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      New Potential Antitumor Pyrazole Derivatives: Synthesis and Cytotoxic Evaluation

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          Abstract

          New pyrazole derivatives were designed and synthesized as potential protein kinase inhibitors in the view to develop specific antitumor therapies. The structures of the compounds were elucidated using spectral and elemental analyses. The antitumor potential was estimated using wheat seeds and the general toxicity was evaluated by alternative methods, using invertebrate animals. One 3-aminopyrazole derivative emerged as a potential candidate for the development of future cytotoxic compounds.

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          Aquatic ecotoxicity of pharmaceuticals including the assessment of combination effects.

          M Cleuvers (2003)
          To evaluate the ecotoxicological potential of ten prescription drugs against aquatic organisms from different taxonornical classes, a set of biotests were performed using the cladoceran Daphnia magna, the chlorophyte Desmodesmus subspicatus and the macrophyte Lemna minor. Endpoints were immobilisation for Daphnia and inhibition of the average growth rate for Desmodesmus and Lemna. For most of the substances, toxicities were moderate, with EC(50)s in the range from 10 to 100 mgl(-1) or even far above, whereas Lemna was the most sensitive test species in the majority of all tested compounds. Tests with combinations of various pharmaceuticals revealed stronger effects than expected from the effects measured singly. Clofibrinic acid and Carbamazepine have been found to act by a non-specific mode of action (non-polar narcosis), and with Daphnia the combination effect of these substances followed the concept of concentration addition, while in the algae test the concept of independent action could be used to calculate the mixture toxicity. The anti-inflammatory drugs Diclofenac and Ibuprofen have also been found to act unspecific by non-polar narcosis and to follow the concept of concentration addition in the algal test as well as in the Daphnia test. The measured toxicities of the tested pharmaceuticals shows that acute effect of single substances in the aquatic environment are very unlikely. But we should keep in mind that considerable combination effects can occur and that toxicity data from chronic studies are needed to assess the environmental risk of drug residues.
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            Identification of N-(4-piperidinyl)-4-(2,6-dichlorobenzoylamino)-1H-pyrazole-3-carboxamide (AT7519), a novel cyclin dependent kinase inhibitor using fragment-based X-ray crystallography and structure based drug design.

            Matthias Reule, Megan A. O’Brien, Rachel L McMenamin … (2008)
            The application of fragment-based screening techniques to cyclin dependent kinase 2 (CDK2) identified multiple (>30) efficient, synthetically tractable small molecule hits for further optimization. Structure-based design approaches led to the identification of multiple lead series, which retained the key interactions of the initial binding fragments and additionally explored other areas of the ATP binding site. The majority of this paper details the structure-guided optimization of indazole (6) using information gained from multiple ligand-CDK2 cocrystal structures. Identification of key binding features for this class of compounds resulted in a series of molecules with low nM affinity for CDK2. Optimisation of cellular activity and characterization of pharmacokinetic properties led to the identification of 33 (AT7519), which is currently being evaluated in clinical trials for the treatment of human cancers.
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              Use of the genus Artemia in ecotoxicity testing.

              L Guilhermino, Aryane E. B. Nunes, Rodrigo Carvalho … (2006)
              Information related to varied uses of several species of the genus Artemia (commonly known as brine shrimp), is dispersed among literature from several scientific areas, such as Ecology, Physiology, Ecotoxicology, Aquaculture and Genetics. The present paper reviews information related to Artemia that may be considered relevant for ecotoxicity testing. Integration of different areas of scientific knowledge concerning biology, life cycle and environmental needs of Artemia is of crucial importance when considering the interpretation of results drawn from tests involving this genus. Furthermore, this paper provides suggestions to overcome problems related to toxicity assessment with the use of Artemia as test organism in bioassays, under the scope of estuarine, marine and hypersaline environments. Aspects related to variability in results, adoptable toxicity end-points, culture conditions, characteristics of species and strains, influence of geographical origins over physiological features and responses to exposure to chemical agents are considered.
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                Author and article information

                Journal
                Journal ID (nlm-ta): Int J Mol Sci
                Journal ID (iso-abbrev): Int J Mol Sci
                Journal ID (publisher-id): ijms
                Title: International Journal of Molecular Sciences
                Publisher: Molecular Diversity Preservation International (MDPI)
                ISSN (Electronic): 1422-0067
                Publication date Collection: November 2013
                Publication date (Electronic): 04 November 2013
                Volume: 14
                Issue: 11
                Pages: 21805-21818
                Affiliations
                [1 ]Faculty of Pharmacy, “Carol Davila” University of Medicine and Pharmacy, Traian Vuia 6, Bucharest 020956, Romania; E-Mail: octav_olaru2002@ 123456yahoo.com
                [2 ]Organic Chemistry Center of the Romanian Academy “Costin D. Nenitescu”, Splaiul Independentei, 202B, Bucharest 060023, Romania; E-Mail: cst_drag@ 123456yahoo.com
                Author notes
                [* ]Author to whom correspondence should be addressed; E-Mail: nitulescu_mihai@ 123456yahoo.com ; Tel.: +40-213-180-739.
                Article
                Publisher ID: ijms-14-21805
                DOI: 10.3390/ijms141121805
                PMC ID: 3856036
                PubMed ID: 24192822
                SO-VID: a193d824-21ca-4127-b6db-a546f6d89c1f
                Copyright © © 2013 by the authors; licensee MDPI, Basel, Switzerland
                License:

                This article is an open access article distributed under the terms and conditions of the Creative Commons Attribution license ( http://creativecommons.org/licenses/by/3.0/).

                History
                Date received : 05 September 2013
                Date revision received : 22 October 2013
                Date accepted : 28 October 2013
                Categories
                Subject: Article

                ScienceOpen disciplines: Molecular biology
                Keywords: pyrazolyl thiourea,triticum aestivum,artemia salina,daphnia magna
                Data availability:
                ScienceOpen disciplines: Molecular biology
                Keywords: pyrazolyl thiourea, triticum aestivum, artemia salina, daphnia magna

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