Results 91 to 100 of about 218 (163)

Synthesis and biological evaluation of CHX-DAPYs as HIV-1 non-nucleoside reverse transcriptase inhibitors

, 2014
A series of new diarylpyrimidines (DAPYs) characterized by a halogen atom on the methylene linker between wing I and the central pyrimidine ring was synthesized and evaluated for their anti-HIV activity in MT-4 cell cultures.
Zihong Yan, Hai-Qiu Wu, Wenxue Chen, Yan Wu, Hu‐Ri Piao, Qiuqin He, Fen‐Er Chen, Erik De Clercq, Christophe Pannecouque   +8 more
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Structural modifications of diarylpyrimidines (DAPYs) as HIV-1 NNRTIs: Synthesis, anti-HIV activities and SAR

, 2017
30 new analogues of diarylpyrimidines were synthesized for further structural modifications, involving not only the linker but also the wing α of DAPYs.
Huan-Huan Lu, Ping Xue, Yuan‐Yuan Zhu, Xiu-Lian Ju, Xiaojiao Zheng, Xun Zhang, Ting Xiao, Christophe Pannecouque, Tingting Li, Shuang‐Xi Gu   +9 more
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Evolution of anti-HIV drug candidates. Part 3: diarylpyrimidine (DAPY) analogues

, 2001
The synthesis and anti-HIV-1 activity of a series of diarylpyrimidines (DAPYs) are described. Several members of this novel class of non-nucleoside reverse transcriptase inhibitors (NNRTIs) are extremely potent against both wild-type and a panel of ...
Donald Ludovici, Bart L. De Corte, Michael J. Kukla, Hong Ye, Chih Y. Ho, Mark. A. Lichtenstein, Robert W. Kavash, Koen Andries, Marie-Pierre de Béthune, Hilde Azijn, Rudi Pauwels, Paul Lewi, Jan Heeres, Lucien M. H. Koymans, Marc R. de Jonge, Koen Van Aken, Frederik F. D. Daeyaert, Kalyan Das, Eddy Arnold, Paul A. J. Janssen   +19 more
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Structural modifications of CH(OH)-DAPYs as new HIV-1 non-nucleoside reverse transcriptase inhibitors

, 2014
A series of CR2(OH)-diarylpyrimidine derivatives (CR2(OH)-DAPYs) featuring a hydrophobic group at CH(OH) linker between wing I and the central pyrimidine were synthesized and evaluated for their anti-HIV activity in MT-4 cell cultures.
Zihong Yan, Xiayun Huang, Hai-Qiu Wu, Wenxue Chen, Qiuqin He, Fen‐Er Chen, Erik De Clercq, Christophe Pannecouque   +7 more
openalex   +2 more sources

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A cautionary (spectral) tail: red-shifted fluorescence by DAPI–DAPI interactions

Biochemical Society Transactions, 2016
The fluorescent dye DAPI is useful for its association with and consequent amplification of an ∼460 nm emission maximum upon binding to dsDNA. Labelling with higher DAPI concentrations is a technique used to reveal Pi polymers [polyphosphate (polyP)], with a red-shift to ∼520–550 nm fluorescence emission.
John Georgiou, Wouter J. E. M. Habraken, Sidney Omelon   +2 more
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Applications of DAPI Cytochemistry to Neurobiology

Biotechnic & Histochemistry, 1992
4',6-Diamidino-2-phenylindole hydrochloride (DAPI) is a fluorescent dye with high affinity for DNA. We have employed it as a fluorescent chromatin counterstain on sections immunofluorescent-stained using rhodamine and on tissues enzymatically stained using beta-galactosidase.
Pietro Paolo Sanna, Gail Lewandowski, Gustav F. Jirikowski, Floyd E. Bloom   +3 more
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The Structure of DAPI Bound to DNA

Journal of Biomolecular Structure and Dynamics, 1989
The structure of the DNA fluorochrome 4'-6-diamidine-2-phenyl indole (DAPI) bound to the synthetic B-DNA oligonucleotide C-G-C-G-A-A-T-T-C-G-C-G has been solved by single crystal x-ray diffraction methods, at a resolution of 2.4 A. The structure is nearly isomorphous with that of the native DNA molecule alone. With one DAPI and 25 waters per DNA double
Teresa A. Larsen, David S. Goodsell, Richard E. Dickerson, Kazimierz Grzeskowiak, Duilio Cascio   +4 more
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EXCITED STATE pK_a BEHAVIOUR OF DAPI. A RATIONALIZATION OF THE FLUORESCENCE ENHANCEMENT OF DAPI IN DAPI‐NUCLEIC ACID COMPLEXES*

Photochemistry and Photobiology, 1986
Abstract— The steady state and time resolved fluorescence of the drug and chromosomal staining agent, 4′,6‐diamidino‐2‐phenylindole dihydrochloride, DAPI, was examined under different solvent conditions. In solutions between pH 3 and pH 9 the fluorescence spectral maximum of DAPI was found at 460 nm.
Szabo, A., Krajcarski, D., Cavatorta, P., Masotti, L., Barcellona, M.   +4 more
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Effects of DAPI on human leukocytes in vitro

Cytogenetic and Genome Research, 1979
DAPI (4’-6-diamidino-2-phenylindole), a fluorochrome specific for AT-rich DNA, was supplied for 24 h at various concentrations to human leukocytes in culture. This treatment caused the appearance on the chromosomes of specific areas lacking spiralization. In particular, the centromeric regions of chromosomes 1, 9, and 16, a short region on the long arm
G. Prantera, M. Di Castro, Angela Rocchi
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A novel family of diarylpyrimidines (DAPYs) featuring a diatomic linker: Design, synthesis and anti-HIV activities

, 2015
To improve the conformational flexibility and positional adaptability of the traditional diarylpyrimidines (DAPYs), a family of diarylpyrimidines featuring a C-N diatomic linker between the left wing benzene ring and the central pyrimidine was firstly ...
Shuang‐Xi Gu, Heng Qiao, Yuan‐Yuan Zhu, Qi-Chao Shu, Hui Liu, Xiu-Lian Ju, Erik De Clercq, Jan Balzarini, Christophe Pannecouque   +8 more
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