TECHNICAL PROGRAM - American Chemical Society Publications
TECHNICAL PROGRAM - American Chemical Society Publications
TECHNICAL PROGRAM - American Chemical Society Publications
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MEDI <strong>TECHNICAL</strong> <strong>PROGRAM</strong><br />
54. Novel tumor-targeting anticancer drug<br />
conjugate bearing a taxoid and a topotecan.<br />
E. S. Zuniga,I.Ojima<br />
55. Synthesis and biological evaluation of<br />
novel carbocycle-containing combretastatin<br />
A-4 analogs. R. Fürst,<br />
C. Nowikow, A. Berenyi, G. F. Ecker,<br />
W. Schmid, I. Zupko, U. Rinner<br />
56. Design of potent guanase inhibitors<br />
based on azepinomycin skeleton.<br />
S. Chakraborty, R. Hosmane<br />
57. Blocking the nuclear translocation of signal<br />
transducer and activator of transcription<br />
3 (STAT3) protein via membrane anchorage.<br />
M. Avadisian, S. Fletcher,<br />
B. Liu, W. Xu, P. Yue, A. D. Schimmer,<br />
J. Turkson, C. Gradinaru, P. T. Gunning*<br />
58. Development of PET and SPECT radiotracers<br />
for the imaging of cancers overexpressing<br />
the ErbB family of growth factor<br />
receptors. E. B. Corcoran, H. T. Pham,<br />
R. N. Hanson<br />
59. Development of a second-generation antiandrogen<br />
for treatment of castration-resistant<br />
prostate cancer (CRPC). D. Yoo,<br />
S. Ouk, C. Chen, C. Tran, J. Wongvipat,<br />
C. L. Sawyers, M. E. Jung<br />
60. Targeting the interaction of mixed lineage<br />
leukemia 1 (MLL1) and wd repeat<br />
domain 5 (WDR5) for new anticancer drug<br />
design. H. Karatas, E. Townsend,<br />
D. Bernard, Y. Dou, S. Wang<br />
61. Rational design and evaluation of small<br />
molecule DNA ligase inhibitors as potential<br />
cancer chemotherapeutics.<br />
G. E. Greco,X.Chen,L.A.Tobin,<br />
R. A. Lapidus, M. Sadowska, A. J. Yang,<br />
N. N. Nemieboka, A. D. MacKerell,<br />
S. Zhong, F. V. Rassool, A. E. Tomkinson<br />
62. Design, synthesis and evaluation of<br />
dibenzo[c,h][1,6]naphthyridines as Top1<br />
inhibitors and potential anticancer<br />
agents. E. Kiselev, T. Dexhemier,<br />
Y. Pommier, M. Cushman<br />
63. Design and synthesis of ezrin inhibitors<br />
for metastatic osteosarcoma.<br />
G. W. Kosturko, G. Bulut, V. Rodriguez,<br />
E. Glasgow, S. Hong, C. Khanna,<br />
M. Brown, M. Paige, A. Üren<br />
64. Small molecule prostate specific membrane<br />
antigen inhibitors with Re/Tc for<br />
the diagnosis and staging of prostate<br />
cancer. G. Lu, K. P. Maresca,<br />
S. M. Hillier, J. C. Marquis,<br />
C. N. Zimmerman, W. C. Eckelman,<br />
J. L. Joyal, J. W. Babich<br />
65. Structure-based design, synthesis, and<br />
evaluation of a new class of potent Bcl-2/<br />
Bcl-X L inhibitors. H. Zhou, J. Chen,<br />
A. Aguilar, X. Cong, L. Liu, L. Bai,<br />
D. McEachern, C. Yang, H. Yi,<br />
J. Meagher, J. A. Stuckey, X. Li, D. Sun,<br />
S. Wang<br />
66. Novel VEGFR2 inhibitors: Pyridylmethylthio<br />
derivatives with intramolecular nonbonded<br />
S-O interaction. H. Tajima,<br />
T. Honda, K. Kawashima, Y. Sasabuchi,<br />
M. Yamamoto, M. Ban, K. Okamoto,<br />
K. Inoue, T. Inaba, Y. Takeno, H. Aono,<br />
T. Tsuboi, A. Tonouchi<br />
67. Design, synthesis and evaluation of<br />
Smac mimetics as selective cIAP-1 and<br />
cIAP-2 inhibitors. H. Sun, J. Lu, L. Liu,<br />
C. Yang, H. Yi, S. Wang<br />
68. DNA methyltransferase inhibitors: Molecular<br />
modeling and virtual screening.<br />
J. L. Medina-Franco, N. Singh,<br />
F. Lopez-Vallejo, D. Kuck, F. Lyko,<br />
A. Dueñas-Gonzalez, G. Sbardella<br />
69. Apoptosis triggers targeting selectively<br />
resistant tumours. E. Genoux,<br />
D. Lorendeau, H. Cortay, A. Di Pietro,<br />
A. Boumendjel<br />
70. 2-Aryl-benzimidazole-4-carboxamides<br />
as novel SIRT1 activators. J. S. Disch,<br />
C. B. Vu, L. McPherson, P. Ng,<br />
J. E. Bemis, D. P. Carney, A. V. Lynch,<br />
C. Loh, S. Ribich, P. Romero, J. J. Smith,<br />
J. Song, D. J. Gagne, A. Cote, M. Davis,<br />
E. Lainez, R. B. Perni<br />
74–TECH<br />
‡ Cooperative Cosponsorship<br />
71. Synthesis and SAR of tricyclic isoquinoline<br />
derivatives as HCV NS3 protease inhibitors.<br />
J. Chen, L. Sun, F. Yu, G. Zhai,<br />
D. Hernandez, A. K. Sheaffer, J. Friborg,<br />
D. Barry, H. Mulherin, M. S. Lee,<br />
F. McPhee, J. O. Knipe, K. Mosure,<br />
N. A. Meanwell, P. M. Scola<br />
72. In vitro and in vivo biological annotation<br />
of a novel B-RAF inhibitor amenable for<br />
clinical evaluation against B-RAF(V600E)harboring<br />
human tumors. J. Lapierre,<br />
C. Chen, Y. Liu, J. Szwaya, E. Chiesa,<br />
C. Bull, E. Chang, C. Waghorne, J. Mao,<br />
D. Lowe, K. Nguyen, E. Volckova,<br />
Y. Wang, T. Hall, R. Savage, D. France,<br />
M. A. Ashwell<br />
73. Design and synthesis of simplified paclitaxel<br />
analogs based on the T-taxol bioactive<br />
conformation. J. Zhao,S.Bane,<br />
K. Mukherjee, J. P. Snyder, H. Hu,<br />
D. G. Kingston<br />
74. Discovery of novel 2,4,6-trisubstituted<br />
pyrimidine and pyridine based SIRT1 activators.<br />
K. J. Koppetsch, C. J. Oalmann,<br />
B. Szczepankiewicz, C. B. Vu,<br />
G. Gualtieri, R. L. Casaubon, J. S. Disch,<br />
A. V. Lynch, J. Song, D. J. Gagne,<br />
A. Cote, M. Davis, E. Lainez, R. B. Perni<br />
75. Discovery of a new class of selective<br />
Chk1 “diazacarbazoles”. J. Drobnick,<br />
B. Appleton, L. Axford, M. Beresini,<br />
B. Burton, H. Chen, D. Clark, K. Clark,<br />
P. Crackett, C. Ellwood, E. Gancia,<br />
A. Ganguli, M. Gill, J. Goldstein,<br />
S. Goodacre, J. Hewitt, D. Hurst, S. Kintz,<br />
P. Lockey, J. Lyssikatos, S. Major,<br />
C. McLeod, D. McNair, G. Medard,<br />
R. Narukulla, R. Newman, S. Sideris,<br />
C. Weismann, H. Hunt, K. Williams,<br />
S. Malek, L. Gazzard<br />
76. Phthalazinone pyrazoles as potent, selective<br />
and orally bio-available inhibitors<br />
of Aurora-A kinase. M. Prime,<br />
F. Brookfield, S. Courtney, G. Georges,<br />
B. Goller, A. Limberg, R. Marston,<br />
P. Rueger, M. Rueth, W. von der Saal<br />
77. Synthesis of novel osteogenic oxysterol<br />
activators of the Hedgehog signaling<br />
pathway. M. Epperson,W.Xiao,<br />
F. Stappenbeck, F. Farouz<br />
78. Putative exosite targeting for optimization<br />
of 4EGI-1, a PPI inhibitor and a potent<br />
anti-cancer agent. K. Takrouri,<br />
Y. Wang, L. Chen, N. Zhang, B. H. Aktas,<br />
G. Wagner, J. A. Halperin, M. Chorev<br />
79. Structure-based computational design of<br />
selective, small molecule PRMT5 inhibitors<br />
for experimental therapeutics of cancer:<br />
Protein modeling, virtual screening<br />
and lead validation. K. V. Mahasenan,<br />
F. Yan, R. Baiocchi, C. Li<br />
80. In vitro and in vivo studies on the effectiveness<br />
of free drug and nanoparticle encapsulated<br />
silver carbene complexes on<br />
H460 lung cancer. M. C. Deblock,<br />
N. Robishaw, A. Knapp, M. J. Panzner,<br />
A. Gupta, W. J. Youngs<br />
81. Design, synthesis, and pharmacological<br />
evaluation of multireceptor modulating<br />
agents as potential atypical antipsychotics.<br />
K. Peprah, S. V. Eyunni,<br />
J. R. Etukala, V. Setola, B. L. Roth,<br />
S. Y. Abblodeppey<br />
82. Selective small molecules targeting<br />
G-protein interactions to combat cancer<br />
metastasis. M. J. Koyack,<br />
R. V. Rajnarayanan<br />
83. Synthetic strategies for developing multivalent<br />
nitric oxide donors.<br />
R. S. Nandurdikar,S.Y.Hong,<br />
O. A. Oladeinde, A. E. Maciag,<br />
J. E. Saavedra, L. K. Keefer<br />
84. Synthesis of carbon-11-labeled casimiroin<br />
analogs as new potential PET agents<br />
for imaging of quinone reductase 2 and<br />
aromatase expression in cancer.<br />
M. Wang, M. Gao, G. D. Hutchins,<br />
Q. Zheng<br />
85. Property based optimization of lactam<br />
based histone deacetylase (HDAC) inhibitors.<br />
M. Cho, D. Song<br />
86. Discovery of potent imidazo[1,2-a]pyrazine<br />
Aurora kinase inhibitors.<br />
D. B. Belanger, P. J. Curran, A. Hruza,<br />
J. Voigt, Z. Meng, A. K. Mandal,<br />
M. A. Siddiqui, A. D. Basso, K. Gray<br />
87. Design, synthesis and biological evaluation<br />
of pemetrexed(PMX) homologs for<br />
folate receptor targeting multiple enzyme<br />
antifolates. A. Gangjee, Y. Wang,<br />
S. K. Desmoulin, C. Cherian,<br />
L. H. Matherly, R. L. Kisliuk<br />
88. Design, synthesis, and testing of orthoamido<br />
diphenylamines as inhibitors of<br />
MEK5. P. T. Flaherty, I. Chopra,<br />
A. Diwan, D. A. Monlish, J. E. Cavanaugh<br />
89. 2-Desamino and 2-methyl-6-substituted<br />
pyrrolo[2,3-d]pyrimidine classical antifolates<br />
as selective folate receptor substrates,<br />
glycinamide ribonucleotide<br />
formyltransferase inhibitors and antitumor<br />
agents. A. Gangjee, S. Zhao, C. Cherian,<br />
S. K. Desmoulin, L. H. Matherly,<br />
R. L. Kisliuk<br />
90. Synthesis and SAR of diaminopyrimidines<br />
as c-Met inhibitors.<br />
L. R. Weinberg, M. S. Albom,<br />
T. S. Angeles, J. L. Diebold, J. Husten,<br />
J. G. Lisko, K. L. Milkiewicz, S. Murthy,<br />
G. R. Ott, B. A. Ruggeri, J. P. Theroff,<br />
T. L. Underiner, B. D. Dorsey<br />
91. Identification of potential proteins targets<br />
of quercetin inhibition of HSP-70 induction<br />
with a biotin-quercetin photoaffinity<br />
agent. R. E. Wang, C. R. Hunt, J. Taylor<br />
92. Development of polyamides as gene inhibitors<br />
of heat shock protein 70 expression.<br />
R. E. Wang, R. Pandita, C. R. Hunt,<br />
J. Taylor<br />
93. Rational design of disubstituted triazole<br />
conjugated acridines with high selectivity<br />
for the human parallel telomeric quadruplex.<br />
S. Sparapani,S.M.Haider,<br />
F. Doria, M. Gunaratnam, S. Neidle<br />
94. Synthesis and characterization of rigidified<br />
4EGI-1 mimetics that block proteinprotein<br />
interaction, inhibit translation initiation,<br />
and have anticancer activity.<br />
R. Yefidoff-Freedman,Y.Wang,<br />
L. Chen, N. Zhang, B. H. Aktas,<br />
G. Wagner, J. A. Halperin, M. Chorev<br />
95. Novel fluorescently labeled omega-3<br />
fatty acid-taxiod conjugates.<br />
W. T. Berger, E. Zuniga, J. D. Seitz,<br />
L. V. Kuznetsova, I. Ojima<br />
96. Discovery of TAK-700, a naphthylmethylimidazole<br />
derivative, as a highly selective,<br />
orally active 17, 20 lyase inhibitor for<br />
prostate cancer. T. Kaku, T. Hitaka,<br />
A. Ojida, N. Matsunaga, N. Terauchi,<br />
F. Itoh, T. Tanaka, T. Hara, M. Yamaoka,<br />
M. Kusaka, T. Okuda, S. Asahi, S. Furuya,<br />
A. Tasaka<br />
97. Structural requirements of histone<br />
deacetylase (HDAC) inhibitors: Suberoyl<br />
anilide hydroxamic acid (SAHA) analogs<br />
modified at the C3 position. S. Choi,<br />
S. V. Weerasinghe, M. H. Pflum<br />
98. Antagonism of the Bak–Bcl-xL complex<br />
by �-helix mimetics of varying curvatures.<br />
S. Fletcher<br />
99. Anticancer properties of gold(I)-N-heterocyclic<br />
carbene complexes and their<br />
silver(I) precursors. T. J. Siciliano,<br />
M. C. Deblock, K. M. Hindi, S. Durmus,<br />
M. J. Panzner, C. A. Tessier,<br />
W. J. Youngs<br />
100. Development of small molecule protein<br />
lysine methyltransferase G9a inhibitors.<br />
J. M. Yost, F. Liu, X. Chen,<br />
A. Allali-Hassani, A. M. Quinn, T. J. Wigle,<br />
D. Barsyte, G. A. Wasney, A. Dong,<br />
I. Kozieradzki, G. Senisterra, I. Chau,<br />
A. Siarheyeva, A. Van Deusen,<br />
D. B. Kireev, A. Jadhav, J. M. Herold,<br />
S. V. Frye, C. H. Arrowsmith,<br />
W. P. Janzen, P. J. Brown, A. Simeonov,<br />
M. Vedadi, J. Jin<br />
101. From isothiazole to thiophene and thiazole:<br />
A bioisosteric approach to the discovery<br />
of potent imidazo[1,2-a]pyrazines<br />
as Aurora kinase inhibitors. Z. Meng,<br />
B. A. Kulkarni, A. D. Kerekes, J. Voigt,<br />
A. K. Mandal, S. J. Esposite,<br />
D. B. Belanger, P. P. Reddy, A. D. Basso,<br />
K. Gray, S. Tevar, J. Jones, E. Smith,<br />
M. A. Siddiqui, R. Doll<br />
102. SAR of various Aurora selective chemotypes.<br />
Z. Ji, Y. Dai, D. H. Albert,<br />
J. J. Bouska, K. B. Glaser,<br />
T. J. Magoc, k. D. Stewart, P. Tapang,<br />
R. Wei, M. Michaelides<br />
103. Development of oxazolidinone and oxazolobenzimidazole<br />
positive allosteric<br />
modulators for the treatment of Schizophrenia.<br />
E. J. Brnardic, R. M. Garbaccio,<br />
M. E. Fraley, M. E. Layton, G. D. Hartman,<br />
M. A. Jacobson, B. C. Magliaro,<br />
S. L. Huszar, P. H. Hutson, J. A. O’Brien,<br />
J. M. Uslaner, K. L. Fillgrove, C. Tang,<br />
Y. Kuo, S. M. Sur<br />
104. 2-Substituted benzimidazoles as<br />
metabotropic glutamate receptor-2 positive<br />
allosteric modulators: A hit to lead<br />
evaluation. C. Chen, U. Topiwala,<br />
H. Jimenez, H. Chen, M. Uberti, K. Jones,<br />
S. Topiol, M. Marzabadi, D. Doller<br />
105. Structure activity relationship studies of<br />
4-((((3S,6S)-6-benzhydryltetrahydro-2Hpyran-3-yl)amino)methyl)phenol<br />
and its<br />
analogs: Development of novel triple uptake<br />
inhibitors as new generation antidepressants.<br />
B. Gopishetty, S. Santra,<br />
S. Ali, M. Reith, a. dutta<br />
106. Probing S1� site of caspase-3: A new<br />
hope for mechanism based treatment of<br />
neurological disorders. A. K. Sharma<br />
107. SAR evaluation of fused heterocyclic<br />
quinolone carboxylic acid M1 positive allosteric<br />
modulators. C. N. Di Marco,<br />
V. Cofre, W. J. Ray, L. Ma, M. Wittmann,<br />
M. A. Seager, K. A. Koeplinger,<br />
C. D. Thompson, G. D. Hartman,<br />
M. T. Bilodeau, S. D. Kuduk<br />
108. New aryl sulfonamides compounds as<br />
potent and selective 5-ht 6 receptor ligands.<br />
A. Shinde, V. Reballi,<br />
V. Tiriveedhi, P. Gudla, L. Kota,<br />
A. Chindhe, N. Rambabu,<br />
R. Kambhampati, R. Nirogi<br />
109. Structure-activity relationships of 2,4diphenyl-1H-imidazole<br />
analogs as CB2<br />
receptor agonists for the treatment of<br />
chronic pain. S. Yang, J. Smotryski,<br />
J. Matasi, G. Ho, D. Tulshian,<br />
W. J. Greenlee, R. Brusa, M. Beltramo,<br />
K. Cox<br />
110. High affinity ligands for opioid receptors<br />
in the picomolar K i range: N-(2-[1,1�-biphenyl]-4-ylethyl)<br />
analogs of 8-CAC.<br />
J. M. Bidlack, D. J. Cohen,<br />
J. M. Gargano, X. Jia, S. Jo,<br />
M. A. VanAlstine, M. P. Wentland<br />
111. Novel series of CB2 selective antagonists<br />
for the treatment of autoimmune<br />
disorders: Synthesis, functional evaluation<br />
and ligand-steered modeling.<br />
S. S. Phatak, R. R. Petrov,<br />
F. Astruc-Diaz, C. N. Cavasotto,P.Diaz<br />
112. 7-Hydroxy-benzopyran-4-one derivatives:<br />
Discovery and structure-activity relationships<br />
of PPAR � and -� (PPAR� and<br />
�) dual agonists. N. Gavande, A. Matin,<br />
M. S. Kim, N. K. Salam, J. R. Hanrahan,<br />
R. H. Roubin, D. E. Hibbs<br />
113. Synthesis and structure-activity relationships<br />
of 3-aminopyridazine derivatives<br />
of �-aminobutyric acid acting as<br />
GABA C (�) antagonists. N. Gavande,<br />
G. A. Johnston, J. R. Hanrahan,<br />
M. Chebib<br />
114. Design, synthesis and pharmacological<br />
evaluation of fluorescent GABA C probes<br />
for receptor visualization and localization<br />
studies. N. Gavande, G. A. Johnston,<br />
J. R. Hanrahan, M. Chebib<br />
115. Design, synthesis, and pharmacological<br />
evaluation of novel, selective �-aminobutyric<br />
acid � (GABA C) receptor antagonists.<br />
N. Gavande, K. Mewett,<br />
G. A. Johnston, J. R. Hanrahan,<br />
M. Chebib<br />
116. Hepatitis C protease inhibitors based<br />
on 2(1H)-pyrazinones. J. Gising,<br />
A. Belfrage,P.Örtqvist, M. Larhed,<br />
U. Danielson, A. Sandström<br />
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