Search Results - "Borzilleri, Robert"

Antibody–drug conjugates: current status and future directions by Perez, Heidi L., Cardarelli, Pina M., Deshpande, Shrikant, Gangwar, Sanjeev, Schroeder, Gretchen M., Vite, Gregory D., Borzilleri, Robert M.

“…•Antibody–drug conjugates represent an exciting new class of cancer therapeutics.•ADCs comprise monoclonal antibodies that selectively deliver potent cytotoxic…”
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Decarboxylative Peptide Macrocyclization through Photoredox Catalysis by McCarver, Stefan J., Qiao, Jennifer X., Carpenter, Joseph, Borzilleri, Robert M., Poss, Michael A., Eastgate, Martin D., Miller, Michael M., MacMillan, David W. C.

“…A method for the decarboxylative macrocyclization of peptides bearing N‐terminal Michael acceptors has been developed. This synthetic method enables the…”
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Discovery and Synthesis of Heterobifunctional Degraders of Rearranged during Transfection (RET) Kinase by Qiao, Jennifer X., Williams, David, Gill, Patrice, Li, Ling, Norris, Derek, Tokarski, John S., Wong, Jessica, Qi, Huilin, Hafeji, Yamnah, Downes, Daniel P., Degnen, Bill, Wang, Ying-Kai, Locke, Gregory, Fang, Hua, Yu, Fei, Xu, Songmei, Naglich, Joseph, Zhang, Jun, Nanjappa, Purushothama, Dai, Chao, Chourb, Lisa, Napoline, Jonathan, Tester, Richland, Jorge, Christine, Li, Yi-Xin, Mathur, Arvind, Barbieri, Christopher, Soars, Matthew G., Venkatanarayan, Avinashnarayan, Lees, Emma, Borzilleri, Robert M., Gavai, Ashvinikumar V., Wichroski, Michael, Dhar, T. G. Murali

“…We describe the design, synthesis, and structure–activity relationship (SAR) of heterobifunctional RET ligand-directed degraders (LDDs) derived from three…”
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Discovery of N-(4-(2-Amino-3-chloropyridin-4-yloxy)-3-fluorophenyl)-4-ethoxy-1-(4-fluorophenyl)-2-oxo-1,2-dihydropyridine-3-carboxamide (BMS-777607), a Selective and Orally Efficacious Inhibitor of the Met Kinase Superfamily by Schroeder, Gretchen M, An, Yongmi, Cai, Zhen-Wei, Chen, Xiao-Tao, Clark, Cheryl, Cornelius, Lyndon A. M, Dai, Jun, Gullo-Brown, Johnni, Gupta, Ashok, Henley, Benjamin, Hunt, John T, Jeyaseelan, Robert, Kamath, Amrita, Kim, Kyoung, Lippy, Jonathan, Lombardo, Louis J, Manne, Veeraswamy, Oppenheimer, Simone, Sack, John S, Schmidt, Robert J, Shen, Guoxiang, Stefanski, Kevin, Tokarski, John S, Trainor, George L, Wautlet, Barri S, Wei, Donna, Williams, David K, Zhang, Yingru, Zhang, Yueping, Fargnoli, Joseph, Borzilleri, Robert M

“…Substituted N-(4-(2-aminopyridin-4-yloxy)-3-fluoro-phenyl)-1-(4-fluorophenyl)-2-oxo-1,2-dihydropyridine-3-carboxamides were identified as potent and selective…”
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The Discovery of Macrocyclic XIAP Antagonists from a DNA-Programmed Chemistry Library, and Their Optimization To Give Lead Compounds with in Vivo Antitumor Activity by Seigal, Benjamin A, Connors, William H, Fraley, Andrew, Borzilleri, Robert M, Carter, Percy H, Emanuel, Stuart L, Fargnoli, Joseph, Kim, Kyoung, Lei, Ming, Naglich, Joseph G, Pokross, Matthew E, Posy, Shana L, Shen, Henry, Surti, Neha, Talbott, Randy, Zhang, Yong, Terrett, Nicholas K

“…Affinity selection screening of macrocycle libraries derived from DNA-programmed chemistry identified XIAP BIR2 and BIR3 domain inhibitors that displace bound…”
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Heterobicyclic inhibitors of transforming growth factor beta receptor I (TGFβRI) by Harikrishnan, Lalgudi S., Warrier, Jayakumar, Tebben, Andrew J., Tonukunuru, Gopikishan, Madduri, Sudhakara R., Baligar, Vishweshwaraiah, Mannoori, Raju, Seshadri, Balaji, Rahaman, Hasibur, Arunachalam, P.N., Dikundwar, Amol G., Fink, Brian E., Fargnoli, Joseph, Fereshteh, Mark, Fan, Yi, Lippy, Jonathan, Ho, Ching-Ping, Wautlet, Barri, Sheriff, Steven, Ruzanov, Max, Borzilleri, Robert M.

“…[Display omitted] The TGFβ-TGFβR signaling pathway has been reported to play a protective role in the later stages of tumorigenesis via increasing…”
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Discovery of N-(2-Chloro-6-methyl- phenyl)-2-(6-(4-(2-hydroxyethyl)- piperazin-1-yl)-2-methylpyrimidin-4- ylamino)thiazole-5-carboxamide (BMS-354825), a Dual Src/Abl Kinase Inhibitor with Potent Antitumor Activity in Preclinical Assays by Lombardo, Louis J, Lee, Francis Y, Chen, Ping, Norris, Derek, Barrish, Joel C, Behnia, Kamelia, Castaneda, Stephen, Cornelius, Lyndon A. M, Das, Jagabandhu, Doweyko, Arthur M, Fairchild, Craig, Hunt, John T, Inigo, Ivan, Johnston, Kathy, Kamath, Amrita, Kan, David, Klei, Herbert, Marathe, Punit, Pang, Suhong, Peterson, Russell, Pitt, Sidney, Schieven, Gary L, Schmidt, Robert J, Tokarski, John, Wen, Mei-Li, Wityak, John, Borzilleri, Robert M

“…A series of substituted 2-(aminopyridyl)- and 2-(aminopyrimidinyl)thiazole-5-carboxamides was identified as potent Src/Abl kinase inhibitors with excellent…”
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Development of a Stereoselective and Scalable Synthesis for the Potent Indoleamine 2,3-Dioxygenase 1 (IDO1) Inhibitor, BMT-297376; N‑((R)‑1-((cis)‑4-(3-(Difluoromethyl)-2-methoxypyridin-4-yl)cyclohexyl)propyl)-6-methoxynicotinamide by Nimje, Roshan Y, Kuppusamy, Prakasam, Krishnamoorthy, Suresh, Shanmugam, Yoganand, Ramasamy, Duraisamy, Manoharan, Haridhas, Arunachalam, Pirama Nayagam, Balog, Aaron, Cherney, Emily C, Zhang, Liping, Borzilleri, Robert M, Hong, Zhenqiu, Kempson, James, Rampulla, Richard R, Mathur, Arvind, Gupta, Anuradha

“…The current work describes a stereoselective and scalable route to…”
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Discovery of Brivanib Alaninate ((S)-((R)-1-(4-(4-Fluoro-2-methyl-1H-indol-5-yloxy)-5-methylpyrrolo[2,1-f][1,2,4]triazin-6-yloxy)propan-2-yl)2-aminopropanoate), A Novel Prodrug of Dual Vascular Endothelial Growth Factor Receptor-2 and Fibroblast Growth Factor Receptor-1 Kinase Inhibitor (BMS-540215) by Cai, Zhen-wei, Zhang, Yongzheng, Borzilleri, Robert M, Qian, Ligang, Barbosa, Stephanie, Wei, Donna, Zheng, Xiaoping, Wu, Lawrence, Fan, Junying, Shi, Zhongping, Wautlet, Barri S, Mortillo, Steve, Jeyaseelan, Robert, Kukral, Daniel W, Kamath, Amrita, Marathe, Punit, D’Arienzo, Celia, Derbin, George, Barrish, Joel C, Robl, Jeffrey A, Hunt, John T, Lombardo, Louis J, Fargnoli, Joseph, Bhide, Rajeev S

“…A series of amino acid ester prodrugs of the dual VEGFR-2/FGFR-1 kinase inhibitor 1 (BMS-540215) was prepared in an effort to improve the aqueous solubility…”
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Discovery of Pyrrolopyridine−Pyridone Based Inhibitors of Met Kinase: Synthesis, X-ray Crystallographic Analysis, and Biological Activities by Kim, Kyoung Soon, Zhang, Liping, Schmidt, Robert, Cai, Zhen-Wei, Wei, Donna, Williams, David K, Lombardo, Louis J, Trainor, George L, Xie, Dianlin, Zhang, Yaquan, An, Yongmi, Sack, John S, Tokarski, John S, Darienzo, Celia, Kamath, Amrita, Marathe, Punit, Zhang, Yueping, Lippy, Jonathan, Jeyaseelan, Robert, Wautlet, Barri, Henley, Benjamin, Gullo-Brown, Johnni, Manne, Veeraswamy, Hunt, John T, Fargnoli, Joseph, Borzilleri, Robert M

“…Conformationally constrained 2-pyridone analogue 2 is a potent Met kinase inhibitor with an IC50 value of 1.8 nM. Further SAR of the 2-pyridone based…”
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Development of a Scalable Synthesis of the Small Molecule TGFβR1 Inhibitor BMS-986260 by Vetrichelvan, Muthalagu, Rakshit, Souvik, Chandrasekaran, Sathishkumar, Chinnakalai, Karthikeyan, Darne, Chetan Padmakar, Doddalingappa, Dyamanna, Gopikumar, Indasi, Gupta, Anuradha, Gupta, Arun Kumar, Karmakar, Ananta, Lakshminarasimhan, Thirumalai, Leahy, David K, Palani, Senthil, Radhakrishnan, Vignesh, Rampulla, Richard, Savarimuthu, Antony, Subramanian, Varadharajan, Velaparthi, Upender, Warrier, Jayakumar, Eastgate, Martin D, Borzilleri, Robert M, Mathur, Arvind, Vaidyanathan, Rajappa

“…A scalable route to the small molecule TGFβR1 inhibitor BMS-986260 (1) was developed. This alternative approach circumvented the purification of intermediates…”
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Mcl-1 antagonism is a potential therapeutic strategy in a subset of solid cancers by Modugno, Michele, Banfi, Patrizia, Gasparri, Fabio, Borzilleri, Robert, Carter, Percy, Cornelius, Lyndon, Gottardis, Marco, Lee, Ving, Mapelli, Claudio, Naglich, Joseph G., Tebben, Andrew, Vite, Gregory, Pastori, Wilma, Albanese, Clara, Corti, Emiliana, Ballinari, Dario, Galvani, Arturo

“…Cancer cell survival is frequently dependent on the elevated levels of members of the Bcl-2 family of prosurvival proteins that bind to and inactivate…”
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Macrocyclic pyrrolobenzodiazepine dimers as antibody-drug conjugate payloads by Donnell, Andrew F., Zhang, Yong, Stang, Erik M., Wei, Donna D., Tebben, Andrew J., Perez, Heidi L., Schroeder, Gretchen M., Pan, Chin, Rao, Chetana, Borzilleri, Robert M., Vite, Gregory D., Gangwar, Sanjeev

“…[Display omitted] Macrocyclic pyrrolobenzodiazepine dimers were designed and evaluated for use as antibody-drug conjugate payloads. Initial structure–activity…”
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Discovery of 4‑Azaindole Inhibitors of TGFβRI as Immuno-oncology Agents by Zhang, Yong, Zhao, Yufen, Tebben, Andrew J, Sheriff, Steven, Ruzanov, Max, Fereshteh, Mark P, Fan, Yi, Lippy, Jonathan, Swanson, Jesse, Ho, Ching-Ping, Wautlet, Barri S, Rose, Anne, Parrish, Karen, Yang, Zheng, Donnell, Andrew F, Zhang, Liping, Fink, Brian E, Vite, Gregory D, Augustine-Rauch, Karen, Fargnoli, Joseph, Borzilleri, Robert M

“…The multifunctional cytokine TGFβ plays a central role in regulating antitumor immunity. It has been postulated that inhibition of TGFβ signaling in concert…”
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Discovery of BMS-986260, a Potent, Selective, and Orally Bioavailable TGFβR1 Inhibitor as an Immuno-oncology Agent by Velaparthi, Upender, Darne, Chetan Padmakar, Warrier, Jayakumar, Liu, Peiying, Rahaman, Hasibur, Augustine-Rauch, Karen, Parrish, Karen, Yang, Zheng, Swanson, Jesse, Brown, Jennifer, Dhar, Gopal, Anandam, Aravind, Holenarsipur, Vinay K, Palanisamy, Kamalavenkatesh, Wautlet, Barri S, Fereshteh, Mark P, Lippy, Jonathan, Tebben, Andrew J, Sheriff, Steven, Ruzanov, Max, Yan, Chunhong, Gupta, Anuradha, Gupta, Arun Kumar, Vetrichelvan, Muthalagu, Mathur, Arvind, Gelman, Marina, Singh, Rajinder, Kinsella, Todd, Murtaza, Anwar, Fargnoli, Joseph, Vite, Gregory, Borzilleri, Robert M

“…Novel imidazole-based TGFβR1 inhibitors were identified and optimized for potency, selectivity, and pharmacokinetic and physicochemical characteristics…”
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Discovery of tetrahydroisoquinoline-based bivalent heterodimeric IAP antagonists by Kim, Kyoung Soon, Zhang, Liping, Williams, David, Perez, Heidi L., Stang, Erik, Borzilleri, Robert M., Posy, Shana, Lei, Ming, Chaudhry, Charu, Emanuel, Stuart, Talbott, Randy

“…[Display omitted] Bivalent heterodimeric IAP antagonists that incorporate (R)-tetrahydroisoquinoline in the P3′ subunit show high affinity for the BIR2 domain…”
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Preclinical discovery of ixabepilone, a highly active antineoplastic agent by Lee, Francis Y. F., Borzilleri, Robert, Fairchild, Craig R., Kamath, Amrita, Smykla, Richard, Kramer, Robert, Vite, Gregory

“…The epothilones and their analogs constitute a novel class of antineoplastic agents, produced by the myxobacterium Sorangium cellulosum . These antimicrotubule…”
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Discovery of Potent Heterodimeric Antagonists of Inhibitor of Apoptosis Proteins (IAPs) with Sustained Antitumor Activity by Perez, Heidi L, Chaudhry, Charu, Emanuel, Stuart L, Fanslau, Caroline, Fargnoli, Joseph, Gan, Jinping, Kim, Kyoung S, Lei, Ming, Naglich, Joseph G, Traeger, Sarah C, Vuppugalla, Ragini, Wei, Donna D, Vite, Gregory D, Talbott, Randy L, Borzilleri, Robert M

“…The prominent role of IAPs in controlling cell death and their overexpression in a variety of cancers has prompted the development of IAP antagonists as…”
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Building homogeneous time-resolved fluorescence resonance energy transfer assays for characterization of bivalent inhibitors of an inhibitor of apoptosis protein target by Chaudhry, Charu, Davis, Jonathan, Zhang, Yong, Posy, Shana, Lei, Ming, Shen, Henry, Yan, Chunhong, Devaux, Brigitte, Zhang, Litao, Blat, Yuval, Metzler, William, Borzilleri, Robert M., Talbott, Randy L.

“…XIAP (X-chromosome-linked inhibitor of apoptosis protein) is a central apoptosis regulator that blocks cell death by inhibiting caspase-3, caspase-7, and…”
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Pharmacology of smac mimetics; chemotype differentiation based on physical association with caspase regulators and cellular transport by Talbott, Randy L., Borzilleri, Robert M., Chaudhry, Charu, Fargnoli, Joseph, Shen, Henry, Fairchild, Craig, Barnhart, Bryan, Ortega, Marie, McDonagh, Thomas E., Vuppugalla, Ragini, Vite, Gregory D., Hunt, John T., Gottardis, Marco, Naglich, Joseph G.

“…Cellular levels of inhibitor of apoptosis (IAP) proteins are elevated in multiple human cancers and their activities often play a part in promoting cancer cell…”
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