Search Results - "Gabarda, Ana E"

Complex Target-Oriented Total Synthesis in the Drug Discovery Process:  The Discovery of a Highly Promising Family of Second Generation Epothilones by Rivkin, Alexey, Yoshimura, Fumihiko, Gabarda, Ana E, Chou, Ting-Chao, Dong, Huajin, Tong, William P, Danishefsky, Samuel J

“…The total synthesis of a family of (E)-9,10-dehydro derivatives of epothilone D (i.e., 12,13-desoxyepothilone B) is described. The route is particularly…”
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Discovery of a 5H-Benzo[4,5]cyclohepta[1,2-b]pyridin-5-one (MK-2461) Inhibitor of c-Met Kinase for the Treatment of Cancer by Katz, Jason D, Jewell, James P, Guerin, David J, Lim, Jongwon, Dinsmore, Christopher J, Deshmukh, Sujal V, Pan, Bo-Sheng, Marshall, C. Gary, Lu, Wei, Altman, Michael D, Dahlberg, William K, Davis, Lenora, Falcone, Danielle, Gabarda, Ana E, Hang, Gaozhen, Hatch, Harold, Holmes, Rachael, Kunii, Kaiko, Lumb, Kevin J, Lutterbach, Bart, Mathvink, Robert, Nazef, Naim, Patel, Sangita B, Qu, Xianlu, Reilly, John F, Rickert, Keith W, Rosenstein, Craig, Soisson, Stephen M, Spencer, Kerrie B, Szewczak, Alexander A, Walker, Deborah, Wang, Wenxian, Young, Jonathan, Zeng, Qinwen

“…c-Met is a transmembrane tyrosine kinase that mediates activation of several signaling pathways implicated in aggressive cancer phenotypes. In recent years,…”
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Total Synthesis of Reblastatin by Wrona, Iwona E, Gabarda, Ana E, Evano, Gwilherm, Panek, James S

“…Enantioselective total synthesis of reblastatin is described. The synthesis highlights hydrozirconation, transmetalation, aldehyde addition sequence to install…”
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Discovery of (E)-9,10-Dehydroepothilones through Chemical Synthesis:  On the Emergence of 26-Trifluoro-(E)-9,10-dehydro-12,13-desoxyepothilone B as a Promising Anticancer Drug Candidate by Rivkin, Alexey, Yoshimura, Fumihiko, Gabarda, Ana E, Cho, Young Shin, Chou, Ting-Chao, Dong, Huajin, Danishefsky, Samuel J

“…We provide a full account of the discovery of the (E)-9,10-dehydro derivatives of 12,13-desoxyepothilone B (dEpoB), a new class of antitumor agents with…”
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Design and Total Synthesis of a Superior Family of Epothilone Analogues, which Eliminate Xenograft Tumors to a Nonrelapsable State by Chou, Ting-Chao, Dong, Huajin, Rivkin, Alexey, Yoshimura, Fumihiko, Gabarda, Ana E., Cho, Young Shin, Tong, William P., Danishefsky, Samuel J.

“…Unusually promising profiles of antitumor activity are displayed by 26‐trifluoro‐(E)‐9,10‐dehydro‐dEpoB (1), the design and practical total synthesis of which…”
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Application of Ring-Closing Metathesis Reactions in the Synthesis of Epothilones by Rivkin, Alexey, Cho, Young Shin, Gabarda, Ana E, Yoshimura, Fumihiko, Danishefsky, Samuel J

“…There is wide interest in the epothilones, which like the taxoids initiate cytotoxicity through microtubule stabilization. Briefly described is an application…”
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Synthesis and Conformational Analysis of (E)-9,10-Dehydroepothilone B: A Suggestive Link between the Chemistry and Biology of Epothilones by Yoshimura, Fumihiko, Rivkin, Alexey, Gabarda, Ana E., Chou, Ting-Chao, Dong, Huajin, Sukenick, George, Morel, Florence F., Taylor, Richard E., Danishefsky, Samuel J.

“…The most potent epothilone analogue reported to date was obtained by incorporation of an E double bond at C9C10 in the epothilone B series (see picture)…”
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Asymmetric total synthesis of (20 R)-homocamptothecin, substituted homocamptothecins and homosilatecans by Gabarda, Ana E, Du, Wu, Isarno, Thomas, Tangirala, Raghuram S, Curran, Dennis P

“…An efficient asymmetric synthesis of a key DE lactone pyridone intermediate in the synthesis of homocamptothecin is reported. The synthesis is scalable and…”
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Formation of cyclopropanes by homolytic substitution reactions of 3-iodopropyl radicals: Preparative and rate studies by Curran, Dennis P., Gabarda, Ana E.

“…Reduction of 2-substituted 1,3-diiodopropane derivatives with tin hydride provides substituted cyclopropanes. The reaction occurs through a homolytic…”
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Discovery of a 5 H -Benzo[4,5]cyclohepta[1,2- b ]pyridin-5-one (MK-2461) Inhibitor of c-Met Kinase for the Treatment of Cancer by Katz, Jason D., Jewell, James P., Guerin, David J., Lim, Jongwon, Dinsmore, Christopher J., Deshmukh, Sujal V., Pan, Bo-Sheng, Marshall, C. Gary, Lu, Wei, Altman, Michael D., Dahlberg, William K., Davis, Lenora, Falcone, Danielle, Gabarda, Ana E., Hang, Gaozhen, Hatch, Harold, Holmes, Rachael, Kunii, Kaiko, Lumb, Kevin J., Lutterbach, Bart, Mathvink, Robert, Nazef, Naim, Patel, Sangita B., Qu, Xianlu, Reilly, John F., Rickert, Keith W., Rosenstein, Craig, Soisson, Stephen M., Spencer, Kerrie B., Szewczak, Alexander A., Walker, Deborah, Wang, Wenxian, Young, Jonathan, Zeng, Qinwen

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The Cascade Radical Annulation Approach to New Analogues of Camptothecins: Combinatorial Synthesis of Silatecans and Homosilatecans by CURRAN, DENNIS P., JOSIEN, HUBERT, BOM, DAVID, GABARDA, ANA E., DU, WU

“…: An overview of the cascade radical annulation approach to the camptothecin family of antitumor drugs is presented. This combinatorial synthetic approach…”
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The Combinatorial Synthesis of Racemic Homosilatecan Libraries via a Cascade Radical Annulation by DU, WU, GABARDA, ANA E., BOM, DAVID, CURRAN, DENNIS P.

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Design and Total Synthesis of a Superior Family of Epothilone Analogues, which Eliminate Xenograft Tumors to a Nonrelapsable State by Chou, Ting-Chao, Dong, Huajin, Rivkin, Alexey, Yoshimura, Fumihiko, Gabarda, Ana E., Cho, Young Shin, Tong, William P., Danishefsky, Samuel J.

“…Ungewöhnlich vielversprechende Antitumoraktivität zeigt 26‐Trifluor‐(E)‐9,10‐dehydro‐dEpoB 1, dessen Design und einfache Totalsynthese beschrieben werden…”
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Synthesis and Conformational Analysis of (E)-9,10-Dehydroepothilone B: A Suggestive Link between the Chemistry and Biology of Epothilones by Yoshimura, Fumihiko, Rivkin, Alexey, Gabarda, Ana E., Chou, Ting-Chao, Dong, Huajin, Sukenick, George, Morel, Florence F., Taylor, Richard E., Danishefsky, Samuel J.

“…Der kleine Unterschied: Das wirksamste bisher bekannte Epothilonderivat wurde durch Einführung einer E‐konfigurierten Doppelbindung zwischen C9 und C10 in der…”
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Solution-Phase Parallel Synthesis of 115 Homosilatecan Analogues by Gabarda, Ana E., Curran, Dennis P.

“…The parallel synthesis of 115 homosilatecans on 1−5 mg scale has been accomplished. Key reactions include N-propargylation of a common iodopyridone lactone…”
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