L. M. MARTIN CABREJAS

Imidazolyl benzimidazoles and imidazo[4,5-b]pyridines as potent p38α MAP kinase inhibitors with excellent in vivo antiinflammatory properties

Mary M. Mader, Alfonso de Dios, Chuan Shih, Rosanne Bonjouklian et autres

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Design of Potent and Selective 2-Aminobenzimidazole-Based p38α MAP Kinase Inhibitors with Excellent in Vivo Efficacy

Alfonso de Dios, Chuan Shih, Beatriz López de Uralde, Concepción Sánchez et autres

We report the design and discovery of a 2-aminobenzimidazole-based series of potent and highly selective p38alphainhibitors. The lead compound 1 had low-nanomolar activity in both ATP competitive enzyme binding and inhibition of TNFalpha release in macrophages. Compound 18 showed excellent pharmacokinetics properties …

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Acyl sulfonamide anti-proliferatives. Part 2: Activity of heterocyclic sulfonamide derivatives

Mary M. Mader, Chuan Shih, Eileen L. Considine, Alfonso de Dios et autres

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Acyl Sulfonamide Anti-Proliferatives: Benzene Substituent Structure−Activity Relationships for a Novel Class of Antitumor Agents

Karen L. Lobb, Philip A. Hipskind, James Aikins, Enrique L. Álvarez et autres

Two closely related diaryl acylsulfonamides were recently reported as potent antitumor agents against a broad spectrum of human tumor xenografts (colon, lung, breast, ovary, and prostate) in nude mice. Especially intriguing was their activity against colorectal cancer xenografts. In this paper, rapid …

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Sanglifehrin−Cyclophilin Interaction: Degradation Work, Synthetic Macrocyclic Analogues, X-ray Crystal Structure, and Binding Data

Richard Sedrani, Jörg Kallen, L. M. MARTIN CABREJAS, Charles D. Papageorgiou et autres

Sanglifehrin A (SFA) is a novel immunosuppressive natural product isolated from Streptomyces sp. A92-308110. SFA has a very strong affinity for cyclophilin A (IC(50) = 6.9 +/- 0.9 nM) but is structurally different from cyclosporin A (CsA) and exerts its immunosuppressive activity …

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CCDC 208687: Experimental Crystal Structure Determination

Richard Sedrani, Joerg Kallen, L. M. MARTIN CABREJAS, Christos Papageorgiou et autres

An entry from the Cambridge Structural Database, the world’s repository for small molecule crystal structures. The entry contains experimental data from a crystal diffraction study. The deposited dataset for this entry is freely available from the CCDC and typically includes 3D coordinates, …

Synthesis of Macrolide Analogues of Sanglifehrin by RCM: Unique Reactivity of a Ruthenium Carbene Complex Bearing an Imidazol-2-ylidene Ligand

Jürgen Wagner, L. M. MARTIN CABREJAS, Catharine E. Grossmith, Charles D. Papageorgiou et autres

ADVERTISEMENT RETURN TO ISSUEPREVNoteNEXTSynthesis of Macrolide Analogues of Sanglifehrin by RCM: Unique Reactivity of a Ruthenium Carbene Complex Bearing an Imidazol-2-ylidene LigandJürgen Wagner, Luisa M. Martin Cabrejas, Catharine E. Grossmith, Charles Papageorgiou, Francesco Senia, Dieter Wagner, Julien France, and Steven P. NolanView …

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ChemInform Abstract: Macrolide Analogues (II) of the Novel Immunosuppressant Sanglifehrin: New Application of the Ring‐Closing Metathesis Reaction.

L. M. MARTIN CABREJAS, Stefan Rohrbach, Dieter Wagner, Joerg Kallen et autres

Abstract ChemInform is a weekly Abstracting Service, delivering concise information at a glance that was extracted from about 100 leading journals. To access a ChemInform Abstract of an article which was published elsewhere, please select a “Full Text” option. The original article …

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Macrolide Analogues of the Novel Immunosuppressant Sanglifehrin: New Application of the Ring-Closing Metathesis Reaction

L. M. MARTIN CABREJAS, Stefan Rohrbach, Dieter Wagner, Jörg Kallen et autres

Macrocycles containing a conjugated 1,3-diene moiety have been synthesized for the first time in good yields by the ring-closing metathesis reaction [Eq. (1)]. The new compounds represent cyclophilin-binding, simplified analogues of the macrocyclic core of sanglifehrin A, an immunosuppressant which binds with …

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Makrolidanaloga des neuartigen Immunsuppressivums Sanglifehrin: eine neue Anwendung der Ringschluß-Metathese

L. M. MARTIN CABREJAS, Stefan Rohrbach, Dieter Wagner, Jörg Kallen et autres

Makrocyclen mit einer konjugierten 1,3-Dien-Einheit wurden erstmals in guter Ausbeute in einer Ringschluß-Metathesereaktion synthetisiert [Gl. (1)]. Bei den neuen Verbindungen handelt es sich um Cyclophilin-bindende, vereinfachte Analoga des makrocyclischen Teils von Sanglifehrin A, einem Immunsuppressivum, das mit hoher Affinität an Cyclophilin bindet.

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ChemInform Abstract: Dienophilic Behavior of (S)‐2‐p‐Tolylsulfinyl Butenolide.

Juan C. Carretero, J.L.G. Ruano, L. M. MARTIN CABREJAS

Abstract ChemInform is a weekly Abstracting Service, delivering concise information at a glance that was extracted from about 100 leading journals. To access a ChemInform Abstract of an article which was published elsewhere, please select a “Full Text” option. The original article …

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ChemInform Abstract: Asymmetric Diels‐Alder Reaction of (S)‐α‐p‐Tolylsulfinyl α, β‐Unsaturated Esters: The Role of the Sulfinyl Group in Asymmetric Diels‐Alder Reactions of Vinylsulfoxides.

Juan C. Carretero, J.L.G. Ruano, L. M. MARTIN CABREJAS

Abstract ChemInform is a weekly Abstracting Service, delivering concise information at a glance that was extracted from about 100 leading journals. To access a ChemInform Abstract of an article which was published elsewhere, please select a “Full Text” option. The original article …