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Synthesis of Biotinylated Galiellalactone Analogues

International Journal of Organic Chemistry 2014年第4期4卷 225-235页

作者： Zilma Escobar Martin Johansson Anders Bjartell Rebecka Hellsten olov sterner Centre for Analysis and Synthesis Department of Chemistry Lund University Lund Sweden Division of Urological Cancers Department of Clinical Sciences Malm&ouml Lund University Malm&ouml Sweden

Two biotinylated derivatives of the fungal metabolite galiellalactone (1) were synthesized in order to facilitate the investigation of the molecular mechanism of action of the galiellalactonoids. Galiellalactone is a STAT3-signaling inhibitor that inhibits growth in vitro as well as in vivo of prostate cancer cells expressing activated STAT3. To provide a suitable point of attachment for biotin, the 8-hydroxymethyl derivative (3) and its 7-phenyl analogue 4 were synthesized by a modified tandem Pd-catalysed carbonylation and intramolecular vinyl allene Diels-Alder procedure previously developed. The two primary alcohols obtained, 3 and 4, were coupled to biotin as the 6-aminohexanoic acid amide, activated as the acid chloride, yielding the derivatives 5 and 6.

关键词： STAT3 Galiellalactone Biotin Synthesis

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Natural and Semi-Synthetic Pseudoguaianolides as Inhibitors of NF-κB

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Journal of Biomedical Science and Engineering 2014年第10期7卷 833-847页

作者： Rodrigo Villagomez Juan Antonio Collado Eduardo Munoz Giovanna Almanza olov sterner Center for Analysis and Synthesis Lund UniversityLundSweden Laboratorio de Bioorganica Instituto de Investigaciones QuímicasUniversidad Mayor de San AndrésLa PazBolivia Instituto Maimónides de Investigación Biomédica de Córdoba(IMIBIC) Departamento de Biología CelularFisiología e InmunologíaUniversidad de CórdobaCórdobaSpain

Damsin (1) is a natural pseudoguaianolide sesquiterpene that inhibits NF-κB, a protein complex that controls the transcription of DNA in mammalian cells, and has a potential for standing model for the development of new anti-cancer lead structures. In order to do a preliminary structure-activity study and improve the anti-cancer activity, fourteen derivatives and analogs were prepared and evaluated. These were chosen to represent both structural diversity and structural novelty. The importance of α methylene-γ-lactone moiety for the anti-cancer activity was confirmed, even though other features in the scaffold were shown to be important for the activity. In some cases a new substitution negatively affected the initial activity, however, two analogues, indolo [3,2-c]-4-desoxydamsin (5) and ambrosin (6), were found to be more potent.

关键词： Damsin α Methylene-γ-Lactone Sesquiterpenoids Anti-Cancer Activity

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3-Arylisothiazoloquinols as potent ligands for the benzodiazepine site of GABA_(A) receptors

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Journal of Biomedical Science and Engineering 2012年第1期5卷 1-9页

作者： Jakob Nilsson Elsebet Φstergaard Nielsen Tommy Liljefors Mogens Nielsen olov sterner Division of Organic Chemistry Lund UniversityLundSweden NeuroSearch A/S BallerupDenmark Faculty of Pharmaceutical Sciences University of CopenhagenCopenhagenDenmark

3-Arylisothiazolo[5,4-b]quinolin-4(9H)-ones and 3-arylisoxazolo[5,4-b]quinolin-4(9H)-ones were synthesized and assayed for affinity for the benzodiazepine binding site of the GABAA receptors. While the 3-arylisothiazoloquinolin-4-ones were found to be potent ligands, with affinities (expressed as the affinity Ki value) down to 1 nM, the 3-arylisoxazoloquinolin-4-ones are less potent. This is suggested to depend on sterical repulsive interaction of the 3-arylisoxazoloquinolin-4-ones with the receptor essential volume of the binding site, and a higher electron density at the nitrogen in the azole ring (N-2) as well as the carbonyl oxygen in the isothiazoloquinolin-4-ones enabling them to interact stronger with hydrogen bond donor sites at the binding site.

关键词： Isothiazolo[5,4-b]quinolin-4(9H)-ones Isoxazolo[5,4-b]quinolin-4(9H)-ones Benzodiazepine Binding Site GABAA Receptors GABA_(A) Receptor Subtypes Pharmacophore Model

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毛地黄黄酮和玄参黄酮抑制[~3H]地西泮和体外大鼠脑膜的结合(英文)

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中国药理学报 1994年第5期15卷 385-388页

作者：沈行良 Mogens NIELSEN Michael Robin WITT olov sterner Ola BERGENDORFF Mohammed KHAYYAL Department of Biochemistry Research Institute of Biological Psychiatry St Hans Hospital DK-4000 Roskilde Denmark Department of Organic Chemistry 2 University of Lund Lund Sweden Department of Pharmacology Faculty of Pharmacy Cairo University Cairo Egypt

从阿拉伯艾蒿提取到两种苯并二氮杂受体的配基,毛地黄黄酮和玄参黄酮。两种化合物在体外可抑制[~3H]地西泮和大鼠皮层细胞膜的结合,IC_(50)值分别为1.3μmol·L^(-1)和23μmol·L^(-1)。两种化合物GABA比分别为1.1和1.2,都可少量增加[... 详细信息

从阿拉伯艾蒿提取到两种苯并二氮杂受体的配基,毛地黄黄酮和玄参黄酮。两种化合物在体外可抑制[~3H]地西泮和大鼠皮层细胞膜的结合,IC_(50)值分别为1.3μmol·L^(-1)和23μmol·L^(-1)。两种化合物GABA比分别为1.1和1.2,都可少量增加[^(35)S]TBPS的结合,提示这种化合物是苯并二氮杂受体的拮抗剂或部分激动剂。

关键词：毛地黄黄酮脑细胞膜玄参黄酮

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从阿拉伯艾蒿分离到两种对苯并二氮杂和α_1肾上腺素能受体有亲和力的黄酮化合物(英文)

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中国药理学与毒理学杂志 1993年第4期7卷 305-306页

作者：沈行良 Michael RWITT Mogens NIELSEN Ola BERGENDORFF olov sterner Mohamed T KHAYYAL Taha SEL-ALFY Hamida EL-GOHARY Biochemical Research Laboratory St Hans Psychiatric HospitalRoskildeDenmark Department of Organic Chemistry 2 University of LundLundSweden Pharmacology Department Pharmacognosy Department Faculty of PharmacyCairo UniversityCairoEgypt

干燥阿拉伯艾蒿的酒精提取物对体外[~3H]地西泮和大鼠大脑皮质细胞膜结合产生抑制作用,两种化合物被分离纯化,其化学结构为毛地黄黄酮和玄参黄酮(IC_(50)分别为1.3±s0.1和22.7±S2.5μmol·L^1),两种化合物在体外还能抑制[~3H]哌唑嗪... 详细信息

干燥阿拉伯艾蒿的酒精提取物对体外[~3H]地西泮和大鼠大脑皮质细胞膜结合产生抑制作用,两种化合物被分离纯化,其化学结构为毛地黄黄酮和玄参黄酮(IC_(50)分别为1.3±s0.1和22.7±S2.5μmol·L^1),两种化合物在体外还能抑制[~3H]哌唑嗪和大鼠脑皮质细胞膜结合,但不能改变[~3H]蝇蕈碱乙酰胆碱受体,[~3H]蝇蕈醇,[~3H]SCH 23390和[~3H]螺哌隆和膜的结合,Scatchard plot分析提示两种化合物对[~3H]地西泮和膜结合的抑制作用是通过竟争性和非竞争性混合机理而实现的。

关键词：阿拉伯艾蒿黄酮类受体,苯并二氮类脑

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INHIBITION OF KAINIC ACID BINDING TO GLUTAMATE RECEPTORS BY EXTRACTS OF GASTRODIA

INHIBITION OF KAINIC ACID BINDING TO GLUTAMATE RECEPTORS BY ...

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作者： MARLA ANDERSSON OLA BERGENDORFF MOGENS NIELSEN olov sterner ROBN WITT JINGLU AI AIPING LU AN MIN WANG Department of Biochemistry Sct.Hans HospitalDK-4000 RoskildeDenmark Division of Organic Chemistry 2 University of LundP.O.Box 124S-22100 Lund.Sweden Division of Organic Chemistry 2 University of LundP.O.Box 124S-221 00 Lund.Sweden Institute of Basic Theory China Academy of Traditional Chinese MedicineBeijing 10700China

INTRODUCTION Gastrodia elata BL.is used as an anticonvulsant,an analgesic and a sedative against vertigo,general paralysis,epilepsy and tetanus,and is listed in the Chinese Pharma—copoeia[1].During a screening of the inhibitory activity of extracts of Chinese medicinal plants in a CNS receptor radioligand binding assay in vitro,water extracts of G.elata inhibited the binding of[H]kainic acid.Kainic acid is a potent neurotoxin in the CNS and its neurotoxic activity is presumed to be mediated by binding and subsequent activation of the

关键词： Index—Gastrodia elata Orchidaceae Kainic acid glutamate receptor glutathione derivative

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