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Items: 11

1.

Discovery of MK-8318, a Potent and Selective CRTh2 Receptor Antagonist for the Treatment of Asthma.

Huang X, Brubaker J, Zhou W, Biju PJ, Xiao L, Shao N, Huang Y, Dong L, Liu Z, Bitar R, Buevich A, Jung J, Peterson SL, Butcher JW, Close J, Martinez M, MacCoss RN, Zhang H, Crawford S, McCormick KD, Aslanian R, Nargund R, Correll C, Gervais F, Qiu H, Yang X, Garlisi C, Rindgen D, Maloney KM, Siliphaivanh P, Palani A.

ACS Med Chem Lett. 2018 Jun 23;9(7):679-684. doi: 10.1021/acsmedchemlett.8b00145. eCollection 2018 Jul 12.

PMID:
30034600
2.

Label-Free, LC-MS-Based Assays to Quantitate Small-Molecule Antagonist Binding to the Mammalian BLT1 Receptor.

Chen X, Stout S, Mueller U, Boykow G, Visconti R, Siliphaivanh P, Spencer K, Presland J, Kavana M, Basso AD, McLaren DG, Myers RW.

SLAS Discov. 2017 Aug 1:2472555217719748. doi: 10.1177/2472555217719748. [Epub ahead of print]

PMID:
28763622
3.

Discovery of 1-(1H-Pyrazolo[4,3-c]pyridin-6-yl)urea Inhibitors of Extracellular Signal-Regulated Kinase (ERK) for the Treatment of Cancers.

Lim J, Kelley EH, Methot JL, Zhou H, Petrocchi A, Chen H, Hill SE, Hinton MC, Hruza A, Jung JO, Maclean JK, Mansueto M, Naumov GN, Philippar U, Raut S, Spacciapoli P, Sun D, Siliphaivanh P.

J Med Chem. 2016 Jul 14;59(13):6501-11. doi: 10.1021/acs.jmedchem.6b00708. Epub 2016 Jul 1.

PMID:
27329786
4.

Anti-inflammatory actions of Chemoattractant Receptor-homologous molecule expressed on Th2 by the antagonist MK-7246 in a novel rat model of Alternaria alternata elicited pulmonary inflammation.

Gil MA, Caniga M, Woodhouse JD, Eckman J, Lee HH, Salmon M, Naber J, Hamilton VT, Sevilla RS, Bettano K, Klappenbach J, Moy L, Correll CC, Gervais FG, Siliphaivanh P, Zhang W, Zhang-Hoover J, McLeod RL, Cicmil M.

Eur J Pharmacol. 2014 Nov 15;743:106-16. doi: 10.1016/j.ejphar.2014.09.021. Epub 2014 Sep 23.

5.

Delayed and Prolonged Histone Hyperacetylation with a Selective HDAC1/HDAC2 Inhibitor.

Methot JL, Hoffman DM, Witter DJ, Stanton MG, Harrington P, Hamblett C, Siliphaivanh P, Wilson K, Hubbs J, Heidebrecht R, Kral AM, Ozerova N, Fleming JC, Wang H, Szewczak AA, Middleton RE, Hughes B, Cruz JC, Haines BB, Chenard M, Kenific CM, Harsch A, Secrist JP, Miller TA.

ACS Med Chem Lett. 2014 Jan 2;5(4):340-5. doi: 10.1021/ml4004233. eCollection 2014 Apr 10.

6.

Quality by design (QbD) of amide isosteres: 5,5-Disubstituted isoxazolines as potent CRTh2 antagonists with favorable pharmacokinetic and drug-like properties.

Xiao D, Zhu X, Yu Y, Shao N, Wu J, McCormick KD, Dhondi P, Qin J, Mazzola R, Tang H, Rao A, Siliphaivanh P, Qiu H, Yang X, Rivelli M, Garlisi CG, Eckel S, Mukhopadhyay G, Correll C, Rindgen D, Aslanian R, Palani A.

Bioorg Med Chem Lett. 2014 Mar 15;24(6):1615-20. doi: 10.1016/j.bmcl.2014.01.043. Epub 2014 Feb 2.

PMID:
24556380
7.

Discovery of a novel ERK inhibitor with activity in models of acquired resistance to BRAF and MEK inhibitors.

Morris EJ, Jha S, Restaino CR, Dayananth P, Zhu H, Cooper A, Carr D, Deng Y, Jin W, Black S, Long B, Liu J, Dinunzio E, Windsor W, Zhang R, Zhao S, Angagaw MH, Pinheiro EM, Desai J, Xiao L, Shipps G, Hruza A, Wang J, Kelly J, Paliwal S, Gao X, Babu BS, Zhu L, Daublain P, Zhang L, Lutterbach BA, Pelletier MR, Philippar U, Siliphaivanh P, Witter D, Kirschmeier P, Bishop WR, Hicklin D, Gilliland DG, Jayaraman L, Zawel L, Fawell S, Samatar AA.

Cancer Discov. 2013 Jul;3(7):742-50. doi: 10.1158/2159-8290.CD-13-0070. Epub 2013 Apr 24.

8.

Purine derivatives as potent gamma-secretase modulators.

Rivkin A, Ahearn SP, Chichetti SM, Hamblett CL, Garcia Y, Martinez M, Hubbs JL, Reutershan MH, Daniels MH, Siliphaivanh P, Otte KM, Li C, Rosenau A, Surdi LM, Jung J, Hughes BL, Crispino JL, Nikov GN, Middleton RE, Moxham CM, Szewczak AA, Shah S, Moy LY, Kenific CM, Tanga F, Cruz JC, Andrade P, Angagaw MH, Shomer NH, Miller T, Munoz B, Shearman MS.

Bioorg Med Chem Lett. 2010 Apr 1;20(7):2279-82. doi: 10.1016/j.bmcl.2010.02.008. Epub 2010 Feb 6.

PMID:
20207146
9.

Phenylglycine and phenylalanine derivatives as potent and selective HDAC1 inhibitors (SHI-1).

Wilson KJ, Witter DJ, Grimm JB, Siliphaivanh P, Otte KM, Kral AM, Fleming JC, Harsch A, Hamill JE, Cruz JC, Chenard M, Szewczak AA, Middleton RE, Hughes BL, Dahlberg WK, Secrist JP, Miller TA.

Bioorg Med Chem Lett. 2008 Mar 15;18(6):1859-63. doi: 10.1016/j.bmcl.2008.02.012. Epub 2008 Feb 10.

PMID:
18304810
10.

Design of novel histone deacetylase inhibitors.

Siliphaivanh P, Harrington P, Witter DJ, Otte K, Tempest P, Kattar S, Kral AM, Fleming JC, Deshmukh SV, Harsch A, Secrist PJ, Miller TA.

Bioorg Med Chem Lett. 2007 Aug 15;17(16):4619-24. Epub 2007 May 27.

PMID:
17555962
11.

Enantioselective total synthesis of (+)-leucascandrolide A macrolactone.

Crimmins MT, Siliphaivanh P.

Org Lett. 2003 Nov 27;5(24):4641-4.

PMID:
14627404

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