The Experts below are selected from a list of 321 Experts worldwide ranked by ideXlab platform
Mouangue Nanimina Alexis - One of the best experts on this subject based on the ideXlab platform.
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Differential estrogen receptor subtype modulators: assessment of estrogen receptor subtype-binding selectivity and transcription-regulating properties of new cycloalkyl Pyrazoles.
The Journal of Steroid Biochemistry and Molecular Biology, 2009Co-Authors: Xanthippi Alexi, Nikolaos Fokialakis, George Lambrinidis, Aggeliki K. Meligova, Serkos A. Haroutounian, Konstantinos M. Kasiotis, Emmanuel Mikros, Mouangue Nanimina AlexisAbstract:Several new cycloalkyl-fused diaryl Pyrazoles were synthesized and their binding affinity for the estrogen receptor (ER) subtypes, ERα and ERβ, and subtype-specific agonist/antagonist properties were determined. Cyclopentane- and cyclohexane-fused Pyrazoles with p-hydroxyphenyl rings at positions 1 and 3 displayed modest ERβ-binding selectivity and variable agonism through ERα, while behaving as full estrogen antagonists through ERβ in estrogen-responsive element (ERE)-dependent gene expression assays. By contrast, the 2,3-diphenolic derivatives were non-selective and considerably less effective ERβ antagonists compared to 1,3-diphenolic ones. The cyclohexane-fused 1,3-diphenolic Pyrazole 8, in particular, behaved as full ERα agonist/ERβ antagonist in these assays. Molecular modelling revealed the structural determinants possibly accounting for the differential regulation of transcription through the two ERs exhibited by 8. The data also shows that the ER subtype-binding selectivity and agonist/antagonist efficacy of the 1,3-diphenolic Pyrazoles is influenced by the cycloalkyl ring fused to the Pyrazole core. Using 8 we show that, though the mutant androgen receptor (AR) of LNCaP cells is required for estrogen as well as androgen stimulation of cell growth, estrogen responsiveness of the cells depends on ERβ and AR but not on ERα.
Safaa M. Baker - One of the best experts on this subject based on the ideXlab platform.
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Synthesis, characterization and in vitro antimicrobial activity of novel fused pyrazolo[3,4-c]pyridazine, pyrazolo[3,4-d]pyrimidine, thieno[3,2-c]Pyrazole and pyrazolo[3′,4′:4,5]thieno[2,3-d]pyrimidine derivatives
Chemistry Central Journal, 2017Co-Authors: Mohamed A. M. Abdel Reheim, Safaa M. BakerAbstract:BackgroundSome novel substituted pyrazolone, pyrazolo[3,4-c]pyridazine, pyrazolo[3,4-d]pyrimidine, pyrazolo[3,4-d]thiazolo[3,2-a]pyrimidinone, thieno[3,2-c]Pyrazole and pyrazolo[3′,4′:4,5]thieno[2,3-d]pyrimidine derivatives have been reported to possess various pharmacological activities like antimicrobial, antitumor and anti-inflammatory.ResultsA novel series of azoles and azines were designed and prepared via reaction of 1,3-diphenyl-1H-pyrazol-5(4H)-one with some electrophilic and nucleophilic reagents. The structures of target compounds were confirmed by elemental analyses and spectral data.ConclusionsThe antimicrobial activity of the target synthesized compounds were tested against various microorganisms such as Escherichia coli; Bacillus megaterium; Bacillus subtilis (Bacterial species), Fusarium proliferatum; Trichoderma harzianum; Aspergillus niger (fungal species) by the disc diffusion method. In general, the novel synthesized compounds showed a good antimicrobial activity against the previously mentioned microorganisms.
Takashi Takahashi - One of the best experts on this subject based on the ideXlab platform.
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Sequential SNAr Reaction/Suzuki–Miyaura Coupling/C−H Direct Arylations Approach for the Rapid Synthesis of Tetraaryl-Substituted Pyrazoles
Chemistry-an Asian Journal, 2015Co-Authors: Taiki Morita, Keisuke Matsumura, Kohei Johmoto, Hidehiro Uekusa, Shinichiro Fuse, Daisuke Kobayashi, Takashi TakahashiAbstract:A rapid synthesis of 1,3,4,5-tetraaryl-substituted Pyrazoles has been achieved through a sequence of SNAr reaction/Suzuki–Miyaura coupling/Pd-catalyzed direct arylations that used 3-iodo-1H-Pyrazole as a scaffold. Pyrazoles with four different aryl groups were synthesized in a straightforward manner with no extra synthetic steps, such as protection/deprotection or the introduction of activating/directing groups, using readily available substrates and reagents. The developed synthetic approach enabled the structurally diverse synthesis of multiaryl-substituted Pyrazoles without using a glovebox technique.
Taiki Morita - One of the best experts on this subject based on the ideXlab platform.
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Directing/Protecting‐Group‐Free Synthesis of Tetraaryl‐Substituted Pyrazoles through Four Direct Arylations on an Unsubstituted Pyrazole Scaffold
Chemistry (Weinheim an der Bergstrasse Germany), 2015Co-Authors: Shinichiro Fuse, Taiki Morita, Kohei Johmoto, Hidehiro Uekusa, Hiroshi TanakaAbstract:A directing/protecting-group-free synthesis of 1,3,4,5-tetraaryl-substituted Pyrazoles was achieved through four transition metal-catalyzed direct arylations. Various Pyrazoles with four different aryl rings were obtained using readily available reagents from an unsubstituted Pyrazole. Two aryl-substituted Pyrazoles showed intense violet fluorescence, high quantum yields (Φf =0.68, 0.64), and large Stokes shifts (19000, 15200 cm(-1) ).
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Sequential SNAr Reaction/Suzuki–Miyaura Coupling/C−H Direct Arylations Approach for the Rapid Synthesis of Tetraaryl-Substituted Pyrazoles
Chemistry-an Asian Journal, 2015Co-Authors: Taiki Morita, Keisuke Matsumura, Kohei Johmoto, Hidehiro Uekusa, Shinichiro Fuse, Daisuke Kobayashi, Takashi TakahashiAbstract:A rapid synthesis of 1,3,4,5-tetraaryl-substituted Pyrazoles has been achieved through a sequence of SNAr reaction/Suzuki–Miyaura coupling/Pd-catalyzed direct arylations that used 3-iodo-1H-Pyrazole as a scaffold. Pyrazoles with four different aryl groups were synthesized in a straightforward manner with no extra synthetic steps, such as protection/deprotection or the introduction of activating/directing groups, using readily available substrates and reagents. The developed synthetic approach enabled the structurally diverse synthesis of multiaryl-substituted Pyrazoles without using a glovebox technique.
Sinan Basceken - One of the best experts on this subject based on the ideXlab platform.
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design of pyrazolo pyrrolo pyrazines and pyrazolo pyrrolo diazepines via aucl catalyzed and nah supported cyclization of n propargyl Pyrazoles
Journal of Organic Chemistry, 2015Co-Authors: Sinan Basceken, Metin BalciAbstract:A concise synthetic methodology for new heterocyclic scaffolds, such as pyrazolo-pyrrolo-pyrazine and pyrazolo-pyrrolo-diazepine skeletons, was developed. The key features of this method include (i) synthesis of pyrrole-derived α,β-alkynyl ketones, (ii) introduction of various substituents into the alkyne functionality by Sonogashira cross-coupling, (iii) synthesis of Pyrazole units by the reaction of α,β-alkynyl compounds with hydrazine monohydrate, (iv) gold-catalyzed cyclization of Pyrazoles with alkyne units, and (v) cyclization with NaH. Furthermore, this methodology allows various substituents to be introduced into all positions of the target compounds.
