Search Results - "Aristoff, Paul"

Antibody-Drug Conjugates for the Treatment of Cancer by Flygare, John A., Pillow, Thomas H., Aristoff, Paul

“…With over 20 antibody‐drug conjugates in clinical trials as well as a recently FDA‐approved drug, it is clear that this is becoming an important and viable…”
Get full text

Rifamycins – Obstacles and opportunities by Aristoff, Paul A, Garcia, George A, Kirchhoff, Paul D, Hollis Showalter, H.D

“…Summary With nearly one-third of the global population infected by Mycobacterium tuberculosis , TB remains a major cause of death (1.7 million in 2006). TB is…”
Get full text

A Novel Allosteric Inhibitor of Macrophage Migration Inhibitory Factor (MIF) by Bai, Fengwei, Asojo, Oluwatoyin A., Cirillo, Pier, Ciustea, Mihai, Ledizet, Michel, Aristoff, Paul A., Leng, Lin, Koski, Raymond A., Powell, Thomas J., Bucala, Richard, Anthony, Karen G.

“…Macrophage migration inhibitory factor (MIF) is a catalytic cytokine and an upstream mediator of the inflammatory pathway. MIF has broad regulatory properties,…”
Get full text

New classes of alanine racemase inhibitors identified by high-throughput screening show antimicrobial activity against Mycobacterium tuberculosis by Anthony, Karen G, Strych, Ulrich, Yeung, Kacheong R, Shoen, Carolyn S, Perez, Oriana, Krause, Kurt L, Cynamon, Michael H, Aristoff, Paul A, Koski, Raymond A

“…In an effort to discover new drugs to treat tuberculosis (TB) we chose alanine racemase as the target of our drug discovery efforts. In Mycobacterium…”
Get full text

Inhibition of mycobacterial alanine racemase activity and growth by thiadiazolidinones by Lee, Yashang, Mootien, Sara, Shoen, Carolyn, Destefano, Michelle, Cirillo, Pier, Asojo, Oluwatoyin A., Yeung, Kacheong R., Ledizet, Michel, Cynamon, Michael H., Aristoff, Paul A., Koski, Raymond A., Kaplan, Paul A., Anthony, Karen G.

“…The genus Mycobacterium includes non-pathogenic species such as M. smegmatis, and pathogenic species such as M. tuberculosis, the causative agent of…”
Get full text

Thiadiazolidinones: A new class of alanine racemase inhibitors with antimicrobial activity against methicillin-resistant Staphylococcus aureus by Ciustea, Mihai, Mootien, Sara, Rosato, Adriana E., Perez, Oriana, Cirillo, Pier, Yeung, Kacheong R., Ledizet, Michel, Cynamon, Michael H., Aristoff, Paul A., Koski, Raymond A., Kaplan, Paul A., Anthony, Karen G.

“…L2-401 (4-[(4-fluorophenyl)methyl]-2-(4-methylphenyl)-1,2,4-thiadiazolidine-3,5-dione). A novel alanine racemase inhibitor. Methicillin-resistant…”
Get full text

Oxazolidinones: a new class of antibacterials by Zurenko, Gary E, Gibson, John K, Shinabarger, Dean L, Aristoff, Paul A, Ford, Charles W, Tarpley, W.Gary

“…The oxazolidinones represent the first truly new class of antibacterial agents to reach the marketplace in several decades. They have a unique mechanism of…”
Get full text

Antibacterial Oxazolidinones Possessing a Novel C-5 Side Chain. (5R)-trans-3-[3-Fluoro-4- (1-oxotetrahydrothiopyran-4-yl)phenyl]-2- oxooxazolidine-5-carboxylic Acid Amide (PF-00422602), a New Lead Compound by Poel, Toni-Jo, Thomas, Richard C, Adams, Wade J, Aristoff, Paul A, Barbachyn, Michael R, Boyer, Frederick E, Brieland, Joan, Brideau, Roger, Brodfuehrer, Joanne, Brown, Alan P, Choy, Allison L, Dermyer, Michael, Dority, Michael, Ford, Charles W, Gadwood, Robert C, Hanna, Debra, Hongliang, Cai, Huband, Michael D, Huber, Christopher, Kelly, Rose, Kim, Ji-Young, Martin, Joseph P, Pagano, Paul J, Ross, Daniel, Skerlos, Laura, Sulavik, Mark C, Zhu, Tong, Zurenko, Gary E, Prasad, J. V. N. Vara

“…Oxazolidinones possessing a C-5 carboxamide functionality (reverse amides) represent a new series of compounds that block bacterial protein synthesis. These…”
Get full text

Synthesis and biological evaluation of benzazepine oxazolidinone antibacterials by Johnson, Paul D., Aristoff, Paul A., Zurenko, Gary E., Schaadt, Ronda D., Yagi, Betty H., Ford, Charles W., Hamel, Judith C., Stapert, Douglas, Moerman, Judy K.

“…Novel benzazepine oxazolidinone antibacterials were synthesized and evaluated against clinically relevant susceptible and resistant organisms. The effect of…”
Get full text

Structure–Activity Relationship of Flavin Analogues That Target the Flavin Mononucleotide Riboswitch by Vicens, Quentin, Mondragón, Estefanía, Reyes, Francis E, Coish, Philip, Aristoff, Paul, Berman, Judd, Kaur, Harpreet, Kells, Kevin W, Wickens, Phil, Wilson, Jeffery, Gadwood, Robert C, Schostarez, Heinrich J, Suto, Robert K, Blount, Kenneth F, Batey, Robert T

“…The flavin mononucleotide (FMN) riboswitch is an emerging target for the development of novel RNA-targeting antibiotics. We previously discovered an FMN…”
Get full text

Novel riboswitch-binding flavin analog that protects mice against Clostridium difficile infection without inhibiting cecal flora by Blount, Kenneth F, Megyola, Cynthia, Plummer, Mark, Osterman, David, O'Connell, Tim, Aristoff, Paul, Quinn, Cheryl, Chrusciel, R Alan, Poel, Toni J, Schostarez, Heinrich J, Stewart, Catherine A, Walker, Daniel P, Wuts, Peter G M, Breaker, Ronald R

“…Novel mechanisms of action and new chemical scaffolds are needed to rejuvenate antibacterial drug discovery, and riboswitch regulators of bacterial gene…”
Get full text

Molecular basis for sequence-specific DNA alkylation by CC-1065 by Hurley, Laurence H, Lee, Chong Soon, McGovren, J. Patrick, Warpehoski, Martha A, Mitchell, Mark A, Kelly, Robert C, Aristoff, Paul A

“…CC-1065 is a potent antitumor antibiotic that binds covalently to N3 of adenine in the minor groove of DNA. The CC-1065 molecule is made up of three repeating…”
Get full text

Structure-activity relationship of flavin analogs that target the FMN riboswitch by Vicens, Quentin, Mondragón, Estefanía, Reyes, Francis E., Coish, Philip, Aristoff, Paul, Berman, Judd, Kaur, Harpreet, Kells, Kevin W., Wickens, Phil, Wilson, Jeffery, Gadwood, Robert C., Schostarez, Heinrich J., Suto, Robert K., Blount, Kenneth F., Batey, Robert T.

“…The flavin mononucleotide (FMN) riboswitch is an emerging target for the development of novel RNA-targeting antibiotics. We previously discovered an FMN…”
Get full text

Synthesis and biochemical evaluation of the CBI-PDE-I-dimer, a benzannelated analog of (+)-CC-1065 that also produces delayed toxicity in mice by Aristoff, Paul A, Johnson, Paul D, Sun, Daekyu, Hurley, Laurence H

“…A practical synthesis of CBI (2) was developed and applied to the synthesis of benzannelated analogs of CC-1065, including CBI-PDE-I-dimer (13) and…”
Get full text

Practical synthesis of 6a-carbaprostaglandin I2 by Aristoff, Paul A

Get full text

Reductive aromatization of quinols. New convenient methods for the regiospecific synthesis of p-hydroxy C-aryl glycals by Parker, Kathlyn A, Coburn, Craig A, Johnson, Paul D, Aristoff, Paul

Get full text

Coupling of cyclopropapyrroloindole (CPI) derivatives. The preparation of CC-1065, ent-CC-1065, and analogs by Kelly, Robert C, Gebhard, Ilse, Wicnienski, Nancy, Aristoff, Paul A, Johnson, Paul D, Martin, David G

Get full text

General procedure for the synthesis of o-aminophenylacetates by a modification of the Gassman reaction by Johnson, Paul D, Aristoff, Paul A

Get full text

Total synthesis of a novel antiulcer agent via a modification of the intramolecular Wadsworth-Emmons-Wittig reaction by Aristoff, Paul A, Johnson, Paul D, Harrison, Allen W

Get full text

Interstrand DNA cross-linking with dimers of the spirocyclopropyl alkylating moiety of CC-1065 by Mitchell, Mark A, Johnson, Paul D, Williams, Marta G, Aristoff, Paul A

“…The cytotoxicity of a number of clinically useful antitumor alkylating agents is often attributed to interstrand cross-linking of cellular DNA. CC-1065, a…”
Get full text