Search Results - "South, Vicki J"

Kinesin Spindle Protein (KSP) Inhibitors. 9. Discovery of (2S)-4-(2,5-Difluorophenyl)-N-[(3R,4S)-3-fluoro-1-methylpiperidin-4-yl]-2-(hydroxymethyl)-N-methyl-2-phenyl-2,5-dihydro-1H-pyrrole-1-carboxamide (MK-0731) for the Treatment of Taxane-Refractory Cancer by Cox, Christopher D, Coleman, Paul J, Breslin, Michael J, Whitman, David B, Garbaccio, Robert M, Fraley, Mark E, Buser, Carolyn A, Walsh, Eileen S, Hamilton, Kelly, Schaber, Michael D, Lobell, Robert B, Tao, Weikang, Davide, Joseph P, Diehl, Ronald E, Abrams, Marc T, South, Vicki J, Huber, Hans E, Torrent, Maricel, Prueksaritanont, Thomayant, Li, Chunze, Slaughter, Donald E, Mahan, Elizabeth, Fernandez-Metzler, Carmen, Yan, Youwei, Kuo, Lawrence C, Kohl, Nancy E, Hartman, George D

“…Inhibition of kinesin spindle protein (KSP) is a novel mechanism for treatment of cancer with the potential to overcome limitations associated with currently…”
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Kinesin spindle protein (KSP) inhibitors. Part 8: Design and synthesis of 1,4-diaryl-4,5-dihydropyrazoles as potent inhibitors of the mitotic kinesin KSP by Roecker, Anthony J., Coleman, Paul J., Mercer, Swati P., Schreier, John D., Buser, Carolyn A., Walsh, Eileen S., Hamilton, Kelly, Lobell, Robert B., Tao, Weikang, Diehl, Ronald E., South, Vicki J., Davide, Joseph P., Kohl, Nancy E., Yan, Youwei, Kuo, Lawrence C., Li, Chunze, Fernandez-Metzler, Carmen, Mahan, Elizabeth A., Prueksaritanont, Thomayant, Hartman, George D.

“…1,4-Diaryl-4,5-dihydropyrazoles (i.e., 25) are reported as potent inhibitors of the mitotic kinesin KSP. Inspired by previous efforts in the…”
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Kinesin spindle protein (KSP) inhibitors. Part 4: Structure-based design of 5-alkylamino-3,5-diaryl-4,5-dihydropyrazoles as potent, water-soluble inhibitors of the mitotic kinesin KSP by COX, Christopher D, TORRENT, Maricel, LOBELL, Robert B, WEIKANG TAO, SOUTH, Vicki J, KOHL, Nancy E, YOUWEI YAN, KUO, Lawrence C, PRUEKSARITANONT, Thomayant, SLAUGHTER, Donald E, CHUNZE LI, MAHAN, Elizabeth, BRESLIN, Michael J, BING LU, HARTMAN, George D, MARIANO, Brenda J, WHITMAN, David B, COLEMAN, Paul J, BUSER, Carolyn A, WALSH, Eileen S, HAMILTON, Kelly, SCHABER, Michael D

“…Molecular modeling in combination with X-ray crystallographic information was employed to identify a region of the kinesin spindle protein (KSP) binding site…”
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Kinesin spindle protein (KSP) inhibitors. Part 7: Design and synthesis of 3,3-disubstituted dihydropyrazolobenzoxazines as potent inhibitors of the mitotic kinesin KSP by Garbaccio, Robert M., Tasber, Edward S., Neilson, Lou Anne, Coleman, Paul J., Fraley, Mark E., Olson, Christy, Bergman, Jeff, Torrent, Maricel, Buser, Carolyn A., Rickert, Keith, Walsh, Eileen S., Hamilton, Kelly, Lobell, Robert B., Tao, Weikang, South, Vicki J., Diehl, Ronald E., Davide, Joseph P., Yan, Youwei, Kuo, Lawrence C., Li, Chunze, Prueksaritanont, Thomayant, Fernandez-Metzler, Carmen, Mahan, Elizabeth A., Slaughter, Donald E., Salata, Joseph J., Kohl, Nancy E., Huber, Hans E., Hartman, George D.

“…Dihydropyrazolobenzoxazines (i.e., 20) are reported as potent inhibitors of the mitotic kinesin KSP. Observations from two structurally related series of KSP…”
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Kinesin spindle protein (KSP) inhibitors. Part V: Discovery of 2-propylamino-2,4-diaryl-2,5-dihydropyrroles as potent, water-soluble KSP inhibitors, and modulation of their basicity by β-fluorination to overcome cellular efflux by P-glycoprotein by Cox, Christopher D., Breslin, Michael J., Whitman, David B., Coleman, Paul J., Garbaccio, Robert M., Fraley, Mark E., Zrada, Matthew M., Buser, Carolyn A., Walsh, Eileen S., Hamilton, Kelly, Lobell, Robert B., Tao, Weikang, Abrams, Marc T., South, Vicki J., Huber, Hans E., Kohl, Nancy E., Hartman, George D.

“…Installation of a C2-aminopropyl side chain to the 2,4-diaryl-2,5-dihydropyrrole series of kinesin spindle protein (KSP) inhibitors results in potent, water…”
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Kinesin spindle protein (KSP) inhibitors. Part 3: Synthesis and evaluation of phenolic 2,4-diaryl-2,5-dihydropyrroles with reduced hERG binding and employment of a phosphate prodrug strategy for aqueous solubility by Garbaccio, Robert M., Fraley, Mark E., Tasber, Edward S., Olson, Christy M., Hoffman, William F., Arrington, Kenneth L., Torrent, Maricel, Buser, Carolyn A., Walsh, Eileen S., Hamilton, Kelly, Schaber, Michael D., Fernandes, Christine, Lobell, Robert B., Tao, Weikang, South, Vicki J., Yan, Youwei, Kuo, Lawrence C., Prueksaritanont, Thomayant, Slaughter, Donald E., Shu, Cathy, Heimbrook, David C., Kohl, Nancy E., Huber, Hans E., Hartman, George D.

“…Phenolic 2,4-diaryl-2,5-dihydropyrroles are reported as potent inhibitors of the mitotic kinesin KSP. 2,4-Diaryl-2,5-dihydropyrroles have been discovered to be…”
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Kinesin spindle protein (KSP) inhibitors. Part 6: Design and synthesis of 3,5-diaryl-4,5-dihydropyrazole amides as potent inhibitors of the mitotic kinesin KSP by Coleman, Paul J., Schreier, John D., Cox, Christopher D., Fraley, Mark E., Garbaccio, Robert M., Buser, Carolyn A., Walsh, Eileen S., Hamilton, Kelly, Lobell, Robert B., Rickert, Keith, Tao, Weikang, Diehl, Ronald E., South, Vicki J., Davide, Joseph P., Kohl, Nancy E., Yan, Youwei, Kuo, Lawrence, Prueksaritanont, Thomayant, Li, Chunze, Mahan, Elizabeth A., Fernandez-Metzler, Carmen, Salata, Joseph J., Hartman, George D.

“…Dihydropyrazole amides such as 24 are potent inhibitors of KSP with favorable physical properties, pharmacokinetics, and in vivo potency. A diastereoselective…”
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Kinesin Spindle Protein (KSP) Inhibitors. 9. Discovery of (2 S )-4-(2,5-Difluorophenyl)- N -[(3 R ,4 S )-3-fluoro-1-methylpiperidin-4-yl]-2-(hydroxymethyl)- N -methyl-2-phenyl-2,5-dihydro-1 H -pyrrole-1-carboxamide (MK-0731) for the Treatment of Taxane-Refractory Cancer by Cox, Christopher D., Coleman, Paul J., Breslin, Michael J., Whitman, David B., Garbaccio, Robert M., Fraley, Mark E., Buser, Carolyn A., Walsh, Eileen S., Hamilton, Kelly, Schaber, Michael D., Lobell, Robert B., Tao, Weikang, Davide, Joseph P., Diehl, Ronald E., Abrams, Marc T., South, Vicki J., Huber, Hans E., Torrent, Maricel, Prueksaritanont, Thomayant, Li, Chunze, Slaughter, Donald E., Mahan, Elizabeth, Fernandez-Metzler, Carmen, Yan, Youwei, Kuo, Lawrence C., Kohl, Nancy E., Hartman, George D.

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Kinesin spindle protein KSP inhibitors. Part 8: Design and synthesis of 1,4-diaryl-4,5-dihydropyrazoles as potent inhibitors of the mitotic kinesin KSP by ROECKER, Anthony J, COLEMAN, Paul J, SOUTH, Vicki J, DAVIDE, Joseph P, KOHL, Nancy E, YOUWEI YAN, KUO, Lawrence C, CHUNZE LI, FERNANDEZ-METZLER, Carmen, MAHAN, Elizabeth A, PRUEKSARITANONT, Thomayant, HARTMAN, George D, MERCER, Swati P, SCHREIER, John D, BUSER, Carolyn A, WALSH, Eileen S, HAMILTON, Kelly, LOBELL, Robert B, WEIKANG TAO, DIEHL, Ronald E

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Kinesin spindle protein (KSP) inhibitors. Part 4: 1 Structure-based design of 5-alkylamino-3,5-diaryl-4,5-dihydropyrazoles as potent, water-soluble inhibitors of the mitotic kinesin KSP by Cox, Christopher D., Torrent, Maricel, Breslin, Michael J., Mariano, Brenda J., Whitman, David B., Coleman, Paul J., Buser, Carolyn A., Walsh, Eileen S., Hamilton, Kelly, Schaber, Michael D., Lobell, Robert B., Tao, Weikang, South, Vicki J., Kohl, Nancy E., Yan, Youwei, Kuo, Lawrence C., Prueksaritanont, Thomayant, Slaughter, Donald E., Li, Chunze, Mahan, Elizabeth, Lu, Bing, Hartman, George D.

“…A successful effort was undertaken to improve potency and solubility in a class of anti-mitotic agents that was guided by computer-generated structural models…”
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