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Your search keyword '"J. William Lown"' showing total 8 results
Start Over Author "J. William Lown" Journal bioorganic & medicinal chemistry letters
8 results on '"J. William Lown"'

1. Design, synthesis, and intracellular localization of a fluorescently labeled DNA binding polyamide related to the antibiotic distamycin

Author

Andrew T Morrissey, Sanjay K. Sharma, Gerald G. Miller, William H. Gmeiner, and J. William Lown

Subjects
endocrine system diseases, Confocal, Clinical Biochemistry, Pharmaceutical Science, Antiviral Agents, Biochemistry, Fluorescence, chemistry.chemical_compound, Drug Discovery, Tumor Cells, Cultured, Humans, Molecular Biology, Cellular localization, Ovarian Neoplasms, Microscopy, Confocal, Chemistry, Distamycins, Organic Chemistry, Biological Transport, DNA, In vitro, Mitochondria, Nylons, Cell culture, Cytoplasm, Drug Design, Molecular Medicine, Female, Intracellular
Abstract

The design and synthesis of the lipophilic (9) and fluorescent (10) conjugates of a structural analogue of distamycin and their in vitro cellular localization studies are reported. Confocal laser scanning microscopy (CLSM) indicates that 10 rapidly enters human ovarian adenocarcinoma (SKOV-3) cells with principal uptake in mitochondria and uniform cytoplasmic distribution.

Published
2001

2. Synthesis and biological evaluation of hybrid molecules containing the pyrroloquinoline nucleus and DNA-minor groove binders

Author

J. William Lown, Rulin Zhao, and Bernadette Oreski

Subjects
Chemistry, Stereochemistry, Organic Chemistry, Clinical Biochemistry, Pharmaceutical Science, Biochemistry, In vitro, chemistry.chemical_compound, medicine.anatomical_structure, Covalent bond, Drug Discovery, medicine, Molecular Medicine, Molecule, Molecular Biology, Nucleus, DNA, Minor groove, Biological evaluation
Abstract

A series of hybrid molecules containing the pyrroloquinoline nucleus covalently linked to polypyrroleamide DNA minor groove binder were synthesized and evaluated for in vitro cytotoxic activity.

Published
1996

3. Synthesis and antitumor activity of camptothecin derivatives bearing five-membered heterocycle containing 10-substituents

Author

Rulin Zhao, J. William Lown, and Bernadette Oreski

Subjects
Antitumor activity, Stereochemistry, Organic Chemistry, Clinical Biochemistry, Pharmaceutical Science, Ring (chemistry), Biochemistry, In vitro, chemistry.chemical_compound, chemistry, Furan, Drug Discovery, polycyclic compounds, Thiophene, medicine, Molecular Medicine, heterocyclic compounds, biological phenomena, cell phenomena, and immunity, neoplasms, Molecular Biology, Camptothecin, Pyrrole, medicine.drug
Abstract

A series of new camptothecin derivatives bearing five-membered ring heterocycle containing substituents in the 10-position were synthesized and evaluated for in vitro cytotoxic activity. Camptothecin derivatives bearing a pyrrole or a thiophene ring were significantly more potent than camptothecin, however those bearing furan were less potent than camptothecin.

Published
1995

4. Novel substituted indolocarbazoles as potent and selective inhibitors of protein kinase C

Author

Hiroyuki Nagata, Guojian Xie, J. William Lown, and Tatsuya Tamaoki

Subjects
chemistry.chemical_classification, Oligopeptide, Chemistry, Kinase, Stereochemistry, Organic Chemistry, Clinical Biochemistry, Pharmaceutical Science, Biochemistry, Drug Discovery, Molecular Medicine, Molecular Biology, Gene, Protein kinase C, Alkyl
Abstract

Novel oligopeptide and amino alkyl substitued indolocarbazoles were synthesized and characterized with respect to inhibition of protein kinases C and A. In both series potent and selective PKC inhibitors could be identified. Structure activity relationships are discussed.

Published
1995

5. Protein kinase C-α inhibitors; structure-activity relationships in bis-indole series

Author

Thomas Meyer, Jürg Zimmermann, Guojian Xie, and J. William Lown

Subjects
Oligopeptide, Stereochemistry, Chemistry, Organic Chemistry, Clinical Biochemistry, Pharmaceutical Science, Biochemistry, Drug Discovery, Molecular Medicine, Amine gas treating, Bis indole, Protein kinase A, Molecular Biology, Protein kinase C
Abstract

To assess the role of the amine and ester containing oligopeptide side-chains in bis-indole protein kinase C inhibitors, six novel hybrids in this series were synthesized. These new compounds displayed effective inhibitory activity against protein kinase C-α.

Published
1995

6. Synthesis and DNA cleaving properties of hybrid molecules containing propargylic sulfones and minor groove binding lexitropsins

Author

J. William Lown, A. Richard Morgan, and Guojian Xie

Subjects
Oligopeptide, Stereochemistry, Lexitropsin, Organic Chemistry, Clinical Biochemistry, Pharmaceutical Science, Cleavage (embryo), Biochemistry, Sulfone, chemistry.chemical_compound, chemistry, Cleave, Drug Discovery, Molecular Medicine, Molecule, Molecular Biology, DNA, Minor groove
Abstract

A series of hybrids incorporating propargylic sulfones and minor groove bindin goligopeptide carriers 2-11 were synthesized and their abilities to cleave DNAd have been demonstrated.

Published
1993

7. Design of DNA-cleaving molecules which incorporate a simplified metal-complexing moiety of bleomycin and lexitropsin carriers

Author

A. Richard Morgan, Liren Huang, and J. William Lown

Subjects
Stereochemistry, Lexitropsin, Organic Chemistry, Clinical Biochemistry, Pharmaceutical Science, respiratory system, Cleavage (embryo), Bleomycin, Biochemistry, Chemical synthesis, respiratory tract diseases, carbohydrates (lipids), Metal, chemistry.chemical_compound, chemistry, visual_art, Drug Discovery, visual_art.visual_art_medium, Molecular Medicine, Moiety, Molecule, Molecular Biology, DNA
Abstract

The syntheses of 1a-c, functional models for bleomycin, which are composed of a simplified metal-complexing moiety of bleomycin and poly-N-methylpyrrole peptides are described. Their functional cleavage of DNA in the presence of reductants is demonstrated.

Published
1993

8. Developmnet of an efficient oligonucleotide derivatization protocol

Author

Richard T. Pon, William H. Gmeiner, Weide Luo, and J. William Lown

Subjects
Chemistry, Oligonucleotide, Stereochemistry, Organic Chemistry, Clinical Biochemistry, Diastereomer, Pharmaceutical Science, Biochemistry, Adenosine, Combinatorial chemistry, chemistry.chemical_compound, Phase (matter), Drug Discovery, medicine, Molecular Medicine, Derivatization, Molecular Biology, medicine.drug
Abstract

An efficient procedure is presented for the introduction of a 6- N -(2-cholesteroloxycarboaminoethyl)-or 6- N -[2-(9-fluorenylmethoxycarboamino)ethyl]moieties into adenosine, which is compatible with solid phase incorporation into antisense oligodeoxyribonucleotides and has the further advantage of lack of diastereomer formation.

Published
1991

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