α-substituted 1-aryl-3-dimethylaminopropanone hydrochlorides: potent cytotoxins towards human WiDr colon cancer cells
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- Pati Hari Narayan
- College of Pharmacy and Nutrition, University of Saskatchewan
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- Das Umashankar
- College of Pharmacy and Nutrition, University of Saskatchewan
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- Dimmock Jonathan Richard
- College of Pharmacy and Nutrition, University of Saskatchewan
書誌事項
- タイトル別名
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- .ALPHA.-Substituted 1-Aryl-3-dimethylaminopropanone Hydrochlorides: Potent Cytotoxins towards Human WiDr Colon Cancer Cells
- アルファ substituted 1 aryl 3 dimethylaminopropanone hydrochlorides potent cytotoxins towards human WiDr colon cancer cells
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説明
A series of 1-aryl-2-dimethylaminomethyl-2-propenone hydrochlorides 1 were prepared which possessed IC50 values of less than 10 μM when examined towards human WiDr colon cancer cells. The related 1-aryl-2-dimethylaminomethyl-3-hydroxypropanone hydrochlorides 2, formed by hydration of the analogs in series 1, also had IC50 values in the low micromolar range. On the other hand, conversion of 2-dimethylaminomethyl-1-(4-nitrophenyl)-2-propenone hydrochloride 1c into the corresponding 2-mercaptoethanol of adduct 3c led to a 37-fold reduction in potency. Two thirds of the compounds prepared in this study were more potent than a reference drug cisplatin while one third of these molecules displayed greater cytotoxicity to the WiDr cells than human CRL-2522 fibroblasts. A stability study of the 4-nitrophenyl analog in each of the series 1—3 in deuterium oxide was undertaken. In the case of 1c, replacement of the dimethylamino hydrochloride group by a hydroxy function was noted while in series 2, the loss of both water and dimethylamine hydrochloride gave rise to a mixture of two enones. The mercaptoethanol adduct 3c underwent deamination. The data obtained provide guidelines for amplifying the project in the future.
収録刊行物
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- CHEMICAL & PHARMACEUTICAL BULLETIN
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CHEMICAL & PHARMACEUTICAL BULLETIN 55 (4), 511-515, 2007
公益社団法人 日本薬学会
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詳細情報 詳細情報について
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- CRID
- 1390282679147313024
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- NII論文ID
- 110006241807
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- NII書誌ID
- AA00602100
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- ISSN
- 13475223
- 00092363
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- NDL書誌ID
- 8691065
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- 本文言語コード
- en
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- データソース種別
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- JaLC
- NDL
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