Search Results - "Girijavallabhan, Viyyoor"

Discovery of (1R,5S)-N-[3-Amino-1-(cyclobutylmethyl)-2,3-dioxopropyl]- 3-[2(S)-[[[(1,1-dimethylethyl)amino]carbonyl]amino]-3,3-dimethyl-1-oxobutyl]- 6,6-dimethyl-3-azabicyclo[3.1.0]hexan-2(S)-carboxamide (SCH 503034), a Selective, Potent, Orally Bioavailable Hepatitis C Virus NS3 Protease Inhibitor:  A Potential Therapeutic Agent for the Treatment of Hepatitis C Infection by Venkatraman, Srikanth, Bogen, Stéphane L, Arasappan, Ashok, Bennett, Frank, Chen, Kevin, Jao, Edwin, Liu, Yi-Tsung, Lovey, Raymond, Hendrata, Siska, Huang, Yuhua, Pan, Weidong, Parekh, Tejal, Pinto, Patrick, Popov, Veljko, Pike, Russel, Ruan, Sumei, Santhanam, Bama, Vibulbhan, Bancha, Wu, Wanli, Yang, Weiying, Kong, Jianshe, Liang, Xiang, Wong, Jesse, Liu, Rong, Butkiewicz, Nancy, Chase, Robert, Hart, Andrea, Agrawal, Sony, Ingravallo, Paul, Pichardo, John, Kong, Rong, Baroudy, Bahige, Malcolm, Bruce, Guo, Zhuyan, Prongay, Andrew, Madison, Vincent, Broske, Lisa, Cui, Xiaoming, Cheng, Kuo-Chi, Hsieh, Yunsheng, Brisson, Jean-Marc, Prelusky, Danial, Korfmacher, Walter, White, Ronald, Bogdanowich-Knipp, Susan, Pavlovsky, Anastasia, Bradley, Prudence, Saksena, Anil K, Ganguly, Ashit, Piwinski, John, Girijavallabhan, Viyyoor, Njoroge, F. George

“…Hepatitis C virus (HCV) infection is the major cause of chronic liver disease, leading to cirrhosis and hepatocellular carcinoma, which affects more than 170…”
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New class of azaheptapyridine FPT inhibitors as potential cancer therapy agents by Zhu, Hugh Y, Desai, Jagdish, Cooper, Alan B, Wang, James, Rane, Dinananth F, Kirschmeier, Paul, Strickland, Corey, Liu, Ming, Nomeir, Amin A, Girijavallabhan, Viyyoor M

“…Tertiary hydroxyl class of C-imidazole bridgehead azaheptapyridine FPT inhibitors were prepared in an attempt to block in vivo oxidation of secondary hydroxyl…”
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Discovery of 2-Hydroxy-N,N-dimethyl-3-{2-[[(R)-1-(5- methylfuran-2-yl)propyl]amino]-3,4-dioxocyclobut-1-enylamino}benzamide (SCH 527123):  A Potent, Orally Bioavailable CXCR2/CXCR1 Receptor Antagonist by Dwyer, Michael P, Yu, Younong, Chao, Jianping, Aki, Cynthia, Chao, Jianhua, Biju, Purakkattle, Girijavallabhan, Viyyoor, Rindgen, Diane, Bond, Richard, Mayer-Ezel, Rosemary, Jakway, James, Hipkin, R. William, Fossetta, James, Gonsiorek, Waldemar, Bian, Hong, Fan, Xuedong, Terminelli, Carol, Fine, Jay, Lundell, Daniel, Merritt, J. Robert, Rokosz, Laura L, Kaiser, Bernd, Li, Ge, Wang, Wei, Stauffer, Tara, Ozgur, Lynne, Baldwin, John, Taveras, Arthur G

“…Structure−activity studies on lead cyclobutenedione 3 led to the discovery of 4 (SCH 527123), a potent, orally bioavailable CXCR2/CXCR1 receptor antagonist…”
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Discovery of Narlaprevir (SCH 900518): A Potent, Second Generation HCV NS3 Serine Protease Inhibitor by Arasappan, Ashok, Bennett, Frank, Bogen, Stephane L, Venkatraman, Srikanth, Blackman, Melissa, Chen, Kevin X, Hendrata, Siska, Huang, Yuhua, Huelgas, Regina M, Nair, Latha, Padilla, Angela I, Pan, Weidong, Pike, Russell, Pinto, Patrick, Ruan, Sumei, Sannigrahi, Mousumi, Velazquez, Francisco, Vibulbhan, Bancha, Wu, Wanli, Yang, Weiying, Saksena, Anil K, Girijavallabhan, Viyyoor, Shih, Neng-Yang, Kong, Jianshe, Meng, Tao, Jin, Yan, Wong, Jesse, McNamara, Paul, Prongay, Andrew, Madison, Vincent, Piwinski, John J, Cheng, Kuo-Chi, Morrison, Richard, Malcolm, Bruce, Tong, Xiao, Ralston, Robert, Njoroge, F. George

“…Boceprevir (SCH 503034), 1, a novel HCV NS3 serine protease inhibitor discovered in our laboratories, is currently undergoing phase III clinical trials…”
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Potent inhibitors of HCV-NS3 protease derived from boronic acids by Venkatraman, Srikanth, Wu, Wanli, Prongay, Andrew, Girijavallabhan, Viyyoor, George Njoroge, F.

“…Chronic hepatitis C infection is the leading causes for cirrhosis of the liver and hepatocellular carcinoma, leading to liver failure and liver…”
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The introduction of P4 substituted 1-methylcyclohexyl groups into Boceprevir®: A change in direction in the search for a second generation HCV NS3 protease inhibitor by Bennett, Frank, Huang, Yuhua, Hendrata, Siska, Lovey, Raymond, Bogen, Stephane L., Pan, Weidong, Guo, Zhuyan, Prongay, Andrew, Chen, Kevin X., Arasappan, Ashok, Venkatraman, Srikanth, Velazquez, Francisco, Nair, Latha, Sannigrahi, Mousumi, Tong, Xiao, Pichardo, John, Cheng, Kuo-Chi, Girijavallabhan, Viyyoor M., Saksena, Anil K., Njoroge, F. George

“…In the search for a second generation HCV protease inhibitor, molecular modeling studies of the X-ray crystal structure of Boceprevir® 1 bound to the NS3…”
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Antitumor activity of SCH 66336, an orally bioavailable tricyclic inhibitor of farnesyl protein transferase, in human tumor xenograft models and Wap-ras transgenic mice by MING LIU, BRYANT, M. S, DELL, J, SINHA, D, SYED, J, KORFMACHER, W. A, NOMEIR, A. A, LIN, C.-C, WANG, L, TAVERAS, A. G, DOLL, R. J, NJOROGE, F. G, JIANPING CHEN, MALLAMS, A. K, REMISZEWSKI, S, CATINO, J. J, GIRIJAVALLABHAN, V. M, KIRSCHMEIER, P, BISHOP, W. R, SUINING LEE, YAREMKO, B, LIPARI, P, MALKOWSKI, M, FERRARI, E, NIELSEN, L, PRIOLI, N

“…We have been developing a series of nonpeptidic, small molecule farnesyl protein transferase inhibitors that share a common tricyclic nucleus and compete with…”
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Discovery of C-imidazole azaheptapyridine FPT inhibitors by Zhu, Hugh Y., Cooper, Alan B., Desai, Jagdish, Njoroge, George, Kirschmeier, Paul, Bishop, W. Robert, Strickland, Corey, Hruza, Alan, Doll, Ronald J., Girijavallabhan, Viyyoor M.

“…The discovery of C-linked imidazole azaheptapyridine bridgehead FPT inhibitors is described. This novel class of compounds are sub nM FPT enzyme inhibitors…”
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Design and Synthesis of Depeptidized Macrocyclic Inhibitors of Hepatitis C NS3-4A Protease Using Structure-Based Drug Design by Venkatraman, Srikanth, Njoroge, F. George, Girijavallabhan, Viyyoor M, Madison, Vincent S, Yao, Nanua H, Prongay, Andrew J, Butkiewicz, Nancy, Pichardo, John

“…Hepatitus C virus (HCV) NS3, when bound to NS-4A cofactor, facilitates development of mature virons by catalyzing cleavage of a polyprotein to form functional…”
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Enzymatic Kinetic Resolution of Piperidine Atropisomers:  Synthesis of a Key Intermediate of the Farnesyl Protein Transferase Inhibitor, SCH66336 by Morgan, Brian, Zaks, Aleksey, Dodds, David R, Liu, Jinchu, Jain, Rama, Megati, Sreeni, Njoroge, F. George, Girijavallabhan, Viyyoor M

“…The resolution of secondary amines via enzyme-catalyzed acylation is a relatively rare process. The kinetic resolution of a series of intermediates of SCH66336…”
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Mass spectrometric studies of potent inhibitors of farnesyl protein transferase--detection of pentameric noncovalent complexes by Mirza, Urooj A, Chen, Guodong, Liu, Yan-Hui, Doll, Ronald J, Girijavallabhan, Viyyoor M, Ganguly, Ashit K, Pramanik, Birendra N

“…Farnesyl protein transferase (FPT) inhibition is an interesting and promising approach to noncytotoxic anticancer therapy. Research in this area has resulted…”
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Hydroxylated analogues of the orally active broad spectrum antifungal, Sch 51048 ( 1), and the discovery of posaconazole [Sch 56592; 2 or ( S, S)- 5] by Bennett, Frank, Saksena, Anil K., Lovey, Raymond G., Liu, Yi-Tsung, Patel, Naginbhai M., Pinto, Patrick, Pike, Russel, Jao, Edwin, Girijavallabhan, Viyyoor M., Ganguly, Ashit K., Loebenberg, David, Wang, Haiyan, Cacciapuoti, Anthony, Moss, Eugene, Menzel, Fred, Hare, Roberta S., Nomeir, Amin

“…As part of a detailed study, the syntheses, biological activities, and pharmacokinetic properties of hydroxylated analogues of the previously described broad…”
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(+)-4-[2-[4-(8-Chloro-3,10-dibromo-6,11-dihydro-5H-benzo[5,6]cyclohepta[1,2-b]- pyridin-11(R)-yl)-1-piperidinyl]-2-oxo-ethyl]-1-piperidinecarboxamide (SCH-66336):  A Very Potent Farnesyl Protein Transferase Inhibitor as a Novel Antitumor Agent by Njoroge, F. George, Taveras, Arthur G, Kelly, Joseph, Remiszewski, Stacy, Mallams, Alan K, Wolin, Ronald, Afonso, Adriano, Cooper, Alan B, Rane, Dinananth F, Liu, Yi-Tsung, Wong, Jesse, Vibulbhan, Bancha, Pinto, Patrick, Deskus, Jeffrey, Alvarez, Carmen S, del Rosario, Joycelyn, Connolly, Michael, Wang, James, Desai, Jagdish, Rossman, Randall R, Bishop, W. Robert, Patton, Robert, Wang, Lynn, Kirschmeier, Paul, Bryant, Mathew S, Nomeir, Amin A, Lin, C.-C, Liu, Ming, McPhail, Andrew T, Doll, Ronald J, Girijavallabhan, Viyyoor M, Ganguly, Ashit K

“…We have previously shown that appropriate modification of the benzocycloheptapyridine tricyclic ring system can provide potent farnesyl protein transferase…”
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Tricyclic Farnesyl Protein Transferase Inhibitors:  Crystallographic and Calorimetric Studies of Structure−Activity Relationships by Strickland, Corey L, Weber, Patricia C, Windsor, William T, Wu, Zhen, Le, Hung V, Albanese, Margaret M, Alvarez, Carmen S, Cesarz, David, del Rosario, Joycelyn, Deskus, Jeffrey, Mallams, Alan K, Njoroge, F. George, Piwinski, John J, Remiszewski, Stacy, Rossman, Randall R, Taveras, Arthur G, Vibulbhan, Bancha, Doll, Ronald J, Girijavallabhan, Viyyoor M, Ganguly, Ashit K

“…Crystallographic and thermodynamic studies of farnesyl protein transferase (FPT) complexed with novel tricyclic inhibitors provide insights into the observed…”
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A Convenient Synthesis of Cis and Trans 4-tert-Butoxycarbonyl-Substituted Cyclohexylglycine by Venkatraman, Srikanth, Njoroge, F. George, Girijavallabhan, Viyyoor, McPhail, Andrew T

“…A novel synthesis of cis and trans substituted 4-tert-butoxycarbonyl cyclohexylglycines via asymmetric aminohydroxylation of vinyl styrene followed by…”
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Concise asymmetric routes to 2,2,4-trisubstituted tetrahydrofurans via chiral titanium imide enolates: Key intermediates towards synthesis of highly active azole antifungals SCH 51048 and SCH 56592 by Saksena, Anil K, Girijavallabhan, Viyyoor M, Wang, Haiyan, Liu, Yi-Tsung, Pike, Russel E, Ganguly, Ashit K

“…Two complimentary approaches to the key (−)-(2 R)-cis-tosylate 1 and its (+)-(2S)-enantiomer 15 via generation of chiral imide enolates having a…”
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Interaction of a Novel GDP Exchange Inhibitor with the Ras Protein by Ganguly, Ashit K, Wang, Yu-Sen, Pramanik, Birendra N, Doll, Ronald J, Snow, Mark E, Taveras, Arthur G, Remiszewski, Stacy, Cesarz, David, del Rosario, J, Vibulbhan, Bancha, Brown, Joan E, Kirschmeier, Paul, Huang, Eric C, Heimark, Larry, Tsarbopoulos, Anthony, Girijavallabhan, Viyyoor M, Aust, Robert M, Brown, Edward L, DeLisle, Dorothy M, Fuhrman, Shella A, Hendrickson, Thomas F, Kissinger, Charles R, Love, Robert A, Sisson, Wess A, Villafranca, J. Ernest, Webber, Steve E

“…Mutated, tumorigenic Ras is present in a variety of human tumors. Compounds that inhibit tumorigenic Ras function may be useful in the treatment of Ras-related…”
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Synthesis and antifungal activity of the 2,2,5-tetrahydrofuran regioisomers of SCH 51048 by Lovey, Raymond G, Saksena, Anil K, Girijavallabhan, Viyyoor M, Blundell, Paul, Guzik, Henry, Loebenberg, David, Parmegiani, Raulo M, Cacciapuoti, Anthony

“…The four 2,2,5-regioisomer counterparts of SCH 51048 were synthesized and evaluated. As with the parent series, only the two cis isomers possessed any in vitro…”
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Identification of Pharmacokinetically Stable 3,10-Dibromo-8-chlorobenzocycloheptapyridine Farnesyl Protein Transferase Inhibitors with Potent Enzyme and Cellular Activities by Taveras, Arthur G, Deskus, Jeff, Chao, Jianping, Vaccaro, Cynthia J, Njoroge, F. George, Vibulbhan, Bancha, Pinto, Pat, Remiszewski, Stacy, del Rosario, Jocelyn, Doll, Ronald J, Alvarez, Carmen, Lalwani, Tarik, Mallams, Alan K, Rossman, Randall R, Afonso, Adriano, Girijavallabhan, Viyyoor M, Ganguly, Ashit K, Pramanik, Birendra, Heimark, Larry, Bishop, W. Robert, Wang, Lynn, Kirschmeier, Paul, James, Linda, Carr, Donna, Patton, Robert, Bryant, Mathew S, Nomeir, Amin A, Liu, Ming

“…Farnesyl protein transferase (FPT) is a promising target for the development of cancer chemotherapeutics because it is responsible for the farnesylation of…”
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Inhibitors of Farnesyl Protein Transferase. 4-Amido, 4-Carbamoyl, and 4-Carboxamido Derivatives of 1-(8-Chloro-6,11-dihydro-5H-benzo[5,6]- cyclohepta[1,2-b]pyridin-11-yl)piperazine and 1-(3-Bromo-8-chloro-6,11- dihydro-5H-benzo[5,6]cyclohepta[1,2-b]pyridin-11-yl)piperazine by Mallams, Alan K, Rossman, Randall R, Doll, Ronald J, Girijavallabhan, Viyyoor M, Ganguly, Ashit K, Petrin, Joanne, Wang, Lynn, Patton, Robert, Bishop, W. Robert, Carr, Donna M, Kirschmeier, Paul, Catino, Joseph J, Bryant, Matthew S, Chen, Kwang-Jong, Korfmacher, Walter A, Nardo, Cymbelene, Wang, Shiyong, Nomeir, Amin A, Lin, Chin-Chung, Li, Zujun, Chen, Jianping, Lee, Suining, Dell, Janet, Lipari, Philip, Malkowski, Michael, Yaremko, Bodan, King, Ivan, Liu, Ming

“…The synthesis of a variety of novel 4-amido, 4-carbamoyl and 4-carboxamido derivatives of…”
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