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Your search keyword '"Nukkala, M. A."' showing total 3 results
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3 results on '"Nukkala, M. A."'

1. Efficacies of ABT-773, a New Ketolide, against Experimental Bacterial Infections

Author

Mitten, M. J., primary, Meulbroek, J., additional, Nukkala, M., additional, Paige, L., additional, Jarvis, K., additional, Oleksijew, A., additional, Tovcimak, A., additional, Hernandez, L., additional, Alder, J. D., additional, Ewing, P., additional, Or, Y. S., additional, Ma, Z., additional, Nilius, A. M., additional, Mollison, K., additional, and Flamm, R. K., additional

Published
2001
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2. New Antimitotic Agents with Activity in Multi-Drug-Resistant Cell Lines and in Vivo Efficacy in Murine Tumor Models

Author

Szczepankiewicz, B. G., Liu, G., Jae, H.-S., Tasker, A. S., Gunawardana, I. W., Geldern, T. W. von, Gwaltney, S. L., II, Wu-Wong, J. R., Gehrke, L., Chiou, W. J., Credo, R. B., Alder, J. D., Nukkala, M. A., Zielinski, N. A., Jarvis, K., Mollison, K. W., Frost, D. J., Bauch, J. L., Hui, Y. H., Claiborne, A. K., Li, Q., and Rosenberg, S. H.

Abstract

During a screen for compounds that could inhibit cell proliferation, a series of new tubulin-binding compounds was identified with the discovery of oxadiazoline 1 (A-105972). This compound showed good cytotoxic activity against non-multi-drug-resistant and multi-drug-resistant cancer cell lines, but its utility in vivo was limited by a short half-life. Medicinal chemistry efforts led to the discovery of indolyloxazoline 22g (A-259745), which maintained all of the in vitro activity seen with oxadiazoline 1, but also demonstrated a better pharmacokinetic profile, and dose-dependent in vivo activity. Over a 28 day study, indolyloxazoline 22g increased the life span of tumor-implanted mice by up to a factor of 3 upon oral dosing. This compound, and others of its structural class, may prove to be useful in the development of new chemotherapeutic agents to treat human cancers.

Published
2001

3. Novel sulfonate analogues of combretastatin A-4: potent antimitotic agents.

Author

Gwaltney SL 2nd, Imade HM, Barr KJ, Li Q, Gehrke L, Credo RB, Warner RB, Lee JY, Kovar P, Wang J, Nukkala MA, Zielinski NA, Frost D, Ng SC, and Sham HL

Subjects
ATP Binding Cassette Transporter, Subfamily B, Member 1 biosynthesis, ATP Binding Cassette Transporter, Subfamily B, Member 1 genetics, Binding Sites physiology, Binding, Competitive, Cell Division drug effects, Colchicine metabolism, Humans, Polymers metabolism, Tubulin metabolism, Tumor Cells, Cultured cytology, Tumor Cells, Cultured drug effects, Antineoplastic Agents chemistry, Antineoplastic Agents pharmacology, Colchicine antagonists & inhibitors, Stilbenes chemistry, Stilbenes pharmacology, Tubulin Modulators
Abstract

Sulfonate analogues of combretastatin A-4 have been prepared. These compounds compete with colchicine and combretastatin A-4 for the colchicine binding site on tubulin and are potent inhibitors of tubulin polymerization and cell proliferation. Importantly, these compounds also inhibit the proliferation of P-glycoprotein positive (+) cancer cells, which are resistant to many other antitumor agents.

Published
2001
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