Discovery and Preclinical Pharmacology of an Oral Bromodomain and Extra-Terminal (BET) Inhibitor Using Scaffold-Hopping and Structure-Guided Drug Design
Gavai, Ashvinikumar V, Norris, Derek, Delucca, George, Tortolani, David, Tokarski, John S, Dodd, Dharmpal, O’Malley, Daniel, Zhao, Yufen, Quesnelle, Claude, Gill, Patrice, Vaccaro, Wayne, Huynh, Tram, Ahuja, Vijay, Han, Wen-Ching, Mussari, Christopher, Harikrishnan, Lalgudi, Kamau, Muthoni, Poss, Michael, Sheriff, Steven, Yan, Chunhong, Marsilio, Frank, Menard, Krista, Wen, Mei-Li, Rampulla, Richard, Wu, Dauh-Rurng, Li, Jianqing, Zhang, Huiping, Li, Peng, Sun, Dawn, Yip, Henry, Traeger, Sarah C, Zhang, Yingru, Mathur, Arvind, Zhang, Haiying, Huang, Christine, Yang, Zheng, Ranasinghe, Asoka, Everlof, Gerry, Raghavan, Nirmala, Tye, Ching Kim, Wee, Susan, Hunt, John T, Vite, Gregory, Westhouse, Richard, Lee, Francis Y
Published in Journal of medicinal chemistry (14.10.2021)
Published in Journal of medicinal chemistry (14.10.2021)
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Development of BET inhibitors as potential treatments for cancer: A search for structural diversity
Hill, Matthew D., Fang, Haiquan, Tokarski, John, Fanslau, Carolynn, Haarhoff, Zuzana, Huang, Christine, Kramer, Melissa, Menard, Krista, Monereau, Laura, Morrison, John, Ranasinghe, Asoka, Shields, Eric E., Tye, Ching Kim, Westhouse, Richard, Everlof, Gerry, Sheriff, Steven, Yan, Chunhong, Marsilio, Frank, Zhang, Lisa, Zvyaga, Tatyana, Lee, Francis, Gavai, Ashvinikumar V., Degnan, Andrew P.
Published in Bioorganic & medicinal chemistry letters (15.07.2021)
Published in Bioorganic & medicinal chemistry letters (15.07.2021)
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Journal Article
Development of BET inhibitors as potential treatments for cancer: A new carboline chemotype
Hill, Matthew D., Quesnelle, Claude, Tokarski, John, Fang, Haiquan, Fanslau, Carolynn, Haarhoff, Zuzana, Kramer, Melissa, Madari, Shilpa, Wiebesiek, Amy, Morrison, John, Simmermacher-Mayer, Jean, Sinz, Michael, Westhouse, Richard, Xie, Chunshan, Zhao, Jiuqiao, Huang, Lisa, Sheriff, Steven, Yan, Chunhong, Marsilio, Frank, Everlof, Gerry, Zvyaga, Tatyana, Lee, Francis, Gavai, Ashvinikumar V., Degnan, Andrew P.
Published in Bioorganic & medicinal chemistry letters (01.11.2021)
Published in Bioorganic & medicinal chemistry letters (01.11.2021)
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Journal Article
Development of BET Inhibitors as Potential Treatments for Cancer: Optimization of Pharmacokinetic Properties
Hill, Matthew D., Fang, Haiquan, Norris, Derek, Delucca, George V., Huang, Hong, DeBenedetto, Mikkel, Quesnelle, Claude, Schmitz, William D., Tokarski, John S., Sheriff, Steven, Yan, Chunhong, Fanslau, Caroline, Haarhoff, Zuzana, Huang, Christine, Kramer, Melissa, Madari, Shilpa, Menard, Krista, Monereau, Laura, Morrison, John, Raghavan, Nirmala, Shields, Eric E., Simmermacher-Mayer, Jean, Sinz, Michael, Tye, Ching Kim, Westhouse, Richard, Xie, Chunshan, Zhang, Haiying, Zhang, Lisa, Zvyaga, Tatyana, Lee, Francis, Gavai, Ashvinikumar V., Degnan, Andrew P.
Published in ACS medicinal chemistry letters (14.07.2022)
Published in ACS medicinal chemistry letters (14.07.2022)
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Journal Article
Crystallization-Induced Dynamic Resolution toward the Synthesis of (S)‑7-Amino‑5H,7H‑dibenzo[b,d]‑azepin-6-one: An Important Scaffold for γ‑Secretase Inhibitors
Karmakar, Sukhen, Byri, Vijay, Gavai, Ashvinikumar V, Rampulla, Richard, Mathur, Arvind, Gupta, Anuradha
Published in Organic process research & development (21.10.2016)
Published in Organic process research & development (21.10.2016)
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Journal Article
A Practical Approach for Enantio- and Diastereocontrol in the Synthesis of 2,3-Disubstituted Succinic Acid Esters: Synthesis of the pan-Notch Inhibitor BMS-906024
Quesnelle, Claude A., Gill, Patrice, Kim, Soong-Hoon, Chen, Libing, Zhao, Yufen, Fink, Brian E., Saulnier, Mark, Frennesson, David, DeMartino, Michael P., Baran, Phil S., Gavai, Ashvinikumar V.
Published in Synlett (19.09.2016)
Published in Synlett (19.09.2016)
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Journal Article
Discovery of Clinical Candidate BMS-906024: A Potent Pan-Notch Inhibitor for the Treatment of Leukemia and Solid Tumors
Gavai, Ashvinikumar V, Quesnelle, Claude, Norris, Derek, Han, Wen-Ching, Gill, Patrice, Shan, Weifang, Balog, Aaron, Chen, Ke, Tebben, Andrew, Rampulla, Richard, Wu, Dauh-Rurng, Zhang, Yingru, Mathur, Arvind, White, Ronald, Rose, Anne, Wang, Haiqing, Yang, Zheng, Ranasinghe, Asoka, D’Arienzo, Celia, Guarino, Victor, Xiao, Lan, Su, Ching, Everlof, Gerry, Arora, Vinod, Shen, Ding Ren, Cvijic, Mary Ellen, Menard, Krista, Wen, Mei-Li, Meredith, Jere, Trainor, George, Lombardo, Louis J, Olson, Richard, Baran, Phil S, Hunt, John T, Vite, Gregory D, Fischer, Bruce S, Westhouse, Richard A, Lee, Francis Y
Published in ACS medicinal chemistry letters (14.05.2015)
Published in ACS medicinal chemistry letters (14.05.2015)
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Journal Article
Discovery of Novel TLR7 Agonists as Systemic Agent for Combination With aPD1 for Use in Immuno-oncology
Poudel, Yam B., He, Liqi, Cox, Matthew, Zhang, Qian, Johnson, Walter L., Cong, Qiang, Cheng, Heng, Chowdari, Naidu S., Tarby, Christine, Donnell, Andrew F., Broekema, Matthais, O’Malley, Daniel P., Zhang, Yong, A. M. Subbaiah, Murugaiah, Kumar, Boda Vijay, Subramani, Lakshumanan, Wang, Bei, Li, Yi-Xin, Sivaprakasam, Prasanna, Critton, David, Mulligan, Dawn, Sandhu, Bhupindar, Xie, Chunshan, Ramakrishnan, Radha, Nagar, Jignesh, Dudhgaonkar, Shailesh, Oderinde, Martins S., Murtaza, Anwar, Schieven, Gary L., Mathur, Arvind, Gavai, Ashvinikumar V., Vite, Gregory, Gangwar, Sanjeev
Published in ACS medicinal chemistry letters (08.02.2024)
Published in ACS medicinal chemistry letters (08.02.2024)
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Journal Article
Discovery of Pyridazinone and Pyrazolo[1,5‑a]pyridine Inhibitors of C‑Terminal Src Kinase
O’Malley, Daniel P, Ahuja, Vijay, Fink, Brian, Cao, Carolyn, Wang, Cindy, Swanson, Jesse, Wee, Susan, Gavai, Ashvinikumar V, Tokarski, John, Critton, David, Paiva, Anthony A, Johnson, Benjamin M, Szapiel, Nicolas, Xie, Dianlin
Published in ACS medicinal chemistry letters (10.10.2019)
Published in ACS medicinal chemistry letters (10.10.2019)
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Journal Article
Identification and Optimization of Small Molecule Pyrazolopyrimidine TLR7 Agonists for Applications in Immuno-oncology
He, Liqi, Zhang, Meng Yao, Cox, Matthew, Zhang, Qian, Donnell, Andrew F., Zhang, Yong, Tarby, Christine, Gill, Patrice, Subbaiah, Murugaiah A. M., Ramar, Thangeswaran, Reddy, Maheswara, Puttapaka, Vijaya, Li, Yi-Xin, Sivaprakasam, Prasanna, Critton, David, Mulligan, Dawn, Xie, Chunshan, Ramakrishnan, Radha, Nagar, Jignesh, Dudhgaonkar, Shailesh, Murtaza, Anwar, Oderinde, Martins S., Schieven, Gary L., Mathur, Arvind, Gavai, Ashvinikumar V., Vite, Gregory, Gangwar, Sanjeev, Poudel, Yam B.
Published in ACS medicinal chemistry letters (08.02.2024)
Published in ACS medicinal chemistry letters (08.02.2024)
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Journal Article
[2.2.1]-Bicyclic sultams as potent androgen receptor antagonists
Shan, Weifang, Balog, Aaron, Nation, Andrew, Zhu, Xiao, Chen, Jing, Cvijic, Mary Ellen, Geng, Jieping, Rizzo, Cheryl A., Spires, Thomas, Attar, Ricardo M., Obermeier, Mary, Traeger, Sarah, Dai, Jun, Zhang, Yingru, Galella, Michael, Trainor, George, Vite, Gregory D., Gavai, Ashvinikumar V.
Published in Bioorganic & medicinal chemistry letters (01.12.2016)
Published in Bioorganic & medicinal chemistry letters (01.12.2016)
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Journal Article
Preclinical Antitumor Activity of BMS-599626, a pan-HER Kinase Inhibitor That Inhibits HER1/HER2 Homodimer and Heterodimer Signaling
WONG, Tai W, LEE, Francis Y, GAVAI, Ashvinikumar V, VITE, Gregory D, YU, Chiang, LUO, Feng R, OPPENHEIMER, Simone, HONGJIAN ZHANG, SMYKLA, Richard A, MASTALERZ, Harold, FINK, Brian E, HUNT, John T
Published in Clinical cancer research (15.10.2006)
Published in Clinical cancer research (15.10.2006)
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Journal Article
BMS-871: A novel orally active pan-Notch inhibitor as an anticancer agent
Shan, Weifang, Balog, Aaron, Quesnelle, Claude, Gill, Patrice, Han, Wen-Ching, Norris, Derek, Mandal, Sunilkumar, Thiruvenkadam, Raja, Gona, Kiran Babu, Thiyagarajan, Kamalraj, Kandula, Sathiah, McGlinchey, Kelly, Menard, Krista, Wen, Mei-Li, Rose, Anne, White, Ronald, Guarino, Victor, Shen, Ding Ren, Cvijic, Mary Ellen, Ranasinghe, Asoka, Dai, Jun, Zhang, Yingru, Wu, Dauh-Rurng, Mathur, Arvind, Rampulla, Richard, Trainor, George, Hunt, John T., Vite, Gregory D., Westhouse, Richard, Lee, Francis Y., Gavai, Ashvinikumar V.
Published in Bioorganic & medicinal chemistry letters (01.05.2015)
Published in Bioorganic & medicinal chemistry letters (01.05.2015)
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Journal Article
Novel pyrrolo[2,1- f][1,2,4]triazin-4-amines: Dual inhibitors of EGFR and HER2 protein tyrosine kinases
Fink, Brian E., Norris, Derek, Mastalerz, Harold, Chen, Ping, Goyal, Bindu, Zhao, Yufen, Kim, Soong-Hoon, Vite, Gregory D., Lee, Francis Y., Zhang, Hongjian, Oppenheimer, Simone, Tokarski, John S., Wong, Tai W., Gavai, Ashvinikumar V.
Published in Bioorganic & medicinal chemistry letters (15.01.2011)
Published in Bioorganic & medicinal chemistry letters (15.01.2011)
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Journal Article
Discovery and Preclinical Evaluation of [4-[[1-(3-fluorophenyl)methyl]-1H-indazol-5-ylamino]-5-methylpyrrolo[2,1-f][1,2,4]triazin-6-yl]carbamic Acid, (3S)-3-Morpholinylmethyl Ester (BMS-599626), a Selective and Orally Efficacious Inhibitor of Human Epidermal Growth Factor Receptor 1 and 2 Kinases
Gavai, Ashvinikumar V, Fink, Brian E, Fairfax, David J, Martin, Gregory S, Rossiter, Lana M, Holst, Christian L, Kim, Soong-Hoon, Leavitt, Kenneth J, Mastalerz, Harold, Han, Wen-Ching, Norris, Derek, Goyal, Bindu, Swaminathan, Shankar, Patel, Bharat, Mathur, Arvind, Vyas, Dolatrai M, Tokarski, John S, Yu, Chiang, Oppenheimer, Simone, Zhang, Hongjian, Marathe, Punit, Fargnoli, Joseph, Lee, Francis Y, Wong, Tai W, Vite, Gregory D
Published in Journal of medicinal chemistry (12.11.2009)
Published in Journal of medicinal chemistry (12.11.2009)
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Journal Article
Identification of a novel series of tetrahydrodibenzazocines as inhibitors of 17β-hydroxysteroid dehydrogenase type 3
Fink, Brian E., Gavai, Ashvinikumar V., Tokarski, John S., Goyal, Bindu, Misra, Raj, Xiao, Hai-Yun, Kimball, S. David, Han, Wen-Ching, Norris, Derek, Spires, Thomas E., You, Dan, Gottardis, Marco M., Lorenzi, Matthew V., Vite, Gregory D.
Published in Bioorganic & medicinal chemistry letters (15.03.2006)
Published in Bioorganic & medicinal chemistry letters (15.03.2006)
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Journal Article
A 3D-QSAR model for CYP2D6 inhibition in the aryloxypropanolamine series
Vaz, Roy J., Nayeem, Akbar, Santone, Kenneth, Chandrasena, Gamini, Gavai, Ashvinikumar V.
Published in Bioorganic & medicinal chemistry letters (01.09.2005)
Published in Bioorganic & medicinal chemistry letters (01.09.2005)
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Journal Article
Discovery of novel 1-arylmethyl pyrrolidin-2-yl ethanol amines as calcium-sensing receptor antagonists
Gavai, Ashvinikumar V., Vaz, Roy J., Mikkilineni, Amarendra B., Roberge, Jacques Y., Liu, Yalei, Lawrence, R. Michael, Corte, James R., Yang, Wu, Bednarz, Mark, Dickson, John K., Ma, Zhengping, Seethala, Ramakrishna, Feyen, Jean H.M.
Published in Bioorganic & medicinal chemistry letters (15.12.2005)
Published in Bioorganic & medicinal chemistry letters (15.12.2005)
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Journal Article
Pyrrolotriazine-5-carboxylate ester inhibitors of EGFR and HER2 protein tyrosine kinases and a novel one-pot synthesis of C-4 subsitituted pyrrole-2,3-dicarboxylate diesters
Mastalerz, Harold, Gavai, Ashvinikumar V, Fink, Brian, Struzynski, Charles, Tarrant, James, Vite, Gregory D, Wong, Tai W, Zhang, Guifen, Vyas, Dolatrai M
Published in Canadian journal of chemistry (01.04.2006)
Published in Canadian journal of chemistry (01.04.2006)
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Journal Article
Abstract 1742: Inhibition of BET signaling leads to reversible GATA1-associated repression of hematopoietic progenitors: translation from preclinical assessment to clinical development
Zhang, Cindy, Xu, Ke, Panzica-Kelly, Julie, Price, Jennifer, Bounous, Denise, Coker, Shodeinde, Unsal-Kacmaz, Kezi, Greenawalt, Danielle, Gavai, Ashvinikumar, Fleming, Ronald, Augustine-Rauch, Karen, Westhouse, Richard
Published in Cancer research (Chicago, Ill.) (15.08.2020)
Published in Cancer research (Chicago, Ill.) (15.08.2020)
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