Synthesis and Antitumor Activity of Novel Pyrimidinyl Pyrazole Derivatives
スポンサーリンク
概要
- 論文の詳細を見る
Novel pyrimidinyl pyrazole derivatives were synthesized and examined for cytotoxic and antitumor activity. Mannich reaction was employed to construct this scaffold. Among the compounds synthesized, a series of propene derivatives exhibited a potent cytotoxic activity against some tumor cell lines including multidrug resistant cell lines due to the overexpression of P-glycoprotein. The vinyl bond moiety in the scaffold was believed to be required for the cytotoxic activity. Among them, compound 14g, when administered intraperitoneally, showed potent antitumor activity against the malignant ascites caused by intraperitoneal inoculation of P388 cells in mice. This compound also showed high activity against a solid tumor Meth A mouse fibrosarcoma when administered both intraperitoneally and orally.
- 公益社団法人日本薬学会の論文
- 1999-12-15
著者
-
中村 康彦
Department Of Formulation Research Dainippon Pharmaceutical Co. Ltd.
-
KUMAZAWA Eiji
New Product Research Laboratories IV, Daiichi Pharmaceutical Co., Ltd.
-
Kumazawa E
New Product Research Laboratories Iii Daiichi Pharmaceutical Co. Ltd.
-
Naito H
Medicinal Chemistry Research Laboratory Daiichi Pharmaceutical Co. Ltd.
-
Naito Hiroyuki
Department Of Veterinary Science Azabu University
-
Nakamura Yoshihide
Technical Department Fuji Chemical Industries Co. Ltd.
-
Nakamura Y
Tohoku Pharmaceutical Univ. Sendai Jpn
-
Kumazawa Eiji
New Product Research Laboratories Iii Daiichi Pharmaceutical Co. Ltd.
-
Ejima A
Medicinal Chemistry Research Laboratory Daiichi Pharmaceutical Co. Ltd.
-
SUGIMORI Masamichi
Discovery Research Laboratory
-
ISHII Mineko
New Product Research Laboratories III, Daiichi Pharmaceutical Co., Ltd.
-
HIROTANI Kenji
New Product Research Laboratories III, Daiichi Pharmaceutical Co., Ltd.
-
NAITO Hiroyuki
New Product Research Laboratories IV, Daiichi Pharmaceutical Co., Ltd.,
-
SUGIMORI Masamichi
Basic Technology Research Laboratory, Daiichi Pharmaceutical Co., Ltd.,
-
MITSUI Ikuo
Basic Technology Research Laboratory, Daiichi Pharmaceutical Co., Ltd.,
-
IWAHANA Michio
New Product Research Laboratories IV, Daiichi Pharmaceutical Co., Ltd.,
-
EJIMA Akio
New Product Research Laboratories IV, Daiichi Pharmaceutical Co., Ltd.,
-
Ishii M
Department Of Physical Chemistry Graduate School Of Pharmaceutical Sciences Chiba University
-
Mitsui Ikuo
New Product Research Laboratories Iv Daiichi Pharmaceitucal Co. Ltd.
-
Iwahana M
Daiichi Pharmaceutical Co. Ltd. Tokyo Jpn
-
Hirotani K
Discovery Research Laboratory Daiichi Pharmaceutical Co. Ltd.
-
Nakamura Y
Department Of Pharmacognosy Tohoku Pharmaceutical University
-
Iwahana Michio
New Product Research Laboratories Iv Daiichi Pharmaceutical Co. Ltd.
関連論文
- An Extract of the Root of Lithospermun erythrorhison Accelerates Wound Healing in Diabetic Mice
- Antitumor Effect of DX-8951, a Novel Camptothecin Analog, on Human Pancreatic Tumor Cells and Their CPT-11-resistant Variants Cultured in vitro and Xenografted into Nude Mice
- Substrate Deacylation Mechanism of Serine beta-lactamases
- Controlled Release by Ca^-Sensitive Recombinant Human Tumor Necrosis Factor-α Liposomes
- Cryoprotective Effect of Gelatin and Albumin on Recombinant Human Tumor Necrosis Factor Liposome
- Synthesis in Vitro Antifungal Activities of Novel Triazole Antifungal Agent CS-758
- Multiparticulate Chitosan-Dispersed System for Drug Delivery
- Design of Controlled Release System with Multi-layers of Powder
- DE-310, a novel macromolecular carrier system for the camptothecin analog DX-8951f : Potent antitumor activities in various murine tumor models
- A New Water-soluble Camptothecin Derivative, DX-8951f, Exhibits Potent Antitumor Activity against Human Tumors in vitro and in vivo
- Design of Novel Controlled-Release Suppositories Containing Polyglycerol Ester of Fatty Acid
- Influence of Solid Fat Index in Triglyceride Suppository Bases on Drug Release
- Antitumor-Promoting Constituents from Chaenomeles sinensis KOEHNE and Their Activities in JB6 Mouse Epidermal Cells
- Antitumor-Promoting Constituents from Dioscorea bulbifera L. in JB6 Mouse Epidermal Cells
- Synthesis and Evaluation of Water-Soluble Non-Prodrug Analogs of Docetaxel Bearing sec-Aminoethyl Group at the C-10 Position
- Studies on Cardiac Ingredients of Plants. XIII : Chemical Modification of Gitoxin to Cardiotonic Compounds without Vascular Contractile Effect
- AN UNUSUAL FLUORIDE-MEDIATED OXIDATION OF GITOXIN
- Isolation and Characterization of Cytotoxic Compounds from Corn
- Effect of Lactational Exposure to Tributyltin Chloride on Innate Immunodefenses in the F1 Generation in Mice
- Effect of Lactational Exposure to 2,3,7,8-Tetrachlorodibenzo-p-dioxin on the Susceptibility to Listeria Infection(Food & Nutrition Science)
- Catalytic Mechanism of Class A β-Lactamase. I. The Role of Glu166 and Ser130 in the Deacylation Reaction
- Synthesis and Antitumor Activity of Novel Pyrimidinyl Pyrazole Derivatives. II. Optimization of the Phenylpiperazine Moiety of 1- [5-Methyl-1-(2-pyrimidinyl)-4-pyrazolyl]-3-phenylpiperazinyl-1-trans-propenes
- Synthesis and Antifungal Activities of R-102557 and Related Dioxane-Triazole Derivatives
- Synthesis and Antitumor Activity of Novel Pyrimidinyl Pyrazole Derivatives
- Pipelining Gauss Seidel Method for Analysis of Discrete Time Cellular Neural Networks
- Effect of Saiko-ka-ryukotsu-borei-to on Amylase Activity in Mice(Pharmacognosy)
- Synthesis and Antitumor Activity of Novel Pyrimidinyl Pyrazole Derivatives. III. Synthesis and Antitumor Activity of 3-Phenylpiperazinyl-1-trans-propenes
- Synthesis and Antitumor Activity of Novel Benzophenone Derivatives
- Synthesis and Structure-Activity Relationships of Novel 2', 2'-Difluoro Analogues of Docetaxel
- Sensitization from cobalt chloride by patch testing