| Year |
Citation |
Score |
| 2020 |
Ellestad G, Zask A, Berova N. The enduring legacy of Koji Nakanishi's research on bioorganic chemistry and natural products. Part 1: Isolation, structure determination and mode of action. Chirality. PMID 32157754 DOI: 10.1002/Chir.23214 |
0.302 |
|
| 2019 |
Bos PH, Lowry ER, Costa J, Thams S, Garcia-Diaz A, Zask A, Wichterle H, Stockwell BR. Development of MAP4 Kinase Inhibitors as Motor Neuron-Protecting Agents. Cell Chemical Biology. PMID 31676236 DOI: 10.1016/J.Chembiol.2019.10.005 |
0.332 |
|
| 2019 |
Dieck C, Reglero-Gomez C, Zask A, Stockwell B, Ferrando A. Abstract C005: NT5C2 small molecule inhibitor for the reversal of 6-MP resistance in acute lymphoblastic leukemia Molecular Cancer Therapeutics. 18. DOI: 10.1158/1535-7163.Targ-19-C005 |
0.305 |
|
| 2017 |
Zask A, Ellestad G. Biomimetic syntheses of racemic natural products. Chirality. PMID 29139568 DOI: 10.1002/Chir.22786 |
0.323 |
|
| 2016 |
Qian J, Chen Y, Meng T, Ma L, Meng L, Wang X, Yu T, Zask A, Shen J, Yu K. Molecular regulation of apoptotic machinery and lipid metabolism by mTORC1/mTORC2 dual inhibitors in preclinical models of HER2+/PIK3CAmut breast cancer. Oncotarget. PMID 27563814 DOI: 10.18632/Oncotarget.11490 |
0.321 |
|
| 2015 |
Zask A, Ellestad GA. Recent Advances in Stereoselective Drug Targeting. Chirality. PMID 26096879 DOI: 10.1002/Chir.22470 |
0.316 |
|
| 2013 |
Joshi D, Field J, Murphy J, Abdelrahim M, Schönherr H, Sparrow JR, Ellestad G, Nakanishi K, Zask A. Synthesis of antioxidants for prevention of age-related macular degeneration. Journal of Natural Products. 76: 450-4. PMID 23346866 DOI: 10.1021/Np300769C |
0.443 |
|
| 2011 |
Zask A, Verheijen JC, Richard DJ. Recent advances in the discovery of small-molecule ATP competitive mTOR inhibitors: a patent review. Expert Opinion On Therapeutic Patents. 21: 1109-27. PMID 21591993 DOI: 10.1517/13543776.2011.584871 |
0.357 |
|
| 2010 |
Zask A, Verheijen JC, Richard DJ, Kaplan J, Curran K, Toral-Barza L, Lucas J, Hollander I, Yu K. Discovery of 2-ureidophenyltriazines bearing bridged morpholines as potent and selective ATP-competitive mTOR inhibitors. Bioorganic & Medicinal Chemistry Letters. 20: 2644-7. PMID 20227881 DOI: 10.1016/J.Bmcl.2010.02.045 |
0.389 |
|
| 2010 |
Richard DJ, Verheijen JC, Yu K, Zask A. Triazines incorporating (R)-3-methylmorpholine are potent inhibitors of the mammalian target of rapamycin (mTOR) with selectivity over PI3Kalpha. Bioorganic & Medicinal Chemistry Letters. 20: 2654-7. PMID 20223664 DOI: 10.1016/J.Bmcl.2010.02.029 |
0.375 |
|
| 2010 |
Verheijen JC, Richard DJ, Curran K, Kaplan J, Yu K, Zask A. 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. Bioorganic & Medicinal Chemistry Letters. 20: 2648-53. PMID 20223663 DOI: 10.1016/J.Bmcl.2010.02.031 |
0.351 |
|
| 2010 |
Curran KJ, Verheijen JC, Kaplan J, Richard DJ, Toral-Barza L, Hollander I, Lucas J, Ayral-Kaloustian S, Yu K, Zask A. Pyrazolopyrimidines as highly potent and selective, ATP-competitive inhibitors of the mammalian target of rapamycin (mTOR): optimization of the 1-substituent. Bioorganic & Medicinal Chemistry Letters. 20: 1440-4. PMID 20089401 DOI: 10.1016/J.Bmcl.2009.12.086 |
0.403 |
|
| 2010 |
Yu K, Shi C, Toral-Barza L, Lucas J, Shor B, Kim JE, Zhang WG, Mahoney R, Gaydos C, Tardio L, Kim SK, Conant R, Curran K, Kaplan J, Verheijen J, ... ... Zask A, et al. Beyond rapalog therapy: preclinical pharmacology and antitumor activity of WYE-125132, an ATP-competitive and specific inhibitor of mTORC1 and mTORC2. Cancer Research. 70: 621-31. PMID 20068177 DOI: 10.1158/0008-5472.Can-09-2340 |
0.372 |
|
| 2010 |
Kaplan J, Verheijen JC, Brooijmans N, Toral-Barza L, Hollander I, Yu K, Zask A. 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). Bioorganic & Medicinal Chemistry Letters. 20: 640-3. PMID 19963384 DOI: 10.1016/J.Bmcl.2009.11.050 |
0.359 |
|
| 2010 |
Ayral-Kaloustian S, Gu J, Lucas J, Cinque M, Gaydos C, Zask A, Chaudhary I, Wang J, Di L, Young M, Ruppen M, Mansour TS, Gibbons JJ, Yu K. 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. Journal of Medicinal Chemistry. 53: 452-9. PMID 19928864 DOI: 10.1021/Jm901427G |
0.341 |
|
| 2010 |
Verheijen JC, Yu K, Toral-Barza L, Hollander I, Zask A. Discovery of 2-arylthieno[3,2-d]pyrimidines containing 8-oxa-3-azabi-cyclo[3.2.1]octane in the 4-position as potent inhibitors of mTOR with selectivity over PI3K. Bioorganic & Medicinal Chemistry Letters. 20: 375-9. PMID 19897362 DOI: 10.1016/J.Bmcl.2009.10.075 |
0.379 |
|
| 2009 |
Zask A, Kaplan J, Verheijen JC, Richard DJ, Curran K, Brooijmans N, Bennett EM, Toral-Barza L, Hollander I, Ayral-Kaloustian S, Yu K. Morpholine derivatives greatly enhance the selectivity of mammalian target of rapamycin (mTOR) inhibitors. Journal of Medicinal Chemistry. 52: 7942-5. PMID 19916508 DOI: 10.1021/Jm901415X |
0.375 |
|
| 2009 |
Richard DJ, Verheijen JC, Curran K, Kaplan J, Toral-Barza L, Hollander I, Lucas J, Yu K, Zask A. Incorporation of water-solubilizing groups in pyrazolopyrimidine mTOR inhibitors: discovery of highly potent and selective analogs with improved human microsomal stability. Bioorganic & Medicinal Chemistry Letters. 19: 6830-5. PMID 19896845 DOI: 10.1016/J.Bmcl.2009.10.096 |
0.371 |
|
| 2009 |
Verheijen JC, Richard DJ, Curran K, Kaplan J, Lefever M, Nowak P, Malwitz DJ, Brooijmans N, Toral-Barza L, Zhang WG, Lucas J, Hollander I, Ayral-Kaloustian S, Mansour TS, Yu K, ... Zask A, et al. 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. Journal of Medicinal Chemistry. 52: 8010-24. PMID 19894727 DOI: 10.1021/Jm9013828 |
0.405 |
|
| 2009 |
Nowak P, Cole DC, Brooijmans N, Bursavich MG, Curran KJ, Ellingboe JW, Gibbons JJ, Hollander I, Hu Y, Kaplan J, Malwitz DJ, Toral-Barza L, Verheijen JC, Zask A, Zhang WG, et al. Discovery of potent and selective inhibitors of the mammalian target of rapamycin (mTOR) kinase. Journal of Medicinal Chemistry. 52: 7081-9. PMID 19848404 DOI: 10.1021/Jm9012642 |
0.387 |
|
| 2009 |
Zask A, Verheijen JC, Curran K, Kaplan J, Richard DJ, Nowak P, Malwitz DJ, Brooijmans N, Bard J, Svenson K, Lucas J, Toral-Barza L, Zhang WG, Hollander I, Gibbons JJ, et al. ATP-competitive inhibitors of the mammalian target of rapamycin: design and synthesis of highly potent and selective pyrazolopyrimidines. Journal of Medicinal Chemistry. 52: 5013-6. PMID 19645448 DOI: 10.1021/Jm900851F |
0.399 |
|
| 2009 |
Yu K, Toral-Barza L, Shi C, Zhang WG, Lucas J, Shor B, Kim J, Verheijen J, Curran K, Malwitz DJ, Cole DC, Ellingboe J, Ayral-Kaloustian S, Mansour TS, Gibbons JJ, ... ... Zask A, et al. Biochemical, cellular, and in vivo activity of novel ATP-competitive and selective inhibitors of the mammalian target of rapamycin. Cancer Research. 69: 6232-40. PMID 19584280 DOI: 10.1158/0008-5472.Can-09-0299 |
0.384 |
|
| 2009 |
Zhang C, Lovering F, Behnke M, Zask A, Sandanayaka V, Sun L, Zhu Y, Xu W, Zhang Y, Levin JI. Synthesis and activity of quinolinylmethyl P1' alpha-sulfone piperidine hydroxamate inhibitors of TACE. Bioorganic & Medicinal Chemistry Letters. 19: 3445-8. PMID 19464885 DOI: 10.1016/J.Bmcl.2009.05.020 |
0.312 |
|
| 2009 |
Tsou HR, Liu X, Birnberg G, Kaplan J, Otteng M, Tran T, Kutterer K, Tang Z, Suayan R, Zask A, Ravi M, Bretz A, Grillo M, McGinnis JP, Rabindran SK, et al. 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. Journal of Medicinal Chemistry. 52: 2289-310. PMID 19317452 DOI: 10.1021/Jm801026E |
0.35 |
|
| 2009 |
Zask A, Kaplan J, Curran K, Verheijen JC, Richard DJ, Brooijmans N, Bennett E, Lucas J, Toral‐Barza L, Hollander I, Gibbons JJ, Abraham RT, Ayral‐Kaloustian S, Mansour TS, Yu K. Abstract B145: Highly selective pyrazolopyrimidine mTOR inhibitors with profound in vivo antitumor activity Molecular Cancer Therapeutics. 8. DOI: 10.1158/1535-7163.Targ-09-B145 |
0.401 |
|
| 2008 |
Zask A, Kaplan J, Toral-Barza L, Hollander I, Young M, Tischler M, Gaydos C, Cinque M, Lucas J, Yu K. Synthesis and structure-activity relationships of ring-opened 17-hydroxywortmannins: potent phosphoinositide 3-kinase inhibitors with improved properties and anticancer efficacy. Journal of Medicinal Chemistry. 51: 1319-23. PMID 18269228 DOI: 10.1021/Jm7012858 |
0.398 |
|
| 2008 |
Yu K, Toral-Barza L, Shi C, Zhang WG, Zask A. Response and determinants of cancer cell susceptibility to PI3K inhibitors: combined targeting of PI3K and Mek1 as an effective anticancer strategy. Cancer Biology & Therapy. 7: 307-15. PMID 18059185 DOI: 10.4161/Cbt.7.2.5334 |
0.338 |
|
| 2008 |
Verheijen J, Yu K, Zask A. Chapter 12 mTOR Inhibitors in Oncology Annual Reports in Medicinal Chemistry. 43: 189-202. DOI: 10.1016/S0065-7743(08)00012-2 |
0.343 |
|
| 2006 |
Zhu T, Gu J, Yu K, Lucas J, Cai P, Tsao R, Gong Y, Li F, Chaudhary I, Desai P, Ruppen M, Fawzi M, Gibbons J, Ayral-Kaloustian S, Skotnicki J, ... ... Zask A, et al. Pegylated wortmannin and 17-hydroxywortmannin conjugates as phosphoinositide 3-kinase inhibitors active in human tumor xenograft models. Journal of Medicinal Chemistry. 49: 1373-8. PMID 16480272 DOI: 10.1021/Jm050901O |
0.345 |
|
| 2005 |
Zask A, Kaplan J, Musto S, Loganzo F. Hybrids of the hemiasterlin analogue taltobulin and the dolastatins are potent antimicrotubule agents. Journal of the American Chemical Society. 127: 17667-71. PMID 16351096 DOI: 10.1021/Ja053663V |
0.33 |
|
| 2005 |
Yu K, Lucas J, Zhu T, Zask A, Gaydos C, Toral-Barza L, Gu J, Li F, Chaudhary I, Cai P, Lotvin J, Petersen R, Ruppen M, Fawzi M, Ayral-Kaloustian S, et al. PWT-458, a novel pegylated-17-hydroxywortmannin, inhibits phosphatidylinositol 3-kinase signaling and suppresses growth of solid tumors. Cancer Biology & Therapy. 4: 538-45. PMID 15846106 DOI: 10.4161/Cbt.4.5.1660 |
0.345 |
|
| 2005 |
Zask A, Kaplan J, Du X, MacEwan G, Sandanayaka V, Eudy N, Levin J, Jin G, Xu J, Cummons T, Barone D, Ayral-Kaloustian S, Skotnicki J. Synthesis and SAR of diazepine and thiazepine TACE and MMP inhibitors. Bioorganic & Medicinal Chemistry Letters. 15: 1641-5. PMID 15745814 DOI: 10.1016/J.Bmcl.2005.01.053 |
0.306 |
|
| 2004 |
Venkatesan AM, Davis JM, Grosu GT, Baker J, Zask A, Levin JI, Ellingboe J, Skotnicki JS, Dijoseph JF, Sung A, Jin G, Xu W, McCarthy DJ, Barone D. Synthesis and structure-activity relationships of 4-alkynyloxy phenyl sulfanyl, sulfinyl, and sulfonyl alkyl hydroxamates as tumor necrosis factor-alpha converting enzyme and matrix metalloproteinase inhibitors. Journal of Medicinal Chemistry. 47: 6255-69. PMID 15566296 DOI: 10.1021/Jm040086X |
0.358 |
|
| 2004 |
Yamashita A, Norton EB, Kaplan JA, Niu C, Loganzo F, Hernandez R, Beyer CF, Annable T, Musto S, Discafani C, Zask A, Ayral-Kaloustian S. Synthesis and activity of novel analogs of hemiasterlin as inhibitors of tubulin polymerization: modification of the A segment. Bioorganic & Medicinal Chemistry Letters. 14: 5317-22. PMID 15454219 DOI: 10.1016/J.Bmcl.2004.08.024 |
0.355 |
|
| 2004 |
Zask A, Birnberg G, Cheung K, Kaplan J, Niu C, Norton E, Suayan R, Yamashita A, Cole D, Tang Z, Krishnamurthy G, Williamson R, Khafizova G, Musto S, Hernandez R, et al. 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). Journal of Medicinal Chemistry. 47: 4774-86. PMID 15341492 DOI: 10.1021/Jm040056U |
0.333 |
|
| 2004 |
Lo MC, Aulabaugh A, Krishnamurthy G, Kaplan J, Zask A, Smith RP, Ellestad G. Probing the interaction of HTI-286 with tubulin using a stilbene analogue. Journal of the American Chemical Society. 126: 9898-9. PMID 15303845 DOI: 10.1021/Ja048619E |
0.336 |
|
| 2004 |
Zask A, Birnberg G, Cheung K, Kaplan J, Niu C, Norton E, Yamashita A, Beyer C, Krishnamurthy G, Greenberger LM, Loganzo F, Ayral-Kaloustian S. D-piece modifications of the hemiasterlin analog HTI-286 produce potent tubulin inhibitors. Bioorganic & Medicinal Chemistry Letters. 14: 4353-8. PMID 15261301 DOI: 10.1016/J.Bmcl.2004.05.005 |
0.347 |
|
| 2004 |
Niu C, Smith D, Zask A, Loganzo F, Discafani C, Beyer C, Greenberger L, Ayral-Kaloustian S. Tubulin inhibitors. Synthesis and biological activity of HTI-286 analogs with B-segment heterosubstituents. Bioorganic & Medicinal Chemistry Letters. 14: 4329-32. PMID 15261296 DOI: 10.1016/J.Bmcl.2004.05.077 |
0.335 |
|
| 2003 |
Aranapakam V, Davis JM, Grosu GT, Baker J, Ellingboe J, Zask A, Levin JI, Sandanayaka VP, Du M, Skotnicki JS, DiJoseph JF, Sung A, Sharr MA, Killar LM, Walter T, et al. Synthesis and structure-activity relationship of N-substituted 4-arylsulfonylpiperidine-4-hydroxamic acids as novel, orally active matrix metalloproteinase inhibitors for the treatment of osteoarthritis. Journal of Medicinal Chemistry. 46: 2376-96. PMID 12773042 DOI: 10.1021/Jm0205550 |
0.37 |
|
| 2003 |
Aranapakam V, Grosu GT, Davis JM, Hu B, Ellingboe J, Baker JL, Skotnicki JS, Zask A, DiJoseph JF, Sung A, Sharr MA, Killar LM, Walter T, Jin G, Cowling R. Synthesis and structure-activity relationship of alpha-sulfonylhydroxamic acids as novel, orally active matrix metalloproteinase inhibitors for the treatment of osteoarthritis. Journal of Medicinal Chemistry. 46: 2361-75. PMID 12773041 DOI: 10.1021/Jm0205548 |
0.314 |
|
| 1999 |
Skotnicki JS, Zask A, Nelson FC, Albright JD, Levin JI. Design and synthetic considerations of matrix metalloproteinase inhibitors. Annals of the New York Academy of Sciences. 878: 61-72. PMID 10415720 DOI: 10.1111/J.1749-6632.1999.Tb07674.X |
0.312 |
|
| 1987 |
Takeda R, Zask A, Nakanishi K, Park MH. Additivity in split Cotton effect amplitudes of p-phenylbenzyl ethers and p-phenylbenzoates Journal of the American Chemical Society. 109: 914-915. DOI: 10.1021/Ja00237A055 |
0.371 |
|
| 1986 |
Zask A, Gonnella N, Nakanishi K, Turner CJ, Imajo S, Nozoe T. Syntheses and spectral properties of tropocoronands, a new class of versatile metal-complexing macrocycles derived from aminotropone imines Inorganic Chemistry. 25: 3400-3407. DOI: 10.1021/Ic00239A017 |
0.422 |
|
| 1985 |
Semmelhack MF, Bozell JJ, Keller L, Sato T, Spiess EJ, Wulff W, Zask A. Synthesis of naphthoquinone antibiotics by intramolecular alkyne cycloaddition to carbene-chromium complexes Tetrahedron. 41: 5803-5812. DOI: 10.1016/S0040-4020(01)91420-6 |
0.61 |
|
| 1985 |
Davis WM, Zask A, Nakanishi K, Lippard SJ. Copper(II) tropocoronands: synthesis, structure, and properties of mononuclear complexes Inorganic Chemistry. 24: 3737-3743. DOI: 10.1002/Chin.198608270 |
0.427 |
|
| 1985 |
Davis WM, Roberts MM, Zask A, Nakanishi K, Nozoe T, Lippard SJ. Stereochemical and electronic spin state tuning of the metal center in the nickel(II) tropocoronands Journal of the American Chemical Society. 107: 3864-3870. DOI: 10.1002/Chin.198542060 |
0.356 |
|
| 1984 |
Nakanishi K, Kuroyanagi M, Nambu H, Oltz EM, Takeda R, Verdine GL, Zask A. Recent applications of circular dichroism to structural problems, especially oligosaccharide structures Pure and Applied Chemistry. 56: 1031-1048. DOI: 10.1351/Pac198456081031 |
0.65 |
|
| 1983 |
Semmelhack MF, Zask A. Synthesis of racemic frenolicin via organochromium and organopalladium intermediates Journal of the American Chemical Society. 105: 2034-2043. DOI: 10.1002/Chin.198328371 |
0.503 |
|
| 1982 |
Semmelhack MF, Bozell JJ, Sato T, Wulff W, Spiess E, Zask A. Synthesis of nanaomycin A and deoxyfrenolicin by alkyne cycloaddition to chromium-carbene complexes Journal of the American Chemical Society. 104: 5850-5852. |
0.497 |
|
| 1978 |
Zask A, Helquist P. Palladium hydrides in organic synthesis. Reduction of aryl halides by sodium methoxide catalyzed by tetrakis(triphenylphosphine)palladium The Journal of Organic Chemistry. 43: 1619-1620. DOI: 10.1021/Jo00402A042 |
0.485 |
|
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