Search Results - "Ernest Hamel"

(−)-Rhazinilam and the diphenylpyridazinone NSC 613241: Two compounds inducing the formation of morphologically similar tubulin spirals but binding apparently to two distinct sites on tubulin by Bai, Ruoli, Hamel, Ernest

“…The most potent microtubule assembly inhibitor of newer diphenylpyridazinone derivatives examined was NSC 613241. Because NSC 613241 and (−)-rhazinilam also…”
Get full text

Insight on [1,3]thiazolo[4,5-e]isoindoles as tubulin polymerization inhibitors by Spanò, Virginia, Barreca, Marilia, Rocca, Roberta, Bortolozzi, Roberta, Bai, Ruoli, Carbone, Anna, Raimondi, Maria Valeria, Piccionello, Antonio Palumbo, Montalbano, Alessandra, Alcaro, Stefano, Hamel, Ernest, Viola, Giampietro, Barraja, Paola

“…A series of [1,3]thiazolo[4,5-e]isoindoles has been synthesized through a versatile and high yielding multistep sequence. Evaluation of the antiproliferative…”
Get full text

12,13-Aziridinyl Epothilones. Stereoselective Synthesis of Trisubstituted Olefinic Bonds from Methyl Ketones and Heteroaromatic Phosphonates and Design, Synthesis, and Biological Evaluation of Potent Antitumor Agents by Nicolaou, K. C, Rhoades, Derek, Wang, Yanping, Bai, Ruoli, Hamel, Ernest, Aujay, Monette, Sandoval, Joseph, Gavrilyuk, Julia

“…The synthesis and biological evaluation of a series of 12,13-aziridinyl epothilone B analogues is described. These compounds were accessed by a practical,…”
Get full text

Effects of substituent pattern on the intracellular target of antiproliferative benzo[b]thiophenyl chromone derivatives by Saito, Yohei, Taniguchi, Yukako, Hirazawa, Sachika, Miura, Yuta, Tsurimoto, Hiroyuki, Nakayoshi, Tomoki, Oda, Akifumi, Hamel, Ernest, Yamashita, Katsumi, Goto, Masuo, Nakagawa-Goto, Kyoko

“…A new biological scaffold was produced by replacing the 6π-electron phenyl ring-B of a natural flavone skeleton with a 10π-electron benzothiophene (BT). Since…”
Get full text

MG-2477, a new tubulin inhibitor, induces autophagy through inhibition of the Akt/mTOR pathway and delayed apoptosis in A549 cells by Viola, Giampietro, Bortolozzi, Roberta, Hamel, Ernest, Moro, Stefano, Brun, Paola, Castagliuolo, Ignazio, Ferlin, Maria Grazia, Basso, Giuseppe

“…Computer model depicting MG-2477 within the colchicine binding domain. We previously demonstrated that MG-2477 (3-cyclopropylmethyl-7-phenyl-3 H-pyrrolo[3,2-…”
Get full text

Synthesis and Biological Evaluation of Novel 2-Aroyl Benzofuran-Based Hydroxamic Acids as Antimicrotubule Agents by Mariotto, Elena, Canton, Martina, Marchioro, Chiara, Brancale, Andrea, Hamel, Ernest, Varani, Katia, Vincenzi, Fabrizio, De Ventura, Tiziano, Padroni, Chiara, Viola, Giampietro, Romagnoli, Romeo

“…Because of synergism between tubulin and HDAC inhibitors, we used the pharmacophore fusion strategy to generate potential tubulin-HDAC dual inhibitors. Drug…”
Get full text

Design, Synthesis, and Biological Evaluation of 5,6,7,8-Tetrahydrobenzo[4,5]thieno[2,3- d ]pyrimidines as Microtubule Targeting Agents by Islam, Farhana, Doshi, Arpit, Robles, Andrew J, Quadery, Tasdique M, Zhang, Xin, Zhou, Xilin, Hamel, Ernest, Mooberry, Susan L, Gangjee, Aleem

“…A series of eleven 4-substituted 5,6,7,8-tetrahydrobenzo[4,5]thieno[2,3- ]pyrimidines were designed and synthesized and their biological activities were…”
Get full text

Toward Highly Potent Cancer Agents by Modulating the C‑2 Group of the Arylthioindole Class of Tubulin Polymerization Inhibitors by La Regina, Giuseppe, Bai, Ruoli, Rensen, Whilelmina Maria, Di Cesare, Erica, Coluccia, Antonio, Piscitelli, Francesco, Famiglini, Valeria, Reggio, Alessia, Nalli, Marianna, Pelliccia, Sveva, Da Pozzo, Eleonora, Costa, Barbara, Granata, Ilaria, Porta, Amalia, Maresca, Bruno, Soriani, Alessandra, Iannitto, Maria Luisa, Santoni, Angela, Li, Junjie, Miranda Cona, Marlein, Chen, Feng, Ni, Yicheng, Brancale, Andrea, Dondio, Giulio, Vultaggio, Stefania, Varasi, Mario, Mercurio, Ciro, Martini, Claudia, Hamel, Ernest, Lavia, Patrizia, Novellino, Ettore, Silvestri, Romano

“…New arylthioindole derivatives having different cyclic substituents at position 2 of the indole were synthesized as anticancer agents. Several compounds…”
Get full text

Synthesis and Biological Evaluation of New Antitubulin Agents Containing 2-(3',4',5'-trimethoxyanilino)-3,6-disubstituted-4,5,6,7-tetrahydrothieno[2,3- c ]pyridine Scaffold by Romagnoli, Romeo, Prencipe, Filippo, Oliva, Paola, Cacciari, Barbara, Balzarini, Jan, Liekens, Sandra, Hamel, Ernest, Brancale, Andrea, Ferla, Salvatore, Manfredini, Stefano, Zurlo, Matteo, Finotti, Alessia, Gambari, Roberto

“…Two novel series of compounds based on the 4,5,6,7-tetrahydrothieno[2,3- ]pyridine and 4,5,6,7-tetrahydrobenzo[ ]thiophene molecular skeleton, characterized by…”
Get full text

Synthesis and biological evaluation of indole-based, anti-cancer agents inspired by the vascular disrupting agent 2-(3′-hydroxy-4′-methoxyphenyl)-3-(3″,4″,5″-trimethoxybenzoyl)-6-methoxyindole (OXi8006) by MacDonough, Matthew T., Strecker, Tracy E., Hamel, Ernest, Hall, John J., Chaplin, David J., Trawick, Mary Lynn, Pinney, Kevin G.

“…The discovery of a 2-aryl-3-aroyl indole-based small-molecule inhibitor of tubulin assembly (referred to as OXi8006) inspired the design, synthesis, and…”
Get full text

New Arylthioindoles:  Potent Inhibitors of Tubulin Polymerization. 2. Structure−Activity Relationships and Molecular Modeling Studies by De Martino, Gabriella, Edler, Michael C, La Regina, Giuseppe, Coluccia, Antonio, Barbera, Maria Chiara, Barrow, Denise, Nicholson, Robert I, Chiosis, Gabriela, Brancale, Andrea, Hamel, Ernest, Artico, Marino, Silvestri, Romano

“…Arylthioindoles (ATIs) that possess a 3-methoxyphenylthio or a 3,5-dimethoxyphenylthio moiety at position 2 of the indole ring were effective tubulin assembly…”
Get full text

Optimization of 4‑(N‑Cycloamino)phenylquinazolines as a Novel Class of Tubulin-Polymerization Inhibitors Targeting the Colchicine Site by Wang, Xiao-Feng, Guan, Fang, Ohkoshi, Emika, Guo, Wanjun, Wang, Lili, Zhu, Dong-Qing, Wang, Sheng-Biao, Wang, Li-Ting, Hamel, Ernest, Yang, Dexuan, Li, Linna, Qian, Keduo, Morris-Natschke, Susan L, Yuan, Shoujun, Lee, Kuo-Hsiung, Xie, Lan

“…The 6-methoxy-1,2,3,4-tetrahydroquinoline moiety in prior leads 2-chloro- and 2-methyl-4-(6-methoxy-3,4-dihydroquinolin-1­(2H)-yl)­quinazoline (1a and 1b) was…”
Get full text

New Indole Tubulin Assembly Inhibitors Cause Stable Arrest of Mitotic Progression, Enhanced Stimulation of Natural Killer Cell Cytotoxic Activity, and Repression of Hedgehog-Dependent Cancer by La Regina, Giuseppe, Bai, Ruoli, Coluccia, Antonio, Famiglini, Valeria, Pelliccia, Sveva, Passacantilli, Sara, Mazzoccoli, Carmela, Ruggieri, Vitalba, Verrico, Annalisa, Miele, Andrea, Monti, Ludovica, Nalli, Marianna, Alfonsi, Romina, Di Marcotullio, Lucia, Gulino, Alberto, Ricci, Biancamaria, Soriani, Alessandra, Santoni, Angela, Caraglia, Michele, Porto, Stefania, Da Pozzo, Eleonora, Martini, Claudia, Brancale, Andrea, Marinelli, Luciana, Novellino, Ettore, Vultaggio, Stefania, Varasi, Mario, Mercurio, Ciro, Bigogno, Chiara, Dondio, Giulio, Hamel, Ernest, Lavia, Patrizia, Silvestri, Romano

“…We designed 39 new 2-phenylindole derivatives as potential anticancer agents bearing the 3,4,5-trimethoxyphenyl moiety with a sulfur, ketone, or methylene…”
Get full text

Concise Synthesis and Biological Evaluation of 2‑Aroyl-5-Amino Benzo[b]thiophene Derivatives As a Novel Class of Potent Antimitotic Agents by Romagnoli, Romeo, Baraldi, Pier Giovanni, Lopez-Cara, Carlota, Preti, Delia, Aghazadeh Tabrizi, Mojgan, Balzarini, Jan, Bassetto, Marcella, Brancale, Andrea, Fu, Xian-Hua, Gao, Yang, Li, Jun, Zhang, Su-Zhan, Hamel, Ernest, Bortolozzi, Roberta, Basso, Giuseppe, Viola, Giampietro

“…The biological importance of microtubules make them an interesting target for the synthesis of antitumor agents. The…”
Get full text

Synthesis and Biological Evaluation of 2-Substituted Benzyl-/Phenylethylamino-4-amino-5-aroylthiazoles as Apoptosis-Inducing Anticancer Agents by Oliva, Paola, Onnis, Valentina, Balboni, Elisa, Hamel, Ernest, Estévez-Sarmiento, Francisco, Quintana, José, Estévez, Francisco, Brancale, Andrea, Ferla, Salvatore, Manfredini, Stefano, Romagnoli, Romeo

“…Induction of apoptosis is a common chemotherapeutic mechanism to kill cancer cells The thiazole system has been reported over the past decades as a building…”
Get full text

Design, Synthesis and Biological Investigation of 2-Anilino Triazolopyrimidines as Tubulin Polymerization Inhibitors with Anticancer Activities by Romagnoli, Romeo, Oliva, Paola, Prencipe, Filippo, Manfredini, Stefano, Budassi, Federica, Brancale, Andrea, Ferla, Salvatore, Hamel, Ernest, Corallo, Diana, Aveic, Sanja, Manfreda, Lorenzo, Mariotto, Elena, Bortolozzi, Roberta, Viola, Giampietro

“…A further investigation aiming to generate new potential antitumor agents led us to synthesize a new series of twenty-two compounds characterized by the…”
Get full text

Design, synthesis, and biological evaluation of water-soluble amino acid prodrug conjugates derived from combretastatin, dihydronaphthalene, and benzosuberene-based parent vascular disrupting agents by Devkota, Laxman, Lin, Chen-Ming, Strecker, Tracy E., Wang, Yifan, Tidmore, Justin K., Chen, Zhi, Guddneppanavar, Rajsekhar, Jelinek, Christopher J., Lopez, Ramona, Liu, Li, Hamel, Ernest, Mason, Ralph P., Chaplin, David J., Trawick, Mary Lynn, Pinney, Kevin G.

“…[Display omitted] Targeting tumor vasculature represents an intriguing therapeutic strategy in the treatment of cancer. In an effort to discover new vascular…”
Get full text

Synthesis and Biological Evaluation of Highly Active 7-Anilino Triazolopyrimidines as Potent Antimicrotubule Agents by Oliva, Paola, Romagnoli, Romeo, Cacciari, Barbara, Manfredini, Stefano, Padroni, Chiara, Brancale, Andrea, Ferla, Salvatore, Hamel, Ernest, Corallo, Diana, Aveic, Sanja, Milan, Noemi, Mariotto, Elena, Viola, Giampietro, Bortolozzi, Roberta

“…Two different series of fifty-two compounds, based on 3',4',5'-trimethoxyaniline ( ) and variably substituted anilines ( ) at the 7-position of the…”
Get full text

Synthesis and evaluation of diaryl sulfides and diaryl selenide compounds for antitubulin and cytotoxic activity by dos Santos, Edson dos A., Hamel, Ernest, Bai, Ruoli, Burnett, James C., Tozatti, Camila Santos Suniga, Bogo, Danielle, Perdomo, Renata T., Antunes, Alexandra M.M., Marques, M. Matilde, Matos, Maria de F.C., de Lima, Dênis P.

“…We have devised a procedure for the synthesis of analogs of combretastatin A-4 (CA-4) containing sulfur and selenium atoms as spacer groups between the…”
Get full text

Antiproliferative Aspidosperma-Type Monoterpenoid Indole Alkaloids from Bousigonia mekongensis Inhibit Tubulin Polymerization by Zhang, Yu, Goto, Masuo, Oda, Akifumi, Hsu, Pei-Ling, Guo, Ling-Li, Fu, Yan-Hui, Morris-Natschke, Susan L, Hamel, Ernest, Lee, Kuo-Hsiung, Hao, Xiao-Jiang

“…Monoterpenoid indole alkaloids are structurally diverse natural products found in plants of the family Apocynaceae. Among them, vincristine and its derivatives…”
Get full text