Browsing by Author "Tsai, Ming-Tsung"

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Capping the upper and lower rims of calix[4]arenes by aryl dinitrile oxide reactions
(2006-11-20)
Shiao, Ya-Jiun
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Chiang, Pei-Chen
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Senthilvelan, Annamalai
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Tsai, Ming-Tsung
;
Lee, Gene-Hsiang
1, 3-Dipolar cycloadditions of upper- and lower-rim diallylcalix[4]arenes (1 and 3) with aryl dinitrile oxides provide a unique and efficient way of capping the calix[4]arenes. When dinitrile oxides reacted with 5-allylcalix[4]arene 7, they underwent a 1,3-dipolar cycloaddition on one side and an electrophilic substitution on the other side, which led to a novel type of asymmetric calix[4]arenes (9 and 12). (c) 2006 Elsevier Ltd. All rights reserved.
Design and synthesis of triazolyl coumarins as Hg2+ selective fluorescent chemosensors
(2012)
Ho, I-Ting
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Lai, Ting-Ling
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Wu, Ren-Tsung
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Tsai, Ming-Tsung
;
Wu, Chun-Ming
A series of triazolyl coumarin derivatives L1-L4, with and without spacer groups between the coumarin and the triazole groups, were synthesized as fluorescent sensors to study their binding ability and selectivity toward metal ions. Ligand L3, which contains an acetyl linker between the triazole and the coumarin, exhibited a high selectivity toward Hg2+ in polar protic solvents MeOH-CHCl3 (9 : 1, v/v) with fluorescent enhancement, furthermore, it was found to bind two Hg2+ at a high concentration (>12.5 mM) of Hg(ClO4)(2). In contrast, L4, in which position 4 of the triazole unit was replaced by a benzyl group instead of the 4-tert-butylphenoxymethyl group used in L1-L3, showed a binding stoichiometry toward only one Hg2+. On the basis of the fluorescent sensing, IR, and H-1 NMR titration results of ligands L1-L4, we proposed that not only the acetyl C=O but also the ether group of the 4-tert-butylphenoxymethyl of L3 assisted the triazole nitrogen atoms in the complexation of Hg2+ to form a 1 : 2 complex (L3 center dot(Hg2+)(2)).
Identification, SAR Studies, and X-ray Co-crystallographic Analysis of a Novel Furanopyrimidine Aurora Kinase A Inhibitor
(2010-02-01)
Coumar, Mohane Selvaraj
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Tsai, Ming-Tsung
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Chu, Chang-Ying
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Uang, Biing-Jiun
;
Lin, Wen-Hsing
Here in we reveal a simple method for the identification of novel Aurora kinase A inhibitors through substructure searching of an in-house compounds for testing. A hydrazone fragment conferring Aurora kinase activity and heterocyclic rings most frequently reported in kinase inhibitors were used as substructure queries to filter the in house compound library collection prior to testing. Five new series of Aurora kinase inhibitors were identified through this strategy with IC(50) values ranging from similar to 300 nm to similar to 15 mu m, by testing only 133 compounds from a database of similar to 125 000 compounds. Structure activity relationship studies and X-ray co-crystallographic analysis of the most potent compound, a furanopyrimidine derivative with an IC(50) value of 309 nm toward Aurora kinase A, were carried out. The knowledge gained through these studies could help in the future design of potent Aurora kinase inhibitors.
MO(CO)(6)-mediated synthesis of calix[4]arenes carrying beta-hydroxy ketones or alpha,beta-unsaturated-beta-amino ketones
(2006-12-18)
Senthilvelan, Annamalai
;
Tsai, Ming-Tsung
;
Chang, Kai-Chi
;
Chung, Wen-Sheng
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應用化學系
MO(CO)(6)-mediated ring opening reactions of calix[4]arene isoxazolines/isoxazoles provide a new synthetic methodology for calix[4]arenes carrying bifunctional beta-hydroxy ketones or alpha,beta-unsaturated-beta-amino ketones. MO(CO)(6) is a highly selective and convenient reagent for the ring opening process of these supramolecular isoxazolines/isoxazoles. (c) 2006 Elsevier Ltd. All rights reserved.