinic patients with myelin oligodendrocyte glycoprotein (MOG)-IgG-associated myelitis (2000-2019). RESULTS The initial spinal cord MRI was negative in 7/73 (10%) patients, despite severe acute disability (median EDSS, 7 (range, 4.5-8)); myelitis symptoms/signs were frequent (paraparesis, neurogenic bladder, sensory level, Lhermitte’s phenomenon). Myelitis lesions became overt at follow-up MRI in three patients. CONCLUSIONS A negative spinal cord MRI should not dissuade from MOG-IgG testing in patients with acute/subacute myelitis.