Search Results - "Zhu, Gui‐Dong"

Discovery of the Poly(ADP-ribose) Polymerase (PARP) Inhibitor 2-[(R)-2-methylpyrrolidin-2-yl]-1H-benzimidazole-4-carboxamide (ABT-888) for the Treatment of Cancer by Penning, Thomas D, Zhu, Gui-Dong, Gandhi, Viraj B, Gong, Jianchun, Liu, Xuesong, Shi, Yan, Klinghofer, Vered, Johnson, Eric F, Donawho, Cherrie K, Frost, David J, Bontcheva-Diaz, Velitchka, Bouska, Jennifer J, Osterling, Donald J, Olson, Amanda M, Marsh, Kennan C, Luo, Yan, Giranda, Vincent L

“…We have developed a series of cyclic amine-containing benzimidazole carboxamide PARP inhibitors with a methyl-substituted quaternary center at the point of…”
Get full text

ABT-888 Confers Broad In vivo Activity in Combination with Temozolomide in Diverse Tumors by PALMA, Joann P, WANG, Yi-Chun, ZHU, Gui-Dong, PENNING, Thomas D, GIRANDA, Vincent L, ROSENBERG, Saul H, FROST, David J, DONAWHO, Cherrie K, RODRIGUEZ, Luis E, MONTGOMERY, Debra, ELLIS, Paul A, BUKOFZER, Gail, NIQUETTE, Amanda, XUESONG LIU, YAN SHI, LASKO, Loren

“…Purpose: ABT-888, currently in phase 2 trials, is a potent oral poly(ADP-ribose) polymerase inhibitor that enhances the activity of multiple DNA-damaging…”
Get full text

Decreased Intrinsic Functional Connectivity of the Salience Network in Drug-Naïve Patients With Obsessive-Compulsive Disorder by Chen, Yun-Hui, Li, Su-Fang, Lv, Dan, Zhu, Gui-Dong, Wang, Yu-Hua, Meng, Xin, Hu, Qiang, Li, Cheng-Chong, Zhang, Liang-Tang, Chu, Xiang-Ping, Wang, Xiao-Ping, Li, Ping

“…Obsessive-compulsive disorder (OCD) patients have difficulty in switching between obsessive thought and compulsive behavior, which may be related to the…”
Get full text

Acquired Resistance to Combination Treatment with Temozolomide and ABT-888 Is Mediated by Both Base Excision Repair and Homologous Recombination DNA Repair Pathways by Liu, Xuesong, Han, Edward K, Anderson, Mark, Shi, Yan, Semizarov, Dimitri, Wang, Gang, McGonigal, Thomas, Roberts, Lisa, Lasko, Loren, Palma, Joann, Zhu, Gui-Dong, Penning, Thomas, Rosenberg, Saul, Giranda, Vincent L, Luo, Yan, Leverson, Joel, Johnson, Eric F, Shoemaker, Alexander R

“…Many established cancer therapies involve DNA-damaging chemotherapy or radiotherapy. Gain of DNA repair capacity of the tumor represents a common mechanism…”
Get full text

Targeting serine/threonine protein kinase B/Akt and cell-cycle checkpoint kinases for treating cancer by Li, Qun, Zhu, Gui-Dong

“…Over the past decade, protein kinases have emerged as a group of molecular targets with the potential to be "cancer-specific", allowing the selective targeting…”
Get more information

Potentiation of Temozolomide Cytotoxicity by Poly(ADP)Ribose Polymerase Inhibitor ABT-888 Requires a Conversion of Single-Stranded DNA Damages to Double-Stranded DNA Breaks by Liu, Xuesong, Shi, Yan, Guan, Ran, Donawho, Cherrie, Luo, Yanping, Palma, Joann, Zhu, Gui-Dong, Johnson, Eric F, Rodriguez, Luis E, Ghoreishi-Haack, Nayereh, Jarvis, Ken, Hradil, Vincent P, Colon-Lopez, Milagros, Cox, Bryan F, Klinghofer, Vered, Penning, Thomas, Rosenberg, Saul H, Frost, David, Giranda, Vincent L, Luo, Yan

“…Poly(ADP-ribose) polymerase (PARP) senses DNA breaks and facilitates DNA repair via the polyADP-ribosylation of various DNA binding and repair proteins. We…”
Get full text

The PARP Inhibitor, ABT-888 Potentiates Temozolomide: Correlation with Drug Levels and Reduction in PARP Activity In Vivo by PALMA, Joann P, RODRIGUEZ, Luis E, XUESONG LIU, OLSON, Amanda, SALTARELLI, Mary J, YAN SHI, STAVROPOULOS, Jason A, ZHU, Gui-Dong, PENNING, Thomas D, YAN LUO, GIRANDA, Vincent L, ROSENBERG, Saul H, BONTCHEVA-DIAZ, Velitchka D, FROST, David J, DONAWHO, Cherrie K, BOUSKA, Jennifer J, BUKOFZER, Gail, COLON-LOPEZ, Milagros, RAN GUAN, JARVIS, Kenneth, JOHNSON, Eric F, KLINGHOFER, Vered

“…ABT-888 is a potent, orally bioavailable PARP-1/-2 inhibitor shown to potentiate DNA damaging agents. The ability to potentiate temozolomide (TMZ) and develop…”
Get full text

Discovery and SAR of oxindole–pyridine-based protein kinase B/Akt inhibitors for treating cancers by Zhu, Gui-Dong, Gandhi, Viraj B., Gong, Jianchun, Luo, Yan, Liu, Xuesong, Shi, Yan, Guan, Ran, Magnone, Shayna R., Klinghofer, Vered, Johnson, Eric F., Bouska, Jennifer, Shoemaker, Alexander, Oleksijew, Anatol, Jarvis, Ken, Park, Chang, Jong, Ron De, Oltersdorf, Tilman, Li, Qun, Rosenberg, Saul H., Giranda, Vincent L.

“…We discovered a series of potent and selective oxindole–pyridine-based protein kinase B/Akt inhibitors with an IC50 of 0.17nM for the most potent compound…”
Get full text

Synthesis and structure–activity relationship of 3,4′-bispyridinylethylenes: Discovery of a potent 3-isoquinolinylpyridine inhibitor of protein kinase B (PKB/Akt) for the treatment of cancer by Li, Qun, Woods, Keith W., Thomas, Sheela, Zhu, Gui-Dong, Packard, Garrick, Fisher, John, Li, Tongmei, Gong, Jianchun, Dinges, Jurgen, Song, Xiaohong, Abrams, Jason, Luo, Yan, Johnson, Eric F., Shi, Yan, Liu, Xuesong, Klinghofer, Vered, Des Jong, Ron, Oltersdorf, Tilman, Stoll, Vincent S., Jakob, Clarissa G., Rosenberg, Saul H., Giranda, Vincent L.

“…Structure-based design and synthesis of the 3,4′-bispyridinylethylene series led to the discovery of 3-isoquinolinylpyridine 13a as a potent PKB/Akt inhibitor…”
Get full text

A facile and general synthesis of 2,4-Di- and 2,4,7-trisubstituted thieno[2,3-c]pyridines by Zhu, Gui-Dong, Gunawardana, Indrani W., Boyd, Steven A., Melcher, Laura M.

“…Treatment of 3,5‐dibromo‐ or 3,5‐dichloro‐pyridine‐4‐carboxaldehyde 2 with one equivalent of methyl thioglycolate, followed by exposure to base, provided…”
Get full text

Poly (ADP-ribose) polymerase activity regulates apoptosis in HeLa cells after alkylating DNA damage by Liu, Xuesong, Luo, Xu, Yan Shi, Yan, Zhu, Gui-dong, Penning, Thomas, Giranda, Vincent L, Luo, Yan

“…Majority of chemotherapeutic agents inhibit tumor growth by inducing apoptosis or necrosis. The DNA alkylating agent, N-methyl-N'-nitro-N-nitrosoguanidine…”
Get full text

Optimization of Phenyl-Substituted Benzimidazole Carboxamide Poly(ADP-Ribose) Polymerase Inhibitors: Identification of ( S )-2-(2-Fluoro-4-(pyrrolidin-2-yl)phenyl)-1 H -benzimidazole-4-carboxamide (A-966492), a Highly Potent and Efficacious Inhibitor by Penning, Thomas D., Zhu, Gui-Dong, Gong, Jianchun, Thomas, Sheela, Gandhi, Viraj B., Liu, Xuesong, Shi, Yan, Klinghofer, Vered, Johnson, Eric F., Park, Chang H., Fry, Elizabeth H., Donawho, Cherrie K., Frost, David J., Buchanan, Fritz G., Bukofzer, Gail T., Rodriguez, Luis E., Bontcheva-Diaz, Velitchka, Bouska, Jennifer J., Osterling, Donald J., Olson, Amanda M., Marsh, Kennan C., Luo, Yan, Giranda, Vincent L.

Get full text

Biological Activity of CD‐Ring Modified 1α,25‐Dihydroxyvitamin D Analogues: C‐Ring and Five‐Membered D‐Ring Analogues by Verstuyf, Annemieke, Verlinden, Lieve, Van Etten, Evelyne, Shi, Ling, Wu, Yusheng, D'Halleweyn, Chris, Van Haver, Dirk, Zhu, Gui‐Dong, Chen, Yong‐Jun, Zhou, Xiaoming, Haussler, Mark R., De Clercq, Pierre, Vandewalle, Maurits, Van Baelen, Hugo, Mathieu, Chantal, Bouillon, Roger

“…Nonsteroidal analogues of 1α,25(OH)2D3, lacking either the full five‐membered D ring (C‐ring analogues) or the full six‐membered C ring (D‐ring analogues) are…”
Get full text

Balancing Properties with Carboxylates: A Lead Optimization Campaign for Selective and Orally Active CDK9 Inhibitors by Tong, Yunsong, Florjancic, Alan S, Clark, Rick F, Lai, Chunqiu, Mastracchio, Anthony, Zhu, Gui-dong, Smith, Morey L, Kovar, Peter J, Shaw, Bailin, Albert, Daniel H, Qiu, Wei, Longenecker, Kenton L, Liu, Xiaoqin, Olson, Amanda M, Osterling, Donald J, Tahir, Stephen K, Phillips, Darren C, Leverson, Joel D, Souers, Andrew J, Penning, Thomas D

“…Cyclin-dependent kinase 9 (CDK9) is a serine/threonine kinase involved in the regulation of transcription elongation. An inhibition of CDK9 downregulates a…”
Get full text

Discovery and SAR of 2-(1-propylpiperidin-4-yl)-1H-benzimidazole-4-carboxamide: A potent inhibitor of poly(ADP-ribose) polymerase (PARP) for the treatment of cancer by Penning, Thomas D, Zhu, Gui-Dong, Gandhi, Viraj B, Gong, Jianchun, Thomas, Sheela, Lubisch, Wilfried, Grandel, Roland, Wernet, Wolfgang, Park, Chang H, Fry, Elizabeth H, Liu, Xuesong, Shi, Yan, Klinghofer, Vered, Johnson, Eric F, Donawho, Cherrie K, Frost, David J, Bontcheva-Diaz, Velitchka, Bouska, Jennifer J, Olson, Amanda M, Marsh, Kennan C, Luo, Yan, Rosenberg, Saul H, Giranda, Vincent L

“…We have developed a series of cyclic amine-containing benzimidazole carboxamide poly(ADP-ribose)polymerase (PARP) inhibitors, with good PARP-1 enzyme potency,…”
Get full text

Synthesis of Vitamin D (Calciferol) by Zhu, Gui-Dong, Okamura, William H

“…The known chemical strategies leading to the synthesis of the steroid hormone 1,25-D3 are provided, and information that can be applied to the synthesis of the…”
Get full text

Discovery and SAR of substituted 3-oxoisoindoline-4-carboxamides as potent inhibitors of poly(ADP-ribose) polymerase (PARP) for the treatment of cancer by Gandhi, Viraj B., Luo, Yan, Liu, Xuesong, Shi, Yan, Klinghofer, Vered, Johnson, Eric F., Park, Chang, Giranda, Vincent L., Penning, Thomas D., Zhu, Gui-Dong

“…We have discovered a series of compounds with a 3-oxoisoindoline-4-carboxamide core structure as potent PARP inhibitors. The highlight of the core is a…”
Get full text

Design and synthesis of pyridine–pyrazolopyridine-based inhibitors of protein kinase B/Akt by Zhu, Gui-Dong, Gong, Jianchun, Gandhi, Viraj B., Woods, Keith, Luo, Yan, Liu, Xuesong, Guan, Ran, Klinghofer, Vered, Johnson, Eric F., Stoll, Vincent S., Mamo, Mulugeta, Li, Qun, Rosenberg, Saul H., Giranda, Vincent L.

“…We have designed and synthesized a series of potent pyridine–pyrazolopyridine-based inhibitors of protein kinase B/Akt. The best compound in this series showed…”
Get full text

Synthesis and SAR of indazole-pyridine based protein kinase B/Akt inhibitors by Woods, Keith W., Fischer, John P., Claiborne, Akiyo, Li, Tongmei, Thomas, Sheela A., Zhu, Gui-Dong, Diebold, Robert B., Liu, Xuesong, Shi, Yan, Klinghofer, Vered, Han, Edward K., Guan, Ran, Magnone, Shayna R., Johnson, Eric F., Bouska, Jennifer J., Olson, Amanda M., Jong, Ron de, Oltersdorf, Tilman, Luo, Yan, Rosenberg, Saul H., Giranda, Vincent L., Li, Qun

“…SAR studies leading from the isoquinoline analogue to the discovery of the indazole moiety are described. A series of heteroaryl-pyridine containing inhibitors…”
Get full text

Synthesis and SAR of novel, potent and orally bioavailable benzimidazole inhibitors of poly(ADP-ribose) polymerase (PARP) with a quaternary methylene-amino substituent by Zhu, Gui-Dong, Gandhi, Viraj B., Gong, Jianchun, Thomas, Sheela, Luo, Yan, Liu, Xuesong, Shi, Yan, Klinghofer, Vered, Johnson, Eric F., Frost, David, Donawho, Cherrie, Jarvis, Ken, Bouska, Jennifer, Marsh, Kennan C., Rosenberg, Saul H., Giranda, Vincent L., Penning, Thomas D.

“…We discovered a novel series of potent and orally bioavailable PARP inhibitors containing a quaternary methylene-amino substituent at the C-2 position of the…”
Get full text