3-Aryl-5-phenoxymethyl-1,3-oxazolidin-2-ones as positive allosteric modulators of mGluR2 for the treatment of schizophrenia: Hit-to-lead efforts
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Published in Bioorganic & medicinal chemistry letters (15.05.2010)
Published in Bioorganic & medicinal chemistry letters (15.05.2010)
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Orally Bioavailable Macrocyclic Peptide That Inhibits Binding of PCSK9 to the Low Density Lipoprotein Receptor
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Optimization of a pyrazoloquinolinone class of Chk1 kinase inhibitors
Brnardic, Edward J., Garbaccio, Robert M., Fraley, Mark E., Tasber, Edward S., Steen, Justin T., Arrington, Kenneth L., Dudkin, Vadim Y., Hartman, George D., Stirdivant, Steven M., Drakas, Bob A., Rickert, Keith, Walsh, Eileen S., Hamilton, Kelly, Buser, Carolyn A., Hardwick, James, Tao, Weikang, Beck, Stephen C., Mao, Xianzhi, Lobell, Robert B., Sepp-Lorenzino, Laura, Yan, Youwei, Ikuta, Mari, Munshi, Sanjeev K., Kuo, Lawrence C., Kreatsoulas, Constantine
Published in Bioorganic & medicinal chemistry letters (01.11.2007)
Published in Bioorganic & medicinal chemistry letters (01.11.2007)
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Novel Phosphate Modified Cathepsin B Linkers: Improving Aqueous Solubility and Enhancing Payload Scope of ADCs
Kern, Jeffrey C., Dooney, Deborah, Zhang, Rena, Liang, Linda, Brandish, Philip E., Cheng, Mangeng, Feng, Guo, Beck, Andrew, Bresson, Damien, Firdos, Juhi, Gately, Dennis, Knudsen, Nick, Manibusan, Anthony, Sun, Ying, Garbaccio, Robert M.
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Published in Bioconjugate chemistry (21.09.2016)
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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
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.
Published in Bioorganic & medicinal chemistry letters (15.10.2007)
Published in Bioorganic & medicinal chemistry letters (15.10.2007)
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Endosomolytic Bioreducible Poly(amido amine disulfide) Polymer Conjugates for the in Vivo Systemic Delivery of siRNA Therapeutics
Parmar, Rubina Giare, Busuek, Marina, Walsh, Eileen S, Leander, Karen R, Howell, Bonnie J, Sepp-Lorenzino, Laura, Kemp, Eric, Crocker, Louis S, Leone, Anthony, Kochansky, Christopher J, Carr, Brian A, Garbaccio, Robert M, Colletti, Steven L, Wang, Weimin
Published in Bioconjugate chemistry (17.04.2013)
Published in Bioconjugate chemistry (17.04.2013)
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Development of thioquinazolinones, allosteric Chk1 kinase inhibitors
Converso, Antonella, Hartingh, Timothy, Garbaccio, Robert M., Tasber, Edward, Rickert, Keith, Fraley, Mark E., Yan, Youwei, Kreatsoulas, Constantine, Stirdivant, Steve, Drakas, Bob, Walsh, Eileen S., Hamilton, Kelly, Buser, Carolyn A., Mao, Xianzhi, Abrams, Marc T., Beck, Stephen C., Tao, Weikang, Lobell, Rob, Sepp-Lorenzino, Laura, Zugay-Murphy, Joan, Sardana, Vinod, Munshi, Sanjeev K., Jezequel-Sur, Sylvie Marie, Zuck, Paul D., Hartman, George D.
Published in Bioorganic & medicinal chemistry letters (15.02.2009)
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Adenosine analogue inhibitors of S-adenosylhomocysteine hydrolase
Converso, Antonella, Hartingh, Timothy, Fraley, Mark E., Garbaccio, Robert M., Hartman, George D., Huang, Shaei Y., Majercak, John M., McCampbell, Alexander, Na, Sang Jin, Ray, William J., Savage, Mary J., Wolffe, Carrie, Yeh, Suzie, Yu, Yuanjiang, White, Rebecca, Zhang, Rena
Published in Bioorganic & medicinal chemistry letters (15.06.2014)
Published in Bioorganic & medicinal chemistry letters (15.06.2014)
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Discovery of 5-aryl-1,3-dihydro-2H-imidazo[4,5-b]pyridin-2-ones as positive allosteric modulators of metabotropic glutamate subtype-2 (mGlu2) receptors with efficacy in a preclinical model of psychosis
Layton, Mark E., Reif, Alexander J., Hartingh, Timothy J., Rodzinak, Kevin, Dudkin, Vadim, Wang, Cheng, Arrington, Ken, Kelly, Michael J., Garbaccio, Robert M., O’Brien, Julie A., Magliaro, Brian C., Uslaner, Jason M., Huszar, Sarah L., Fillgrove, Kerry L., Tang, Cuyue, Kuo, Yuhsin, Jacobson, Marlene A.
Published in Bioorganic & medicinal chemistry letters (15.02.2016)
Published in Bioorganic & medicinal chemistry letters (15.02.2016)
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Improving the In Vivo Therapeutic Index of siRNA Polymer Conjugates through Increasing pH Responsiveness
Guidry, Erin N, Farand, Julie, Soheili, Arash, Parish, Craig A, Kevin, Nancy J, Pipik, Brenda, Calati, Kathleen B, Ikemoto, Nori, Waldman, Jacob H, Latham, Andrew H, Howell, Bonnie J, Leone, Anthony, Garbaccio, Robert M, Barrett, Stephanie E, Parmar, Rubina Giare, Truong, Quang T, Mao, Bing, Davies, Ian W, Colletti, Steven L, Sepp-Lorenzino, Laura
Published in Bioconjugate chemistry (19.02.2014)
Published in Bioconjugate chemistry (19.02.2014)
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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
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.
Published in Bioorganic & medicinal chemistry letters (15.05.2007)
Published in Bioorganic & medicinal chemistry letters (15.05.2007)
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Kinesin spindle protein (KSP) inhibitors. Part 2: The design, synthesis, and characterization of 2,4-diaryl-2,5-dihydropyrrole inhibitors of the mitotic kinesin KSP
Fraley, Mark E., Garbaccio, Robert M., Arrington, Kenneth L., Hoffman, William F., Tasber, Edward S., Coleman, Paul J., Buser, Carolyn A., Walsh, Eileen S., Hamilton, Kelly, Fernandes, Christine, Schaber, Michael D., Lobell, Robert B., Tao, Weikang, South, Victoria J., Yan, Youwei, Kuo, Lawrence C., Prueksaritanont, Thomayant, Shu, Cathy, Torrent, Maricel, Heimbrook, David C., Kohl, Nancy E., Huber, Hans E., Hartman, George D.
Published in Bioorganic & medicinal chemistry letters (01.04.2006)
Published in Bioorganic & medicinal chemistry letters (01.04.2006)
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Blagg, Brian S.J., Johnson, Douglas S., Garbaccio, Robert M.
Published in Bioorganic & medicinal chemistry letters (01.05.2011)
Published in Bioorganic & medicinal chemistry letters (01.05.2011)
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Development of 6-substituted indolylquinolinones as potent Chek1 kinase inhibitors
Huang, Shaei, Garbaccio, Robert M., Fraley, Mark E., Steen, Justin, Kreatsoulas, Constantine, Hartman, George, Stirdivant, Steve, Drakas, Bob, Rickert, Keith, Walsh, Eileen, Hamilton, Kelly, Buser, Carolyn A., Hardwick, James, Mao, Xianzhi, Abrams, Marc, Beck, Steve, Tao, Weikang, Lobell, Rob, Sepp-Lorenzino, Laura, Yan, Youwei, Ikuta, Mari, Murphy, Joan Zugay, Sardana, Vinod, Munshi, Sanjeev, Kuo, Lawrence, Reilly, Michael, Mahan, Elizabeth
Published in Bioorganic & medicinal chemistry letters (15.11.2006)
Published in Bioorganic & medicinal chemistry letters (15.11.2006)
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Synthesis and evaluation of substituted benzoisoquinolinones as potent inhibitors of Chk1 kinase
Garbaccio, Robert M., Huang, Shaei, Tasber, Edward S., Fraley, Mark E., Yan, Youwei, Munshi, Sanjeev, Ikuta, Mari, Kuo, Lawrence, Kreatsoulas, Constanine, Stirdivant, Steve, Drakas, Bob, Rickert, Keith, Walsh, Eileen S., Hamilton, Kelly A., Buser, Carolyn A., Hardwick, James, Mao, Xianzhi, Beck, Stephen C., Abrams, Marc T., Tao, Weikang, Lobell, Rob, Sepp-Lorenzino, Laura, Hartman, George D.
Published in Bioorganic & medicinal chemistry (15.11.2007)
Published in Bioorganic & medicinal chemistry (15.11.2007)
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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
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.
Published in Bioorganic & medicinal chemistry letters (01.04.2006)
Published in Bioorganic & medicinal chemistry letters (01.04.2006)
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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
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.
Published in Bioorganic & medicinal chemistry letters (01.10.2007)
Published in Bioorganic & medicinal chemistry letters (01.10.2007)
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Preface
Garbaccio, Robert M., Johnson, Douglas S., Hong, Jiyong, Disney, Matthew D.
Published in Bioorganic & medicinal chemistry letters (01.11.2015)
Published in Bioorganic & medicinal chemistry letters (01.11.2015)
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