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Items: 31

1.

Design, Synthesis, and SAR of C-3 Benzoic Acid, C-17 Triterpenoid Derivatives. Identification of the HIV-1 Maturation Inhibitor 4-((1 R,3a S,5a R,5b R,7a R,11a S,11b R,13a R,13b R)-3a-((2-(1,1-Dioxidothiomorpholino)ethyl)amino)-5a,5b,8,8,11a-pentamethyl-1-(prop-1-en-2-yl)-2,3,3a,4,5,5a,5b,6,7,7a,8,11,11a,11b,12,13,13a,13b-octadecahydro-1 H-cyclopenta[ a]chrysen-9-yl)benzoic Acid (GSK3532795, BMS-955176).

Regueiro-Ren A, Swidorski JJ, Liu Z, Chen Y, Sin N, Sit SY, Chen J, Venables BL, Zhu J, Nowicka-Sans B, Protack T, Lin Z, Terry B, Samanta H, Zhang S, Li Z, Easter J, Beno BR, Arora V, Huang XS, Rahematpura S, Parker DD, Haskell R, Santone KS, Cockett MI, Krystal M, Meanwell NA, Jenkins S, Hanumegowda U, Dicker IB.

J Med Chem. 2018 Aug 23;61(16):7289-7313. doi: 10.1021/acs.jmedchem.8b00854. Epub 2018 Aug 1.

PMID:
30067361
2.

Development of 1H-Pyrazolo[3,4-b]pyridines as Metabotropic Glutamate Receptor 5 Positive Allosteric Modulators.

Hill MD, Fang H, Brown JM, Molski T, Easton A, Han X, Miller R, Hill-Drzewi M, Gallagher L, Matchett M, Gulianello M, Balakrishnan A, Bertekap RL, Santone KS, Whiterock VJ, Zhuo X, Bronson JJ, Macor JE, Degnan AP.

ACS Med Chem Lett. 2016 Oct 3;7(12):1082-1086. eCollection 2016 Dec 8.

3.

Difluorocyclobutylacetylenes as positive allosteric modulators of mGluR5 with reduced bioactivation potential.

Degnan AP, Maxwell D, Balakrishnan A, Brown JM, Easton A, Gulianello M, Hanumegowda U, Hill-Drzewi M, Miller R, Santone KS, Senapati A, Shields EE, Sivarao DV, Westphal R, Whiterock VJ, Zhuo X, Bronson JJ, Macor JE.

Bioorg Med Chem Lett. 2016 Dec 15;26(24):5871-5876. doi: 10.1016/j.bmcl.2016.11.014. Epub 2016 Nov 9.

PMID:
27856084
4.

Oxazolidinone-based allosteric modulators of mGluR5: Defining molecular switches to create a pharmacological tool box.

Huang H, Degnan AP, Balakrishnan A, Easton A, Gulianello M, Huang Y, Matchett M, Mattson G, Miller R, Santone KS, Senapati A, Shields EE, Sivarao DV, Snyder LB, Westphal R, Whiterock VJ, Yang F, Bronson JJ, Macor JE.

Bioorg Med Chem Lett. 2016 Sep 1;26(17):4165-9. doi: 10.1016/j.bmcl.2016.07.065. Epub 2016 Jul 28.

PMID:
27496211
5.

Inhibition of AAK1 Kinase as a Novel Therapeutic Approach to Treat Neuropathic Pain.

Kostich W, Hamman BD, Li YW, Naidu S, Dandapani K, Feng J, Easton A, Bourin C, Baker K, Allen J, Savelieva K, Louis JV, Dokania M, Elavazhagan S, Vattikundala P, Sharma V, Das ML, Shankar G, Kumar A, Holenarsipur VK, Gulianello M, Molski T, Brown JM, Lewis M, Huang Y, Lu Y, Pieschl R, O'Malley K, Lippy J, Nouraldeen A, Lanthorn TH, Ye G, Wilson A, Balakrishnan A, Denton R, Grace JE, Lentz KA, Santone KS, Bi Y, Main A, Swaffield J, Carson K, Mandlekar S, Vikramadithyan RK, Nara SJ, Dzierba C, Bronson J, Macor JE, Zaczek R, Westphal R, Kiss L, Bristow L, Conway CM, Zambrowicz B, Albright CF.

J Pharmacol Exp Ther. 2016 Sep;358(3):371-86. doi: 10.1124/jpet.116.235333. Epub 2016 Jul 13.

6.

Discovery of BMS-955176, a Second Generation HIV-1 Maturation Inhibitor with Broad Spectrum Antiviral Activity.

Regueiro-Ren A, Liu Z, Chen Y, Sin N, Sit SY, Swidorski JJ, Chen J, Venables BL, Zhu J, Nowicka-Sans B, Protack T, Lin Z, Terry B, Samanta H, Zhang S, Li Z, Beno BR, Huang XS, Rahematpura S, Parker DD, Haskell R, Jenkins S, Santone KS, Cockett MI, Krystal M, Meanwell NA, Hanumegowda U, Dicker IB.

ACS Med Chem Lett. 2016 Apr 22;7(6):568-72. doi: 10.1021/acsmedchemlett.6b00010. eCollection 2016 Jun 9.

7.

Discovery and Preclinical Evaluation of BMS-955829, a Potent Positive Allosteric Modulator of mGluR5.

Yang F, Snyder LB, Balakrishnan A, Brown JM, Sivarao DV, Easton A, Fernandes A, Gulianello M, Hanumegowda UM, Huang H, Huang Y, Jones KM, Li YW, Matchett M, Mattson G, Miller R, Santone KS, Senapati A, Shields EE, Simutis FJ, Westphal R, Whiterock VJ, Bronson JJ, Macor JE, Degnan AP.

ACS Med Chem Lett. 2016 Jan 4;7(3):289-93. doi: 10.1021/acsmedchemlett.5b00450. eCollection 2016 Mar 10.

8.

Preclinical characterization of BMS-791325, an allosteric inhibitor of hepatitis C Virus NS5B polymerase.

Lemm JA, Liu M, Gentles RG, Ding M, Voss S, Pelosi LA, Wang YK, Rigat KL, Mosure KW, Bender JA, Knipe JO, Colonno R, Meanwell NA, Kadow JF, Santone KS, Roberts SB, Gao M.

Antimicrob Agents Chemother. 2014 Jun;58(6):3485-95. doi: 10.1128/AAC.02495-13. Epub 2014 Apr 14.

9.

Discovery and early clinical evaluation of BMS-605339, a potent and orally efficacious tripeptidic acylsulfonamide NS3 protease inhibitor for the treatment of hepatitis C virus infection.

Scola PM, Wang AX, Good AC, Sun LQ, Combrink KD, Campbell JA, Chen J, Tu Y, Sin N, Venables BL, Sit SY, Chen Y, Cocuzza A, Bilder DM, D'Andrea S, Zheng B, Hewawasam P, Ding M, Thuring J, Li J, Hernandez D, Yu F, Falk P, Zhai G, Sheaffer AK, Chen C, Lee MS, Barry D, Knipe JO, Li W, Han YH, Jenkins S, Gesenberg C, Gao Q, Sinz MW, Santone KS, Zvyaga T, Rajamani R, Klei HE, Colonno RJ, Grasela DM, Hughes E, Chien C, Adams S, Levesque PC, Li D, Zhu J, Meanwell NA, McPhee F.

J Med Chem. 2014 Mar 13;57(5):1708-29. doi: 10.1021/jm401840s. Epub 2014 Feb 20.

PMID:
24555570
10.

Hepatitis C virus NS5A replication complex inhibitors: the discovery of daclatasvir.

Belema M, Nguyen VN, Bachand C, Deon DH, Goodrich JT, James CA, Lavoie R, Lopez OD, Martel A, Romine JL, Ruediger EH, Snyder LB, St Laurent DR, Yang F, Zhu J, Wong HS, Langley DR, Adams SP, Cantor GH, Chimalakonda A, Fura A, Johnson BM, Knipe JO, Parker DD, Santone KS, Fridell RA, Lemm JA, O'Boyle DR 2nd, Colonno RJ, Gao M, Meanwell NA, Hamann LG.

J Med Chem. 2014 Mar 13;57(5):2013-32. doi: 10.1021/jm401836p. Epub 2014 Feb 12.

PMID:
24521299
11.

Discovery and preclinical characterization of the cyclopropylindolobenzazepine BMS-791325, a potent allosteric inhibitor of the hepatitis C virus NS5B polymerase.

Gentles RG, Ding M, Bender JA, Bergstrom CP, Grant-Young K, Hewawasam P, Hudyma T, Martin S, Nickel A, Regueiro-Ren A, Tu Y, Yang Z, Yeung KS, Zheng X, Chao S, Sun JH, Beno BR, Camac DM, Chang CH, Gao M, Morin PE, Sheriff S, Tredup J, Wan J, Witmer MR, Xie D, Hanumegowda U, Knipe J, Mosure K, Santone KS, Parker DD, Zhuo X, Lemm J, Liu M, Pelosi L, Rigat K, Voss S, Wang Y, Wang YK, Colonno RJ, Gao M, Roberts SB, Gao Q, Ng A, Meanwell NA, Kadow JF.

J Med Chem. 2014 Mar 13;57(5):1855-79. doi: 10.1021/jm4016894. Epub 2014 Jan 7.

PMID:
24397558
12.

Design and characterization of a novel fluorinated magnetic resonance imaging agent for functional analysis of bile Acid transporter activity.

Vivian D, Cheng K, Khurana S, Xu S, Whiterock V, Witter D, Lentz KA, Santone KS, Raufman JP, Polli JE.

Pharm Res. 2013 May;30(5):1240-51. doi: 10.1007/s11095-012-0963-6. Epub 2013 Jan 15.

13.

Discovery of (5S,6S,9R)-5-amino-6-(2,3-difluorophenyl)-6,7,8,9-tetrahydro-5H-cyclohepta[b]pyridin-9-yl 4-(2-oxo-2,3-dihydro-1H-imidazo[4,5-b]pyridin-1-yl)piperidine-1-carboxylate (BMS-927711): an oral calcitonin gene-related peptide (CGRP) antagonist in clinical trials for treating migraine.

Luo G, Chen L, Conway CM, Denton R, Keavy D, Signor L, Kostich W, Lentz KA, Santone KS, Schartman R, Browning M, Tong G, Houston JG, Dubowchik GM, Macor JE.

J Med Chem. 2012 Dec 13;55(23):10644-51. doi: 10.1021/jm3013147. Epub 2012 Nov 15.

PMID:
23153230
14.

Studies on the pharmacokinetics and metabolism of a gamma-secretase inhibitor BMS-299897, and exploratory investigation of CYP enzyme induction.

Zheng M, Wang J, Lubinski J, Flint OP, Krishna R, Yao M, Pursley JM, Thakur A, Boulton DW, Santone KS, Barten DM, Anderson JJ, Felsenstein KM, Hansel SB.

Xenobiotica. 2009 Jul;39(7):544-55. doi: 10.1080/00498250902928555.

PMID:
19480557
15.

An automated high throughput liquid chromatography-mass spectrometry process to assess the metabolic stability of drug candidates.

Drexler DM, Belcastro JV, Dickinson KE, Edinger KJ, Hnatyshyn SY, Josephs JL, Langish RA, McNaney CA, Santone KS, Shipkova PA, Tymiak AA, Zvyaga TA, Sanders M.

Assay Drug Dev Technol. 2007 Apr;5(2):247-64.

PMID:
17477833
16.

Analogs of a potent maxi-K potassium channel opener with an improved inhibitory profile toward cytochrome P450 isozymes.

Vrudhula VM, Dasgupta B, Boissard CG, Gribkoff VK, Santone KS, Dalterio RA, Lodge NJ, Starrett JE Jr.

Bioorg Med Chem Lett. 2005 Oct 1;15(19):4286-90.

PMID:
16061379
17.

Biaryl isoxazolinone antibacterial agents.

Quesnelle CA, Gill P, Roy S, Dodier M, Marinier A, Martel A, Snyder LB, D'Andrea SV, Bronson JJ, Frosco M, Beaulieu D, Warr GA, Denbleyker KL, Stickle TM, Yang H, Chaniewski SE, Ferraro CA, Taylor D, Russell JW, Santone KS, Clarke J, Drain RL, Knipe JO, Mosure K, Barrett JF.

Bioorg Med Chem Lett. 2005 Jun 2;15(11):2728-33.

PMID:
15869878
18.

Disposition of radiolabeled ifetroban in rats, dogs, monkeys, and humans.

Dockens RC, Santone KS, Mitroka JG, Morrison RA, Jemal M, Greene DS, Barbhaiya RH.

Drug Metab Dispos. 2000 Aug;28(8):973-80.

PMID:
10901709
19.

Doxorubicin blocks the increase in intracellular Ca++, part of a second messenger system in N1E-115 murine neuroblastoma cells.

Oakes SG, Schlager JJ, Santone KS, Abraham RT, Powis G.

J Pharmacol Exp Ther. 1990 Mar;252(3):979-83.

PMID:
2319480
20.

Studies of chemical toxicity to fresh and cryopreserved rat hepatocytes.

Santone KS, Melder DC, Powis G.

Toxicol Appl Pharmacol. 1989 Feb;97(2):370-6.

PMID:
2922764
22.

Cryopreservation of rat and dog hepatocytes for studies of xenobiotic metabolism and activation.

Powis G, Santone KS, Melder DC, Thomas L, Moore DJ, Wilke TJ.

Drug Metab Dispos. 1987 Nov-Dec;15(6):826-32.

PMID:
2893709
23.

Quinoneimines as substrates for quinone reductase (NAD(P)H: (quinone-acceptor)oxidoreductase) and the effect of dicumarol on their cytotoxicity.

Powis G, See KL, Santone KS, Melder DC, Hodnett EM.

Biochem Pharmacol. 1987 Aug 1;36(15):2473-9.

PMID:
2440444
24.
25.

Role of metabolism and oxidation-reduction cycling in the cytotoxicity of antitumor quinoneimines and quinonediimines.

Powis G, Hodnett EM, Santone KS, See KL, Melder DC.

Cancer Res. 1987 May 1;47(9):2363-70.

26.

Anthracycline-induced inhibition of a calcium action potential in differentiated murine neuroblastoma cells.

Santone KS, Oakes SG, Taylor SR, Powis G.

Cancer Res. 1986 Jun;46(6):2659-64.

27.

Enhanced formation of ethane and n-pentane by rat hepatocytes in the presence of dimethyl sulfoxide.

Santone KS, Kroschel DM, Powis G.

Biochem Pharmacol. 1986 Apr 15;35(8):1287-92.

PMID:
3008757
28.

Effects of advanced leukemia on hepatic drug-metabolizing activity in the mouse.

Powis G, Harris RN, Basseches PJ, Santone KS.

Cancer Chemother Pharmacol. 1986;16(1):43-9.

PMID:
3940219
29.

An in vitro approach to the study of target organ toxicity of drugs and chemicals.

Acosta D, Sorensen EM, Anuforo DC, Mitchell DB, Ramos K, Santone KS, Smith MA.

In Vitro Cell Dev Biol. 1985 Sep;21(9):495-504.

PMID:
4044468
30.

Cadmium toxicity in primary cultures of rat hepatocytes.

Santone KS, Acosta D, Bruckner JV.

J Toxicol Environ Health. 1982 Jul;10(1):169-77.

PMID:
7131585
31.

Lack of cytotoxicity of ticrynafen in primary cultures of rat liver cells.

Acosta D, Mitchell DB, Santone KS, Bock A, Lewis W.

Toxicol Lett. 1982 Mar;10(4):385-8.

PMID:
7089992

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