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The clinical success of a compound is often curtailed because of inadequate safety, pharmacokinetics or efficacy. Human tissue can be used to identify the potential shortcomings of new drugs before they undergo testing in man. This review highlights the consent and ethical approval required for the use of human tissues and discusses their use for predicting human ADME and safety profiles of drugs in preclinical development. The ability to retrieve a wide range of viable tissues from human donors provides the opportunity to test drugs for many potential use-limiting side-effects.

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In this project, Ni(II) ion stabilized on zeolite-Y (NNZ) was developed as a high efficient nanoporous catalyst for the synthesis of 3-benzimidazolyl-1,3?thiazolidin-4-one derivatives via condensation of 2-aminobenzimidazole, aromatic aldehydes and thioglycolic acid in ethanol under ambient conditions. Compared with conventional protocols, this methodology has promising features such as the use of inexpensive, stable, recyclable and safe catalyst, shorter reaction times and higher yields, nontoxic solvent and easy isolation of the products.

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Benzothiazole (BTA) belongs to the heterocyclic class of bicyclic compounds. BTA derivatives possesses broad spectrum biological activities such as anticancer, antioxidant, anti-inflammatory, anti-tumour, antiviral, antibacterial, anti-proliferative, anti-diabetic, anti-convulsant, analgesic, anti-tubercular, antimalarial, anti-leishmanial, anti-histaminic and anti-fungal among others. The BTA scaffolds showed a crucial role in the inhibition of the metalloenzyme carbonic anhydrase (CA). In this review an extensive literature survey over the last decade discloses the role of BTA derivatives mainly as anticancer agents. Such compounds are effective against various types of cancer cell lines through a multitude of mechanisms, some of which are poorly studied or understood. The inhibition of tumour associated CAs by BTA derivatives is on the other hand better investigated and such compounds may serve as anticancer leads for the development of agents effective against hypoxic tumours.

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The present invention relates to a composition for maintaining the chromosomal stability of pluripotent stem cells, which contains a small-molecule compound, and more particularly, to a composition for maintaining the chromosomal stability of induced pluripotent stem cells, which contains a ROCK inhibitor, a MEK inhibitor, an ALK5 inhibitor or an antioxidant, which is capable of inhibiting chromosomal structural and numerical mutations or DNA damage during induction of induced pluripotent stem cell and the subsequent culture of the cells. The small-molecule compound-containing composition for maintaining the chromosomal stability of induced pluripotent stem cells increases the reprogramming rate and efficiency during production of induced pluripotent stem cells and exhibits excellent effects on the inhibition of chromosomal structural and numerical mutations or DNA damage. Thus, the composition of the present invention is very useful for the development of induced pluripotent stem cell therapeutic agents having excellent chromosomal stability.

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The organocatalytic cyclization of propargylic amines/amides with carbonyl sulfide (COS) was firstly achieved by employing COS adducts of Lewis base (LB) as organocatalysts, affording various functionalized 1,3-thiazolidine-2-ones, and 1,3-thiazolidine-2,4-diones derivatives in a highly chemo- and stereoselective manner. The isotope labeling and stoichiometric experiments suggested the LB-COS adducts preferentially mediated basic ionic pair mechanism. Furthermore, the practical application of this methodology was highlighted by the highly efficient synthesis of rosiglitazone using COS as sulfur source.

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Thiazolidinone is a biologically important five-membered heterocyclic ring having almost all types of biological activities. This review covers various types of thiazolidinones, such as 2-thiazolidinones, 4-thiazolidinones, 5-thiazolidinones, 2-thioxo-4-thiazolidinones, and thiazolidiene-2,4-dione. The literature related to the physical properties, chemical reactions, and synthesis for these derivatives has been included. Recent advances in the biological activities reported for 4-thiazolidinone derivatives, such as peroxisome proliferator-activated receptor gamma binders, follicle-stimulating hormone agonists, cystic fibrosis transmembrane conductance regulator inhibitors, and antioxidants, have been covered in this review. Thus, this study may help in further optimizing these thiazolidinone derivatives as more effective drug agents.

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Disclosed are prodrugs as follows:(I) a prodrug of the formula where A is a sulfur or a selenium, and R is a mono- di- or oligo-saccharide;(II) a prodrug of the formula where A is sulfur or selenium, R? is a sugar, or =O, and the R? groups are hydrogen, alkyl, alkoxy, carboxy;(III) a conjugate of an antioxidant vitamin and a thiolamine or selenolamine;(IV) a prodrug of the formula where A is sulfur or selenium, and R? is a sugar, or an alkyl or aryl group, or =O, and R? is an alkoxy, or an amine group;(V) a prodrug of the formula R is COOH or H, and R? is a sugar or =O.

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09/15/21 News Properties and Exciting Facts About 2682-49-7

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Cancer is the second leading cause of death worldwide. There is always a huge demand for novel anticancer drugs and diverse new natural or synthetic compounds are developed continuously by scientists. Presently, a large number of drugs in clinical practice have showed pervasive side effect and multidrug resistance. Sulfonyl or sulfonamide hybrids became one of the most attractive subjects due to their broad spectrum of pharmacological activities. Sulfonyl hybrids were broadly explored for their anticancer activities and it was found that they possess minimum side effect along with multi-drug resistance activity. This review describes the most recent applications of sulfonyl hybrid analogues in anticancer drug discovery and further discusses the mechanistic insights, structure-activity relationships and molecular docking studies for the potent derivatives.

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In the modern scenario, the quinolone scaffold has emerged as a very potent motif considering its clinical significance. Quinolones possess wide range of pharmacological activities such as anticancer, antibacterial, antifungal, antiprotozoal, antiviral, anti-inflammatory, carbonic anhydrase inhibitory and diuretic activity etc. The versatile synthetic approaches have been successfully applied and several of the resulted synthesized compounds exhibit fascinating biological activities in numerous fields. This has prompted to discover quinolone-based analogues among the researchers due to its great diversity in biological activities. In the past few years, various new, efficient and convenient synthetic approaches (including green chemistry and microwave-assisted synthesis) have been designed and developed to synthesize diverse quinolone-based scaffolds which represent a growing area of interest in academic and industry as well as to explore their biological activities. In this review, an attempt has been made by the authors to summarize (1) One of the most comprehensive listings of quinolone-based drugs or agents in the market or under various stages of clinical development; (2) Recent advances in the synthetic strategies for quinolone derivatives as well as their biological implications including insight of mechanistic studies. (3) Further, the biological data is correlated with structure-activity relationship studies to provide an insight into the rational design of more active agents.

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Infectious tropical diseases such as malaria, tuberculosis, and the so-called neglected tropical diseases are causing tremendous suffering to millions of people and huge impact on national economies, seriously worsening life conditions in the poorest parts of the world, where these diseases are endemic. Despite the existence of drugs for most of these diseases, they are far from adequate. Lack of efficacy, toxicity, and emergence of pathogen resistance are among the most important flaws of currently available drugs. Thus, apart from improving prevention and vector control measures, there is an urgent need for developing new efficacious, safe, and inexpensive drugs that desirably feature novel chemotypes. Multicomponent reactions (MCRs), where three or more reactants are combined in a one-pot reaction, constitute a very powerful tool for such endeavors, inasmuch as they enable a very rapid access to structurally diverse, usually complex scaffolds, shortening the synthesis of the novel drugs and, hence, lowering production costs, and affording original chemotypes. In this chapter, we provide an overview of the application of different types of MCRs to drug discovery against infectious tropical diseases, with particular emphasis on how structural complexity and molecular diversity can be readily introduced through their use.

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