Search Results - "Huang, Buwen"

Discovery of PF-06873600, a CDK2/4/6 Inhibitor for the Treatment of Cancer by Freeman-Cook, Kevin D, Hoffman, Robert L, Behenna, Douglas C, Boras, Britton, Carelli, Jordan, Diehl, Wade, Ferre, Rose Ann, He, You-Ai, Hui, Andrea, Huang, Buwen, Huser, Nanni, Jones, Rhys, Kephart, Susan E, Lapek, John, McTigue, Michele, Miller, Nichol, Murray, Brion W, Nagata, Asako, Nguyen, Lisa, Niessen, Sherry, Ninkovic, Sacha, O’Doherty, Inish, Ornelas, Martha A, Solowiej, James, Sutton, Scott C, Tran, Khanh, Tseng, Elaine, Visswanathan, Ravi, Xu, Meirong, Zehnder, Luke, Zhang, Qin, Zhang, Cathy, Dann, Stephen

“…Control of the cell cycle through selective pharmacological inhibition of CDK4/6 has proven beneficial in the treatment of breast cancer. Extending this level…”
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Design and Synthesis of Pyridone-Containing 3,4-Dihydroisoquinoline-1(2H)‑ones as a Novel Class of Enhancer of Zeste Homolog 2 (EZH2) Inhibitors by Kung, Pei-Pei, Rui, Eugene, Bergqvist, Simon, Bingham, Patrick, Braganza, John, Collins, Michael, Cui, Mei, Diehl, Wade, Dinh, Dac, Fan, Connie, Fantin, Valeria R, Gukasyan, Hovhannes J, Hu, Wenyue, Huang, Buwen, Kephart, Susan, Krivacic, Cody, Kumpf, Robert A, Li, Gary, Maegley, Karen A, McAlpine, Indrawan, Nguyen, Lisa, Ninkovic, Sacha, Ornelas, Martha, Ryskin, Michael, Scales, Stephanie, Sutton, Scott, Tatlock, John, Verhelle, Dominique, Wang, Fen, Wells, Peter, Wythes, Martin, Yamazaki, Shinji, Yip, Brian, Yu, Xiu, Zehnder, Luke, Zhang, Wei-Guo, Rollins, Robert A, Edwards, Martin

“…A new enhancer of zeste homolog 2 (EZH2) inhibitor series comprising a substituted phenyl ring joined to a dimethylpyridone moiety via an amide linkage has…”
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Chemogenetic evaluation of the mitotic kinesin CENP-E reveals a critical role in triple-negative breast cancer by Kung, Pei-Pei, Martinez, Ricardo, Zhu, Zhou, Zager, Michael, Blasina, Alessandra, Rymer, Isha, Hallin, Jill, Xu, Meirong, Carroll, Christopher, Chionis, John, Wells, Peter, Kozminski, Kirk, Fan, Jeffery, Guicherit, Oivin, Huang, Buwen, Cui, Mei, Liu, Chaoting, Huang, Zhongdong, Sistla, Anand, Yang, Jennifer, Murray, Brion W

“…Breast cancer patients with tumors lacking the three diagnostic markers (ER, PR, and HER2) are classified as triple-negative (primarily basal-like) and have…”
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Dihydroxyphenylisoindoline Amides as Orally Bioavailable Inhibitors of the Heat Shock Protein 90 (Hsp90) Molecular Chaperone by Kung, Pei-Pei, Huang, Buwen, Zhang, Gang, Zhou, Joe Zhongxiang, Wang, Jeff, Digits, Jennifer A, Skaptason, Judith, Yamazaki, Shinji, Neul, David, Zientek, Michael, Elleraas, Jeff, Mehta, Pramod, Yin, Min-Jean, Hickey, Michael J, Gajiwala, Ketan S, Rodgers, Caroline, Davies, Jay F, Gehring, Michael R

“…The discovery and optimization of potency and metabolic stability of a novel class of dihyroxyphenylisoindoline amides as Hsp90 inhibitors are presented…”
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Synthesis of Aryl Ethers via a Sulfonyl Transfer Reaction by Sach, Neal W, Richter, Daniel T, Cripps, Stephan, Tran-Dubé, Michelle, Zhu, Huichun, Huang, Buwen, Cui, Jean, Sutton, Scott C

“…A general synthesis of aryl ethers from primary and secondary alcohols and aryl mesylates is presented. The reaction proceeds via a sulfonyl-transfer…”
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Azaindole N-methyl hydroxamic acids as HIV-1 integrase inhibitors-II. The impact of physicochemical properties on ADME and PK by Tanis, Steven P., Plewe, Michael B., Johnson, Ted W., Butler, Scott L., Dalvie, Deepak, DeLisle, Dorothy, Dress, Klaus R., Hu, Qiyue, Huang, Buwen, Kuehler, Jon E., Kuki, Atsuo, Liu, Wen, Peng, Qinghai, Smith, Graham L., Solowiej, Jim, Tran, Khanh T., Wang, Hai, Yang, Anle, Yin, Chunfeng, Yu, Xiaoming, Zhang, Junhu, Zhu, Huichun

“…HIV-1 integrase is one of three enzymes encoded by the HIV genome and is essential for viral replication, and HIV-1 IN inhibitors have emerged as a new…”
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Methyl 3-[3-(ethoxycarbonyl)thioureido]-1H-pyrazole-5-carboxylate by Buwen Huang, Pei-Pei Kung, Arnold L. Rheingold, Antonio DiPasquale, Alex Yanovsky

“…The title compound, C9H12N4O4S, was proven to be the product of the reaction of methyl 5-amino-1H-pyrazole-3-carboxylate with ethyl isothiocyanatocarbonate…”
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A short asymmetric synthesis of methyl 2-((1S,3R)-3-((tert-butyldiphenylsilyl)oxy)cyclopentyl)acetate from norbornene by Huang, Buwen, Elleraas, Jeff, Ewanicki, Jason, Sutton, Scott C.

“…[Display omitted] •Pd-(S)-MOP catalyzed hydrosilation of norbornene gives modest dr (84:16, exo/endo)•(S)-MOP catalyzed hydrosilation of norbornene gives 99%ee…”
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Discovery of Novel Disaccharide Antibacterial Agents Using a Combinatorial Library Approach by Sofia, Michael J, Allanson, Nigel, Hatzenbuhler, Nicole T, Jain, Rakesh, Kakarla, Ramesh, Kogan, Natan, Liang, Rui, Liu, Dashan, Silva, Domingos J, Wang, Huiming, Gange, David, Anderson, Jan, Chen, Anna, Chi, Feng, Dulina, Richard, Huang, Buwen, Kamau, Muthoni, Wang, Chunguang, Baizman, Eugene, Branstrom, Arthur, Bristol, Neil, Goldman, Robert, Han, Kiho, Longley, Clifford, Midha, Sunita, Axelrod, Helena R

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Optimization of Orally Bioavailable Enhancer of Zeste Homolog 2 (EZH2) Inhibitors Using Ligand and Property-Based Design Strategies: Identification of Development Candidate (R)-5,8-Dichloro-7-(methoxy(oxetan-3-yl)methyl)-2-((4-methoxy-6-methyl-2-oxo-1,2-dihydropyridin-3-yl)methyl)-3,4-dihydroisoquinolin-1(2H)-one (PF-06821497) by Kung, Pei-Pei, Bingham, Patrick, Brooun, Alexei, Collins, Michael, Deng, Ya-Li, Dinh, Dac, Fan, Connie, Gajiwala, Ketan S, Grantner, Rita, Gukasyan, Hovhannes J, Hu, Wenyue, Huang, Buwen, Kania, Robert, Kephart, Susan E, Krivacic, Cody, Kumpf, Robert A, Khamphavong, Penney, Kraus, Manfred, Liu, Wei, Maegley, Karen A, Nguyen, Lisa, Ren, Shijian, Richter, Dan, Rollins, Robert A, Sach, Neal, Sharma, Shikhar, Sherrill, John, Spangler, Jillian, Stewart, Albert E, Sutton, Scott, Uryu, Sean, Verhelle, Dominique, Wang, Hui, Wang, Shuiwang, Wythes, Martin, Xin, Shuibo, Yamazaki, Shinji, Zhu, Huichun, Zhu, JinJiang, Zehnder, Luke, Edwards, Martin

“…A new series of lactam-derived EZH2 inhibitors was designed via ligand-based and physicochemical-property-based strategies to address metabolic stability and…”
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Design and Characterization of a Pyridone-Containing EZH2 Inhibitor Phosphate Prodrug by Kung, Pei-Pei, Fan, Connie, Gukasyan, Hovhannes J, Huang, Buwen, Kephart, Susan, Kraus, Manfred, Lee, Joseph H, Sutton, Scott C, Yamazaki, Shinji, Zehnder, Luke

“…A pyridone-derived phosphate prodrug of an enhancer of zeste homolog 2 (EZH2) inhibitor was designed and synthesized to improve the inhibitor’s aqueous…”
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Structure-Based Drug Design and Synthesis of PI3Kα-Selective Inhibitor (PF-06843195) by Cheng, Hengmiao, Orr, Suvi T M, Bailey, Simon, Brooun, Alexei, Chen, Ping, Deal, Judith G, Deng, Yali L, Edwards, Martin P, Gallego, Gary M, Grodsky, Neil, Huang, Buwen, Jalaie, Mehran, Kaiser, Stephen, Kania, Robert S, Kephart, Susan E, Lafontaine, Jennifer, Ornelas, Martha A, Pairish, Mason, Planken, Simon, Shen, Hong, Sutton, Scott, Zehnder, Luke, Almaden, Chau D, Bagrodia, Shubha, Falk, Matthew D, Gukasyan, Hovhannes J, Ho, Caroline, Kang, Xiaolin, Kosa, Rachel E, Liu, Ling, Spilker, Mary E, Timofeevski, Sergei, Visswanathan, Ravi, Wang, Zhenxiong, Meng, Fanxiu, Ren, Shijian, Shao, Li, Xu, Feng, Kath, John C

“…The phosphoinositide 3-kinase (PI3K)/mammalian target of rapamycin (mTOR) signaling pathway is a frequently dysregulated pathway in human cancer, and PI3Kα is…”
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Synthesis of oxetane-3-carboxaldehyde and methyl oxetane-3-carboxylate via homologation of oxetane-3-one by Kephart, Susan E., Zehnder, Luke R., Huang, Buwen, Sutton, Scott C.

“…A 4-pot telescoped procedure to prepare oxetane-3-carboxaldehyde and methyl oxetane-3-carboxylate was developed using readily available starting materials…”
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SAH derived potent and selective EZH2 inhibitors by Kung, Pei-Pei, Huang, Buwen, Zehnder, Luke, Tatlock, John, Bingham, Patrick, Krivacic, Cody, Gajiwala, Ketan, Diehl, Wade, Yu, Xiu, Maegley, Karen A.

“…[Display omitted] A series of novel enhancer of zeste homolog 2 (EZH2) inhibitors was designed based on the chemical structure of the histone methyltransferase…”
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Design strategies to target crystallographic waters applied to the Hsp90 molecular chaperone by Kung, Pei-Pei, Sinnema, Piet-Jan, Richardson, Paul, Hickey, Michael J., Gajiwala, Ketan S., Wang, Fen, Huang, Buwen, McClellan, Guy, Wang, Jeff, Maegley, Karen, Bergqvist, Simon, Mehta, Pramod P., Kania, Robert

“…A series of pyrrolopyrimines as Hsp90 inhibitor was discovered from a HTS hit using structure based design strategies. A series of novel and potent small…”
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Optimization of Potent, Selective, and Orally Bioavailable Pyrrolodinopyrimidine-Containing Inhibitors of Heat Shock Protein 90. Identification of Development Candidate 2-Amino-4-{4-chloro-2-[2-(4-fluoro-1H-pyrazol-1-yl)ethoxy]-6-methylphenyl}-N-(2,2-difluoropropyl)-5,7-dihydro-6H-pyrrolo[3,4-d]pyrimidine-6-carboxamide by Zehnder, Luke, Bennett, Michael, Meng, Jerry, Huang, Buwen, Ninkovic, Sacha, Wang, Fen, Braganza, John, Tatlock, John, Jewell, Tanya, Zhou, Joe Zhongxiang, Burke, Ben, Wang, Jeff, Maegley, Karen, Mehta, Pramod P, Yin, Min-Jean, Gajiwala, Ketan S, Hickey, Michael J, Yamazaki, Shinji, Smith, Evan, Kang, Ping, Sistla, Anand, Dovalsantos, Elena, Gehring, Michael R, Kania, Robert, Wythes, Martin, Kung, Pei-Pei

“…A novel class of heat shock protein 90 (Hsp90) inhibitors was discovered by high-throughput screening and was subsequently optimized using a combination of…”
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Correction to Design and Synthesis of Pyridone-Containing 3,4-Dihydroisoquinoline-1(2H)‑ones as a Novel Class of Enhancer of Zeste Homolog 2 (EZH2) Inhibitors by Kung, Pei-Pei, Rui, Eugene, Bergqvist, Simon, Bingham, Patrick, Braganza, John, Collins, Michael, Cui, Mei, Diehl, Wade, Dinh, Dac, Fan, Connie, Fantin, Valeria R, Gukasyan, Hovhannes J, Hu, Wenyue, Huang, Buwen, Kephart, Susan, Krivacic, Cody, Kumpf, Robert A, Li, Gary, Maegley, Karen A, McAlpine, Indrawan, Nguyen, Lisa, Ninkovic, Sacha, Ornelas, Martha, Ryskin, Michael, Scales, Stephanie, Sutton, Scott, Tatlock, John, Verhelle, Dominique, Wang, Fen, Wells, Peter, Wythes, Martin, Yamazaki, Shinji, Yip, Brian, Yu, Xiu, Zehnder, Luke, Zhang, Wei-Guo, Rollins, Robert A, Edwards, Martin

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2-(6-Bromo-3-pyridyl)-8-methylimidazo[1,2- a ]pyrazine by Huang, Buwen, Rui, Eugene, Wythes, Martin, Kung, Pei-Pei, Moore, Curtis, Rheingold, Arnold L., Yanovsky, Alex

“…The structure of the title compound, C12H9BrN4, prepared by the reaction of 2-bromo-1-(6-bromo-3-pyridyl)ethanone with 2-amino-3-methylpyrazine indicates that…”
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Optimization of Potent, Selective, and Orally Bioavailable Pyrrolodinopyrimidine-Containing Inhibitors of Heat Shock Protein 90. Identification of Development Candidate 2-Amino-4-{4-chloro-2-[2-(4-fluoro-1 H -pyrazol-1-yl)ethoxy]-6-methylphenyl}- N -(2,2-difluoropropyl)-5,7-dihydro-6 H -pyrrolo[3,4- d ]pyrimidine-6-carboxamide by Zehnder, Luke, Bennett, Michael, Meng, Jerry, Huang, Buwen, Ninkovic, Sacha, Wang, Fen, Braganza, John, Tatlock, John, Jewell, Tanya, Zhou, Joe Zhongxiang, Burke, Ben, Wang, Jeff, Maegley, Karen, Mehta, Pramod P., Yin, Min-Jean, Gajiwala, Ketan S., Hickey, Michael J., Yamazaki, Shinji, Smith, Evan, Kang, Ping, Sistla, Anand, Dovalsantos, Elena, Gehring, Michael R., Kania, Robert, Wythes, Martin, Kung, Pei-Pei

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Structure-based and property-compliant library design of 11β-HSD1 adamantyl amide inhibitors by Paderes, Genevieve D, Dress, Klaus, Huang, Buwen, Elleraas, Jeff, Rejto, Paul A, Pauly, Tom

“…Multiproperty lead optimization that satisfies multiple biological endpoints remains a challenge in the pursuit of viable drug candidates. Optimization of a…”
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