Joshua A Kaplan

发表

Cells resistant to HTI-286 do not overexpress P-glycoprotein but have reduced drug accumulation and a point mutation in alpha-tubulin.

T. Fojo, F. Loganzo, M. Poruchynsky, 2004, Molecular cancer therapeutics.

Ex Vivo Profiling of PD-1 Blockade Using Organotypic Tumor Spheroids.

Zhi Wei, Hongye Liu, Wei Huang, 2018, Cancer discovery.

Morpholine derivatives greatly enhance the selectivity of mammalian target of rapamycin (mTOR) inhibitors.

N. Brooijmans, L. Toral-Barza, K. Curran, 2009, Journal of medicinal chemistry.

2,4,6-Triaminopyrimidine as a Novel Hinge Binder in a Series of PI3Kδ Selective Inhibitors.

J. Chandrasekhar, J. R. Somoza, M. Mcgrath, 2016, Journal of medicinal chemistry.

ATP-competitive inhibitors of the mammalian target of rapamycin: design and synthesis of highly potent and selective pyrazolopyrimidines.

R. Abraham, N. Brooijmans, J. Gibbons, 2009, Journal of medicinal chemistry.

Discovery of 3,6-dihydro-2H-pyran as a morpholine replacement in 6-aryl-1H-pyrazolo[3,4-d]pyrimidines and 2-arylthieno[3,2-d]pyrimidines: ATP-competitive inhibitors of the mammalian target of rapamycin (mTOR).

N. Brooijmans, L. Toral-Barza, A. Zask, 2010, Bioorganic & medicinal chemistry letters.

Discovery of 2-ureidophenyltriazines bearing bridged morpholines as potent and selective ATP-competitive mTOR inhibitors.

L. Toral-Barza, J. Lucas, K. Curran, 2010, Bioorganic & medicinal chemistry letters.

2-Arylureidophenyl-4-(3-oxa-8-azabicyclo[3.2.1]octan-8-yl)triazines as highly potent and selective ATP competitive mTOR inhibitors: optimization of human microsomal stability.

K. Curran, A. Zask, Joshua A Kaplan, 2010, Bioorganic & medicinal chemistry letters.

Pyrazolopyrimidines as highly potent and selective, ATP-competitive inhibitors of the mammalian target of rapamycin (mTOR): optimization of the 1-substituent.

L. Toral-Barza, J. Lucas, K. Curran, 2010, Bioorganic & medicinal chemistry letters.

Synthesis and structure-activity relationships of ring-opened 17-hydroxywortmannins: potent phosphoinositide 3-kinase inhibitors with improved properties and anticancer efficacy.

L. Toral-Barza, J. Lucas, M. Young, 2008, Journal of medicinal chemistry.

Discovery of 4-morpholino-6-aryl-1H-pyrazolo[3,4-d]pyrimidines as highly potent and selective ATP-competitive inhibitors of the mammalian target of rapamycin (mTOR): optimization of the 6-aryl substituent.

N. Brooijmans, L. Toral-Barza, J. Lucas, 2009, Journal of medicinal chemistry.

Synthesis and SAR of diazepine and thiazepine TACE and MMP inhibitors.

J. Skotnicki, J. Levin, Xuemei Du, 2005, Bioorganic & medicinal chemistry letters.

Discovery of 4-(benzylaminomethylene)isoquinoline-1,3-(2H,4H)-diones and 4-[(pyridylmethyl)aminomethylene]isoquinoline-1,3-(2H,4H)-diones as potent and selective inhibitors of the cyclin-dependent kinase 4.

S. Rabindran, T. Mansour, H. Tsou, 2009, Journal of medicinal chemistry.

D-piece modifications of the hemiasterlin analog HTI-286 produce potent tubulin inhibitors.

F. Loganzo, G. Krishnamurthy, L. Greenberger, 2004, Bioorganic & medicinal chemistry letters.

Discovery of a Phosphoinositide 3-Kinase (PI3K) β/δ Inhibitor for the Treatment of Phosphatase and Tensin Homolog (PTEN) Deficient Tumors: Building PI3Kβ Potency in a PI3Kδ-Selective Template by Targeting Nonconserved Asp856.

J. Chandrasekhar, M. Mcgrath, G. Phillips, 2017, Journal of medicinal chemistry.

Synthesis and biological activity of analogues of the antimicrotubule agent N, β, β-trimethyl-L-phenylalanyl-N1-[(1S, 2E)-3-carboxy-1-isopropylbut-2-enyl]-N1, 3 -dimethyl-L-valinamide (HTI-286)

R. Williamson, F. Loganzo, C. Discafani, 2004 .

Beyond rapalog therapy: preclinical pharmacology and antitumor activity of WYE-125132, an ATP-competitive and specific inhibitor of mTORC1 and mTORC2.

R. Abraham, J. Gibbons, L. Toral-Barza, 2010, Cancer research.

Incorporation of water-solubilizing groups in pyrazolopyrimidine mTOR inhibitors: discovery of highly potent and selective analogs with improved human microsomal stability.

L. Toral-Barza, J. Lucas, K. Curran, 2009, Bioorganic & medicinal chemistry letters.

Hybrids of the hemiasterlin analogue taltobulin and the dolastatins are potent antimicrotubule agents.

F. Loganzo, A. Zask, S. Musto, 2005, Journal of the American Chemical Society.

Probing the interaction of HTI-286 with tubulin using a stilbene analogue.

G. Krishnamurthy, A. Aulabaugh, A. Zask, 2004, Journal of the American Chemical Society.

Two Photoaffinity Analogues of the Tripeptide, Hemiasterlin, Exclusively Label α-Tubulin

F. Loganzo, G. Krishnamurthy, A. Zask, 2005 .

Discovery of potent and selective inhibitors of the mammalian target of rapamycin (mTOR) kinase.

Joshua Kaplan, Irwin Hollander, Natasja Brooijmans, 2009, Journal of medicinal chemistry.

Synthesis and biological activity of analogues of the antimicrotubule agent N,beta,beta-trimethyl-L-phenylalanyl-N(1)-[(1S,2E)-3-carboxy-1-isopropylbut-2-enyl]- N(1),3-dimethyl-L-valinamide (HTI-286).

R. Williamson, F. Loganzo, C. Discafani, 2004, Journal of medicinal chemistry.