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310 results on '"Menendez, J. Carlos"'

4. Bifunctional carbazole derivatives for simultaneous therapy and fluorescence imaging in prion disease murine cell models

Author

Staderini, Matteo, Vanni, Silvia, Baldeschi, Arianna Colini, Giachin, Gabriele, Zattoni, Marco, Celauro, Luigi, Ferracin, Chiara, Bistaffa, Edoardo, Moda, Fabio, Pérez, Daniel I., Martínez, Ana, Martín, M. Antonia, Martín-Cámara, Olmo, Cores, Ángel, Bianchini, Giulia, Kammerer, Robert, Menéndez, J. Carlos, Legname, Giuseppe, and Bolognesi, Maria Laura

Published
2023
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32. A new route toward 4-substituted pyrazino[2,1-b]quinazoline-3,6-dione systems. total synthesis of glyantrypine

Author

Cledera, pilar, Avendano, Carmen, and Menendez, J. Carlos

Subjects
Organic compounds -- Synthesis, Natural products -- Composition, Glycine -- Usage, Ring formation (Chemistry) -- Analysis, Biological sciences, Chemistry
Abstract

The retrosynthetic route for preparing 1,2-unsubstituted pyrazino[2,1-b]quinazoline-3,6-diones starts with the unprotected glycine derivatives and double cyclization of open-chain 'tripeptides', in which the N-terminal residue is the anthranilic acid unit bearing an azido group with an amino function.

Published
2000

34. New synthetic applications of aryllead triacetates. N-Arylation of amides

Author

Lopez-Alvarado, Pilar, Avendano, Carmen, and Menendez, J. Carlos

Subjects
Amides -- Research, Organic compounds -- Synthesis, Organometallic compounds -- Usage, Biological sciences, Chemistry
Abstract

Aryllead triacetates were utilized for the N-arylation of amides in the presence of two important functional groups, the amino and beta-dicarbonyl units. p-Tollylead was employed as a model reagent. Results revealed the efficient arylation of nucleophilic carbon atoms including those in beta-dicarbonyl compounds. The efficient arylation of the nitrogen atom of carboxamide, sulfonamide, imide and hydantoin anions was also observed.

Published
1996

35. New synthetic applications of aryllead triacetates: N-arylation of azoles

Author

Lopez-Alvarado, Pilar, Avendano, Carmen, and Menendez, J. Carlos

Subjects
Triacetate -- Research, Halides -- Research, Aromatic compounds -- Research, Biological sciences, Chemistry
Abstract

Excellent yields of the corresponding N-aryl derivatives were obtained by the arylation of diazoles and triazoles or their anions by p-tolyllead triacetate in the presence of copper-(II) acetate. This method allows for the efficient N-arylation of azoles, under mild conditions and with yields that are usually excellent and reproducible. It was also observed that azole nitrogen atoms do not interfere with the arylation of aromatic amino groups.

Published
1995

37. List of contributors

Author

Aharoni, Rina, Ahmad, Zulfiqar, Akhtar, Suhail, Atmuri, N. D. Prasad, Avendaño, Carmen, Banga, Ivneet, Bel, Shai, Berlicki, Łukasz, Blumberg, Yair, Bourguet, Carine, Cardoso, Marlon Henrique, Choudhury, Samraggi, Diarra, Sitan, Driessen, Marvin N., Dunn, Michael K., Duong, Vandon T., Ertracht, Offir, Ferro, Emer S., Franco, Octavio Luiz, Galochkina, Tatiana, Gandhi, Sonu, Ge, Shikun, Gelly, Jean-Christophe, Gewehr, Mayara C.F., Ghorpade, Rujuta, Gross, Eric R., Hanout, Wessal, Harris, Tamia A., Joseph, Adrienne, Kannan, Srinivasaraghavan, Kappo, Abidemi Paul, Kumar, Krishna, Kumar, Maushmi S., Lama, Dilraj, Lau, Jolene L., Li, Jianguo, Litmanovich, Adi, Liu, Jamie, Lubell, William D., Mabonga, Lloyd, Mahari, Subhasis, Masamba, Priscilla, Menéndez, J. Carlos, Moady, Gassan, Nanjappan, Satheesh Kumar, Navon, Ami, Neundorf, Ines, Nuriel-Ohayon, Meital, Orlov, Dmitriy, Paul, David, Piran, Ron, Porto, William Farias, Qvit, Nir, Rubin, Samuel J.S., Saad, Mussa, Shahdeo, Deepshikha, Shamova, Olga, Sicinski, Kathleen M., Singh, Abhishek, Sirhan, Worood, Surendran, Shruti, Surprenant, Simon, Tan, Yaw Sing, Thakur, Mukesh, Umnyakova, Ekaterina, Ünsal, Özge, Verma, Chandra S, Wagner, Nana-Maria, Wang, Zhipeng A., Xie, Bryan J., Xu, Long, Zambelli, Vanessa O., Zhang, Xiaoying, and Zheng, Ji-Shen

Published
2022
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38. L-proline-catalyzed three-component domino [3+2+1] annulation for the regio- and diastereoselective synthesis of highly substituted thienothiopyrans containing three or four stereocenters

Author

Indumathi, Sethuraman, Perumal, Subbu, and Menendez, J. Carlos

Subjects
Aldehydes -- Chemical properties, Aldehydes -- Structure, Elimination reactions -- Usage, Proline -- Chemical properties, Proline -- Structure, Biological sciences, Chemistry
Abstract

A variety of highly substituted thieno[3,2-c]thiopyran derivatives are furnished through L-proline-catalyzed three-component reactions of ethyl 2-[(2-oxo-2-arylethyl)sulfonyl]acetate or ethyl 2-[(2-ethoxy-2-oxoethyl)sulfonyl]acetate, aromatic aldehydes, and 5-aryltetrahydro-3-thiophenone. The facile transformations are assumed to occur via a one-pot domino sequence of enamine formation/aldol condensation/Michael addition/6-exo-trig cyclization/elimination and involved the creation in a single operation of three C-C bonds.

Published
2010

39. Efficient generation of highly functionalized fused oxazepine frameworks based on a CAN-catalyzed four-component tetrahydropyridine synthesis/ring-closing metathesis sequence

Author

Sridharan, Vellaisamy, Maiti, Swarupananda, and Menendez, J. Carlos

Subjects
Allylic compounds -- Chemical properties, Allylic compounds -- Structure, Pyridine -- Chemical properties, Pyridine -- Structure, Biological sciences, Chemistry
Abstract

The transformation of 1-a llyl(propargyl)-6-allyl(propargyl)oxy-1,4,5,6-tetrahydropyridines, obtained through a CAN-catalyzed four-component reaction into highly functionalized pyrido[2,1-b][1,3]oxazepines is described. The process involved ring-closing metathesis (RCM) and ring-closing enyne metathesis (RCEYM) which comprise the first examples of the preparation of 1,3-oxazepine systems utilizing metathesis reactions.

Published
2009

40. Cerium(IV) ammonium nitrate is an excellent, general catalyst for the Friedlander and Friedlander-Borsche quinoline syntheses: very efficient access to the antitumor alkaloid luotonin A

Author

Sridharan, Vellaisamy, Ribelles, Pascual, Ramos, Ma Teresa, and Menendez, J. Carlos

Subjects
Cerium -- Usage, Cerium -- Research, Chemical reactions -- Research, Quinoline -- Research, Biological sciences, Chemistry
Abstract

Cerium(IV) ammonium nitrate is used as a catalyst of the Friedlander reaction that has allowed the synthesis of polysubstituted quinoline derivatives, avoiding the traditionally harshly basic or acidic conditions. CAN has allowed double condensations and is also an excellent catalyst for the Borsche variation of the Friedlander reaction, which is applied to the efficient synthesis of the antitumor alkaloid luotonin A.

Published
2009

41. Correction to Tetrahydroisoquinoline-Derived Urea and 2,5-Diketopiperazine Derivatives as Selective Antagonists of the Transient Receptor Potential Melastatin 8 (TRPM8) Channel Receptor and Antiprostate Cancer Agents (vol 59, pg 5661, 2016)

Author

De Petrocellis, Luciano, Arroyo, Francisco J., Orlando, Pierangelo, Moriello, Aniello Schiano, Vitale, Rosa Maria, Amodeo, Pietro, Sanchez, Aranzazu, Roncero, Cesareo, Bianchini, Giulia, Martin, M. Antonia, Lopez-Alvarado, Pilar, and Menendez, J. Carlos

Subjects
anti-prostate cancer activity, Tetrahydroisoquinolines, ureas, apoptosis, TRPM8 channels, diketopiperazines
Abstract

Tetrahydroisoquinoline derivatives containing embedded urea functions were identified as selective TRPM8 channel receptor antagonists. Structure-activity relationships were investigated, with the following conclusions: (a) The urea function and the tetrahydroisoquinoline system are necessary for activity. (b) Bis(1-aryl-6,7dimethoxy-1,2,3,4-tetrahydroisoquinolyl)ureas are more active than compounds containing one tetrahydroisoquinoline ring and than an open phenetylamine ureide. (c) Trans compounds are more active than their cis isomers. (d) Aryl substituents are better than alkyls at the isoquinoline C-1 position. (e) Electron-withdrawing substituents lead to higher activities. The most potent compound is the 4-F derivative, with IC50 in the 10(-8) M range and selectivities around 1000:1 for most other TRP receptors. Selected compounds were found to be active in reducing the growth of LNCaP prostate cancer cells. TRPM8 inhibition reduces proliferation in the tumor cells tested but not in nontumor prostate cells, suggesting that the activity against prostate cancer is linked to TRPM8 inhibition.

Published
2016
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42. Brief total synthesis of the cell cycle inhibitor tryptostatin B and related preparation of its alanine analogue

Author

Caballero, Esmeralda, Avendano, Carmen, and Menendez, J. Carlos

Subjects
Cyclic compounds -- Composition, Alanine, Chemical inhibitors, Organic compounds -- Composition, Chemistry, Organic -- Research, Biological sciences, Chemistry
Abstract

Research has been conducted on tryptostatin B. The authors describe the strategy developed for the synthesis of this compound which is based on the preparation of a fused pentacyclic compound from cyclo-(L-Tpr-L-Pro) and the rearrangement of the prenyl chain.

Published
2003

49. Medicinal Chemistry of Anticancer Drugs Ed. 2

Author

Avendano, Carmen, Menendez, J. Carlos, Avendano, Carmen, Avendano, Carmen, Menendez, J. Carlos, and Avendano, Carmen

Abstract

Medicinal Chemistry of Anticancer Drugs, Second Edition, provides an updated treatment from the point of view of medicinal chemistry and drug design, focusing on the mechanism of action of antitumor drugs from the molecular level, and on the relationship between chemical structure and chemical and biochemical reactivity of antitumor agents. Antitumor chemotherapy is a very active field of research, and a huge amount of information on the topic is generated every year. Cytotoxic chemotherapy is gradually being supplemented by a new generation of drugs that recognize specific targets on the surface or inside cancer cells, and resistance to antitumor drugs continues to be investigated. While these therapies are in their infancy, they hold promise of more effective therapies with fewer side effects. Although many books are available that deal with clinical aspects of cancer chemotherapy, this book provides a sorely needed update from the point of view of medicinal chemistry and drug design.Presents information in a clear and concise way using a large number of figuresHistorical background provides insights on how the process of drug discovery in the anticancer field has evolvedExtensive references to primary literature

Published
2015

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