DESIGN AND SYNTHESIS OF 4-(2-PYRROLYL)-4-PHENYLHEPTANE DERIVATIVES AS ESTROGEN RECEPTOR ANTAGONISTS

Naganuma Miyako; Yokoo Hidetomo; Misawa Takashi; Matsuno Kenji; Tsuji Genichiro; Demizu Yosuke

首页> 外文期刊>Heterocycles: An International Journal for Reviews and Communications in Heterocyclic Chemistry >DESIGN AND SYNTHESIS OF 4-(2-PYRROLYL)-4-PHENYLHEPTANE DERIVATIVES AS ESTROGEN RECEPTOR ANTAGONISTS

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DESIGN AND SYNTHESIS OF 4-(2-PYRROLYL)-4-PHENYLHEPTANE DERIVATIVES AS ESTROGEN RECEPTOR ANTAGONISTS

机译：作为雌激素受体拮抗剂的4-（2-吡咯基）-4-苯基庚烷衍生物的设计与合成

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The estrogen receptor (ER) has been recognized as a potential target for the treatment of breast cancer, which is the most common malignancy found in woman. In this study, a series of 4-(2-pyrrolyl)-4-phenylheptane derivatives as ER antagonists were designed and synthesized. The ER antagonistic activity of these compounds was evaluated to study their structure-activity relationships.

机译：雌激素受体（ER）被认为是治疗乳腺癌的潜在目标，这是女性中最常见的恶性肿瘤。在该研究中，设计并合成了一系列4-（2-吡咯基）-4-苯基庚烷衍生物作为ER拮抗剂。评价这些化合物的ER拮抗活性以研究其结构活性关系。

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《Heterocycles: An International Journal for Reviews and Communications in Heterocyclic Chemistry》 |2020年第2期|共6页
作者
Naganuma Miyako; Yokoo Hidetomo; Misawa Takashi; Matsuno Kenji; Tsuji Genichiro; Demizu Yosuke;
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Natl Inst Hlth Sci Div Organ Chem Kawasaki Ku 3-25-26 Tonomachi Kawasaki Kanagawa 2109501 Japan;

Natl Inst Hlth Sci Div Organ Chem Kawasaki Ku 3-25-26 Tonomachi Kawasaki Kanagawa 2109501 Japan;

Natl Inst Hlth Sci Div Organ Chem Kawasaki Ku 3-25-26 Tonomachi Kawasaki Kanagawa 2109501 Japan;

Kogakuin Univ Dept Chem &

Life Sci 2665-1 Nakano Machi Hachioji Tokyo 1920015 Japan;

Natl Inst Hlth Sci Div Organ Chem Kawasaki Ku 3-25-26 Tonomachi Kawasaki Kanagawa 2109501 Japan;

Natl Inst Hlth Sci Div Organ Chem Kawasaki Ku 3-25-26 Tonomachi Kawasaki Kanagawa 2109501 Japan;

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1. DESIGN AND SYNTHESIS OF 4-(2-PYRROLYL)-4-PHENYLHEPTANE DERIVATIVES AS ESTROGEN RECEPTOR ANTAGONISTS [J] . Naganuma Miyako, Yokoo Hidetomo, Misawa Takashi, Heterocycles: An International Journal for Reviews and Communications in Heterocyclic Chemistry . 2020,第2期

机译：作为雌激素受体拮抗剂的4-（2-吡咯基）-4-苯基庚烷衍生物的设计与合成
2. Design, synthesis and biological evaluation of 1,4-dihydrothieno 3′,2′:5,6thiopyrano 4,3-cpyrazole-3-carboxylic amide derivatives as potential estrogen receptor antagonists [J] . Rui Sun, Jing Song, Si Jie Liu, 中国化学快报（英文版） . 2011,第003期

机译：1,4-二氢噻吩并3'，2'：5,6硫代吡喃并4,3-c吡唑-3-羧酸酰胺衍生物作为潜在雌激素受体拮抗剂的设计，合成及生物学评价
3. Design and synthesis of 2-(4-(4-(m-(ethylsulfonamido)-phenyl) piperazin-1-yl)butyl)-1,3-dioxoperhydropyrrolo(1,2-c)imidazole (EF-7412) using neural networks. A selective derivative with mixed 5-HT1A/D2 antagonist properties. [J] . Lopez Rodriguez-ML, Morcillo MJ, Fernandez E, Bioorganic and Medicinal Chemistry Letters . 1999,第12期

机译：使用神经网络设计和合成2-（4-（4-（间-（乙基-磺酰胺基）-苯基）哌嗪-1-基）丁基）-1,3-二氧杂氢吡咯并（1,2-c）咪唑（EF-7412）网络。具有5-HT1A / D2拮抗剂混合特性的选择性衍生物。
4. Design and synthesis of bifunctional peptides:antagonists at CCKA/CCKB receptors and agonists as mu/delta opioid receptors [C] . Richard S.Agnes, Yeon Sun Lee, Peg Davis, the International Peptide Symposium . 2001

机译：双官能肽的设计与合成：Ccka / Cckb受体的拮抗剂和穆/δ阿片受体的激动剂
5. Design, synthesis and docking models of estrogen and androgen receptor antagonists. [D] . Tinder, Robert J. 2010

机译：雌激素和雄激素受体拮抗剂的设计，合成和对接模型。
6. Design and Synthesis of 4-(4-Benzoylaminophenoxy)phenolDerivatives As Androgen Receptor Antagonists [O] . Ayumi Yamada, Shinya Fujii, *, 2013

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7. Spiro-Substituted Piperidines as Neurokinin Receptor Antagonists. I. Design and Synthesis of (.+-.)-N-(2-(3,4-Dichlorophenyl)-4-(spiro(isobenzofuran-1(3H),4'-piperidin)-1'-yl)butyl)-N-methylbenzamide, YM-35375, as a New Lead Compound for Novel Neurokinin Receptor Antagonists. [O] . Hirokazu KUBOTA, Masahiro FUJII, Ken IKEDA, 1998

机译：螺替代的哌啶作为神经激素受体拮抗剂。 I.（。+ - 。） - N-（2-（3,4-二氯苯基）-4-（螺呋喃 - 1（3H），4'-哌啶）-1'-y1）丁基的设计和合成）-N-甲基苄酰胺，YM-35375，作为新型神经蛋白受体拮抗剂的新型铅化合物。

DESIGN AND SYNTHESIS OF 4-(2-PYRROLYL)-4-PHENYLHEPTANE DERIVATIVES AS ESTROGEN RECEPTOR ANTAGONISTS

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