Synthesis and Antitumor Activity of Duocarmycin Derivatives : Modification of Segment A of Duocarmycin B2
スポンサーリンク
概要
- 論文の詳細を見る
Several A-ring pyrrole derivatives of duocarmycin B2 were synthesized effectively from the 3-hydroxy compounds by utilizing an interesting acid-catalyzed rearrangement, their anticellular activity was preliminarily evaluated by assays of growth inhibition of HeLa S_3 cells (in vitro) and antitumor activity against murine sarcoma 180 (in vivo). The 8-O-N, N-dialkylcarbamoyl derivatives of the A-ring pyrrole compound showed remarkably potent in vivo antitumor activity, superior to that of duocarmycin B2. These derivatives were subjected to further biological evaluation. They exhibited potent antitumor activity toward murine solid tumors including M5076 sarcoma, B-16 melanoma and Colon 26 adenocarcinoma. Their most noteworthy feature was their efficacy against various human xenografts including LC-6 (lung), St-4 (stomach), and Co-3 (colon).
- 公益社団法人日本薬学会の論文
- 1996-09-15
著者
-
Kobayashi E
Pharmaceutical Research Institute Kyowa Hakko Kogyo Company Ltd.
-
Asai Akira
Pharmaceutical Research Institute Kyowa Hakko Kogyo Co. Ltd.
-
Asai Akira
Kyowa Hakko Kogyo Co. Ltd.
-
斉藤 博満
協和発酵・東京研
-
NAGAMURA Satoru
Kyowa Hakko Kogyo Co., Ltd., Tokyo Research Laboratories
-
KANDA Yutaka
Kyowa Hakko Kogyo Co., Ltd., Tokyo Research Laboratories
-
SAITO Hiromitsu
Kyowa Hakko Kogyo Co., Ltd., Tokyo Research Laboratories
-
Asai Akira
Department Of Angiogenesis And Vascular Development Kanazawa University
-
Kanda Y
Fukuoka Inst. Techol. Fukuoka Jpn
-
Kanda Yutaka
Kyowa Hakko Kogyo Co. Ltd. Tokyo Research Laboratories
-
Saito Hideyuki
Department Of Pharmacology College Of Pharmacy Nihon University
-
Kobayashi E
Gifu Pharmaceutical University : Gifu Prefectural Institute Of Health And Environmental Sciences
-
Saito H
Department Of Pharmacology College Of Pharmacy Nihon University
-
Asai Akira
Laboratory Of Biodynamic Chemistry Tohoku University Graduate School Of Agriculture
-
Gomi Katsushige
Pharmaceutical Research Institute Kyowa Hakko Kogyo Company Ltd.
-
Nagamura S
Pharmaceutical Research Institute Kyowa Hakko Kogyo Company Ltd.
-
Nagamura Satoru
Kyowa Hakko Kogyo Co. Ltd.
関連論文
- Endogenous Cryogens Existing in the Blood of a Hypothermic Patient
- A young female patient suffering from hypothermia in a cool environment
- Modulation of Voltage-Gated Ca^ Current by 4-Hydroxynonenal in Dentate Granule Cells(Highlighted paper setected by Editor-in-cfiief)(Pharmacology)
- Protective effect of S-allyl-L-cysteine, a garlic compound, on amyloid β-protein-induced cell death in nerve growth factor-differentiated PC12 cells
- Morphine augments excitatory synaptic transmission in the dentate gyrus through GABAergic disinhibition
- 11 レイナマイシンの全合成(口頭発表の部)
- Does Helicobacter pylori eradication depend on the period of amoxicillin treatment? A retrospective study
- Pharmacokinetic Drug Interactions between Ampiroxicam and Sulfaphenazole in Rats
- 120(P64) 抗腫瘍性抗生物質レイナマイシンによるDNAアルキル化反応(ポスター発表の部)
- Synthesis and Antitumor Activity of Duocarmycin Derivatives : A-Ring Pyrrole Compounds Bearing 5-Membered Heteroarylacryloyl Groups
- Synthesis and Antitumor Activity of Duocarmycin Derivatives : Modification of Segment A of Duocarmycin B2
- Wagner-Meerwein Rearrangement of Duocarmycins
- Antioxidative Effects of Turmeric, Rosemary and Capsicum Extracts on Membrane Phospholipid Peroxidation and Liver Lipid Metabolism in Mice
- Pyrronamycin A and B, Novel Antitumor Antibiotics Containing Pyrrole-amide Repeating Unit, Produced by Streptomyces sp.
- UCT1072s, New Antitumor Antibiotics with Topoisomerase II Mediated DNA Cleavage Activity, from Aspergillus sp.
- Improvement of Fatigue and Acceleration of Recovery from Stress-Induced Deficient Sexual Behavior in Mice Following Oral Administration of Soft-Shelled Turtle Powder
- Anti-tumor Effects of Orally Administered Soft-Shelled Turtle Powder in Mice
- Effect of α-Galactosylceramides on Bone Marrow Cells in Vitro and Hematopoiesis in Vivo
- Enhancing Effects of Agelasphin-11 on Natural Killer Cell Activities of Normal and Tumor-Bearing Mice
- Suppression of Synaptogenesis by Epileptiform Discharges in Hippocampal Slice Culture
- Activin Selectively Abolishes Hippocampal Long-Term Potentiation Induced by Weak Tetanic Stimulation In Vivo
- Antiemetic Effects of Morphine on Motion- and Drug-Induced Emesis in Suncus murinus
- Furosemide : Sensitive Calcium Rise Induced by GABA_A : Receptor Stimulation in Cultures of Embryonic Rat Striatal Neurons
- Involvement of a Peripheral Mechanism in the Emesis Induced by Cardiac Glycosides in Suncus murinus
- Cytotoxic Benzophenone Derivatives from Garcinia Species Display a Strong Apoptosis-Inducing Effect against Human Leukemia Cell Lines
- Chrolactomycin, a Novel Antitumor Antibiotic Produced by Streptomyces sp.
- UCS1O25A, a Novel Antibiotic Produced by Acremonium sp.
- A-20. Clincial Consideration of the Ophthalmological Symptom on the Cerebral Aneurysm
- CP2289,a New 5-HT_3 Receptor Ligand : Agonistic Activities on Gastroenteric Motility
- CHARACTERIZATION OF RECEPTORS FOR HUMAN RECOMBINANT INTERFERON-γ IN HUMAN CELLS
- ANTITUMOR EFFECT OF HUMAN RECOMBINANT INTERFERON-γ AND -β AGAINST HUMAN OSTEOSARCOMA TRANSPLANTED INTO NUDE MICE
- SYNERGISTIC ANTICELLULAR AND ANTIVIRAL ACTIVITIES OF HUMAN RECOMBINANT INTERFERON-γ AND -β
- Synthesis and Antitumor Activity of Duocarmycin Derivatives
- Belactosin A, a Novel Antitumor Antibiotic Acting on Cyclin/CDK Mediated Cell Cycle Regulation, Produced by Streptomyces sp.
- A Case of Syringomyelia with Type I Arnold-Chiali Malformation(ACM):Growth Hormone(GH)Therapy and the Size of Syrinx on Serial MR Images
- タキソールに関する最近の合成研究
- L-Glutamate Suppresses Astrocyte Stellation Induced by Actin Breakdown in Culture
- Selective Cytotoxicity of Piperine on Cultured Rat Hippocampal Neurons in Comparison with Cultured Astrocytes : The Possible Involvement of Lipid Peroxidation
- Practical Preparation of K-252a from a Fermentation Solution
- ANTITUMOR EFFECT OF HUMAN RECOMBINANT INTERFERON-β AGAINST HUMAN MELANOMAS TRANSPLANTED INTO NUDE MICE
- Decreased Cyclosporin A Concentrations in the Absorption Phase Using Microemulsion Preconcentrate Formulation in Rats with Cisplatin-Induced Acute Renal Failure(Biopharmacy)