S. Ayral-Kaloustian

发表

4-(Phenylaminomethylene)isoquinoline-1,3(2H,4H)-diones as potent and selective inhibitors of the cyclin-dependent kinase 4 (CDK4).

R. Nilakantan, M. B. Floyd, S. Rabindran, 2008, Journal of medicinal chemistry.

TTI-237: a novel microtubule-active compound with in vivo antitumor activity.

C. Discafani, J. Gibbons, J. Lucas, 2008, Cancer research.

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.

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.

HTI-286, a synthetic analogue of the tripeptide hemiasterlin, is a potent antimicrotubule agent that circumvents P-glycoprotein-mediated resistance in vitro and in vivo.

T. Fojo, R. Andersen, J. Nieman, 2003, Cancer research.

Acetylenic TACE inhibitors. Part 1. SAR of the acyclic sulfonamide hydroxamates.

R. Black, J. Skotnicki, J. Levin, 2003, Bioorganic & medicinal chemistry letters.

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.

Biochemical, cellular, and in vivo activity of novel ATP-competitive and selective inhibitors of the mammalian target of rapamycin.

Kevin Curran, Judy Lucas, John Ellingboe, 2009, Cancer research.

4-Substituted-7-azaindoles bearing a ureidobenzofuranone moiety as potent and selective, ATP-competitive inhibitors of the mammalian target of rapamycin (mTOR).

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

Discovery and optimization of 2-(4-substituted-pyrrolo[2,3-b]pyridin-3-yl)methylene-4-hydroxybenzofuran-3(2H)-ones as potent and selective ATP-competitive inhibitors of the mammalian target of rapamycin (mTOR).

N. Brooijmans, L. Toral-Barza, J. Bard, 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.

PWT-458, a novel pegylated-17-hydroxywortmannin, inhibits phosphatidylinositol 3-kinase signaling and suppresses growth of solid tumors

P. Frost, J. Skotnicki, P. Cai, 2005, Cancer biology & therapy.

Synthesis and SAR of 6-chloro-4-fluoroalkylamino-2-heteroaryl-5-(substituted)phenylpyrimidines as anti-cancer agents.

N. Zhang, C. Discafani, J. Lucas, 2009, Bioorganic & medicinal chemistry.

Chapter 18. Ras Farnesyltransferase Inhibitors

J. Skotnicki, S. Ayral-Kaloustian, 1996 .

Hybrid inhibitors of phosphatidylinositol 3-kinase (PI3K) and the mammalian target of rapamycin (mTOR): design, synthesis, and superior antitumor activity of novel wortmannin-rapamycin conjugates.

J. Gibbons, J. Lucas, Jianxin Gu, 2010, Journal of medicinal chemistry.

Pegylated wortmannin and 17-hydroxywortmannin conjugates as phosphoinositide 3-kinase inhibitors active in human tumor xenograft models.

J. Skotnicki, P. Cai, J. Gibbons, 2006, Journal of medicinal chemistry.

2-cyanoaminopyrimidines as a class of antitumor agents that promote tubulin polymerization.

N. Zhang, S. Ayral-Kaloustian, C. Beyer, 2007, Bioorganic & medicinal chemistry letters.

Abstract 723: Beyond temsirolimus: Discovery of PKI-587 a highly efficacious dual PI3K/mTOR inhibitor

R. Abraham, N. Brooijmans, L. Feldberg, 2010 .

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.

Synthesis and SAR of novel 4-morpholinopyrrolopyrimidine derivatives as potent phosphatidylinositol 3-kinase inhibitors.

N. Brooijmans, L. Feldberg, R. Mallon, 2010, Journal of medicinal chemistry.

Facile synthesis of 1,1-gem-dialkylperfluoroalkylamines

Nan Zhang, S. Ayral-Kaloustian, 2002 .

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.

Synthesis and SAR of [1,2,4]triazolo[1,5-a]pyrimidines, a class of anticancer agents with a unique mechanism of tubulin inhibition.

Nan Zhang, Judy Lucas, N. Zhang, 2007, Journal of medicinal chemistry.

5-ureidobenzofuranone indoles as potent and efficacious inhibitors of PI3 kinase-alpha and mTOR for the treatment of breast cancer.

N. Brooijmans, N. Zhang, R. Mallon, 2010, Bioorganic & medicinal chemistry letters.

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

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

An asymmetric synthesis of differentially protected meso-2,6-diaminopimelic acid

S. Schow, D. Powell, S. Ayral-Kaloustian, 1994 .

Pyrolysis of the tosylhydrazone sodium salts of two bicyclic lactones

S. Ayral-Kaloustian, W. Agosta, 1982 .

Synthesis of partially-protected d-fructofuranoses and d-fructose-6-phosphates

M. B. Floyd, S. Ayral-Kaloustian, 1991 .

Photochemistry of two .beta.,.beta.'-epoxy ketones, 3-oxatricyclo[3.2.1.02,4]octan-8-one and 3-oxatricyclo[3.3.1.02.4]nonan-9-one. Intramolecular reactions of .alpha.,.beta.-unsaturated aldehydo ketenes

S. Ayral-Kaloustian, William C. Agosta, S. Wolff, 1978 .

Lead optimization of N-3-substituted 7-morpholinotriazolopyrimidines as dual phosphoinositide 3-kinase/mammalian target of rapamycin inhibitors: discovery of PKI-402.

R. Abraham, N. Brooijmans, L. Feldberg, 2010, Journal of medicinal chemistry.

Absolute configurations of tubulin inhibitors taltobulin (HTI-286) and HTI-042 characterized by X-ray diffraction analysis and NMR studies.

R. Williamson, C. Niu, S. Ayral-Kaloustian, 2010, Bioorganic & medicinal chemistry letters.

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 .

Photochemistry of 4-isobutyl-4-methyl- and 4-(2-methoxyethyl)-4-methyl-2-cyclopentenone. Stereochemical effects in intramolecular abstraction of hydrogen by the .beta.-carbon atom of cyclopentenones

S. Ayral-Kaloustian, William C. Agosta, S. Wolff, 1977 .

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.

Anticancer Agents from Unique Natural Products Sources

M. K. Harper, T. Fojo, R. Andersen, 2003 .

Antitumor Efficacy of PKI-587, a Highly Potent Dual PI3K/mTOR Kinase Inhibitor

L. Feldberg, R. Mallon, J. Lucas, 2011, Clinical Cancer Research.

Cancer Therapy : Preclinical Antitumor Efficacy of PKI-587 , a Highly Potent Dual PI 3 K / mTOR Kinase Inhibitor

L. Feldberg, R. Mallon, J. Lucas, 2011 .

PKI-179: an orally efficacious dual phosphatidylinositol-3-kinase (PI3K)/mammalian target of rapamycin (mTOR) inhibitor.

L. Feldberg, R. Mallon, J. Lucas, 2010, Bioorganic & medicinal chemistry letters.

Antitumor Efficacy Profile of PKI-402, a Dual Phosphatidylinositol 3-Kinase/Mammalian Target of Rapamycin Inhibitor

L. Feldberg, R. Mallon, J. Gibbons, 2010, Molecular Cancer Therapeutics.

Identification of 2-oxatriazines as highly potent pan-PI3K/mTOR dual inhibitors.

N. Brooijmans, L. Feldberg, R. Mallon, 2011, Bioorganic & medicinal chemistry letters.

Novel imidazolopyrimidines as dual PI3-Kinase/mTOR inhibitors.

R. Abraham, N. Brooijmans, L. Feldberg, 2010, Bioorganic & medicinal chemistry letters.

Bis(morpholino-1,3,5-triazine) derivatives: potent adenosine 5'-triphosphate competitive phosphatidylinositol-3-kinase/mammalian target of rapamycin inhibitors: discovery of compound 26 (PKI-587), a highly efficacious dual inhibitor.

Judy Lucas, Irwin Hollander, Robert Mallon, 2010, Journal of medicinal chemistry.

Design and synthesis of novel diaminoquinazolines with in vivo efficacy for beta-catenin/T-cell transcriptional factor 4 pathway inhibition.

M. Follettie, N. Brooijmans, J. Lucas, 2010, Journal of medicinal chemistry.

2,4-Diamino-quinazolines as inhibitors of beta-catenin/Tcf-4 pathway: Potential treatment for colorectal cancer.

J. Lucas, T. Mansour, K. Arndt, 2009, Bioorganic & medicinal chemistry letters.

The microtubule-active antitumor compound TTI-237 has both paclitaxel-like and vincristine-like properties

J. Gibbons, S. Ayral-Kaloustian, N. Zhang, 2009, Cancer Chemotherapy and Pharmacology.

Stereoselective synthesis of an active metabolite of the potent PI3 kinase inhibitor PKI-179.

T. Mansour, S. Ayral-Kaloustian, L. McDonald, 2010, The Journal of organic chemistry.

Cevipabulin (TTI-237): preclinical and clinical results for a novel antimicrotubule agent.

S. Ayral-Kaloustian, C. Beyer, N. Zhang, 2009, Methods and findings in experimental and clinical pharmacology.

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

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

Protein farnesyltransferase inhibitors.

S. Ayral-Kaloustian, E. J. Salaski, 2002, Current medicinal chemistry.

Acetylenic TACE inhibitors. Part 1. SAR of the acyclic sulfonamide hydroxamates.

R. Black, J. Skotnicki, J. Levin, 2003, Bioorganic & medicinal chemistry letters.

Benzodiazepine inhibitors of the MMPs and TACE. Part 2.

F. C. Nelson, James M. Chen, J. Levin, 2004, Bioorganic & Medicinal Chemistry Letters.

Biochemical, cellular, and in vivo activity of novel ATP-competitive and selective inhibitors of the mammalian target of rapamycin.

R. Abraham, J. Gibbons, J. Lucas, 2009, Cancer Research.

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.

R. Abraham, N. Brooijmans, R. Mallon, 2010, Journal of medicinal chemistry.

Lead optimization of N-3-substituted 7-morpholinotriazolopyrimidines as dual phosphoinositide 3-kinase/mammalian target of rapamycin inhibitors: discovery of PKI-402.

R. Abraham, N. Brooijmans, R. Mallon, 2010, Journal of medicinal chemistry.

Novel imidazolopyrimidines as dual PI3-Kinase/mTOR inhibitors.

R. Abraham, N. Brooijmans, R. Mallon, 2010, Bioorganic & medicinal chemistry letters.