Uses of Cyclohexan-1,4-dione for the Synthesis of 2-Amino-4,5-dihydrobenzo[b]thiophen-6(7H)-one Derivatives with Anti-proliferative and Pim-1 Kinase Activities
-
- Mohareb Rafat Milad
- Department of Chemistry, Faculty of Science, Cairo University
-
- Abbas Nermeen Saeed
- Department of Chemistry, Faculty of Science, Helwan University Department of Chemistry, Faculty of Science, Taibah University
-
- Ibrahim Rehab Ali
- Institute of Engineering and Technology
書誌事項
- タイトル別名
-
- Uses of Cyclohexan-1,4-dione for the Synthesis of 2-Amino-4,5-dihydrobenzo[<i>b</i>]thiophen-6(7<i>H</i>)-one Derivatives with Anti-proliferative and Pim-1 Kinase Activities
この論文をさがす
説明
<p>The reaction of cyclohexan-1,4-dione with elemental sulfur and any of the 2-cyano-N-arylacetamide derivatives 2a–c gave the 2-amino-4,5-dihydrobenzo[b]thiophen-6(7H)-one derivatives 3a–c to be used in some heterocyclization reactions. The multicomponent reactions of any of compounds 3a–c with aromatic aldehydes 6a–c and either of malononitrile or ethylcyanoacetate gave the 5,9-dihydro-4H-thieno[2,3-f]chromene derivatives 9a–r, respectively. The anti-proliferative evaluation of the newly synthesized compounds against the six cancer cell lines A549, HT-29, MKN-45, U87MG, SMMC-7721 and H460 showed that the nine compounds 3c, 5c, 9e, 9h, 9i, 9j, 9l, 9q, 11e and 13e with highest cytotoxcity. Toxicity of these compounds against shrimp larvae revealed that compounds 3c, 9j, 9q, and 13e showed no toxicity against the tested organisms. The c-Met kinase inhibition of the most potent compounds showed that compounds 9j, 9q, 10e, 12e and 13e have the highest activities. Compounds 9j, 9l, 9q and 11e showed high activity towards tyrosine kinases. Moreover, compounds 9j, 9q and 13e showed the highest inhibitor activity towards Pim-1 kinase.</p>
収録刊行物
-
- CHEMICAL & PHARMACEUTICAL BULLETIN
-
CHEMICAL & PHARMACEUTICAL BULLETIN 65 (12), 1117-1131, 2017
公益社団法人 日本薬学会
- Tweet
詳細情報 詳細情報について
-
- CRID
- 1390282679153930240
-
- NII論文ID
- 130006235014
-
- NII書誌ID
- AA00602100
-
- ISSN
- 13475223
- 00092363
-
- NDL書誌ID
- 028675181
-
- PubMed
- 29199218
-
- 本文言語コード
- en
-
- データソース種別
-
- JaLC
- NDL
- Crossref
- PubMed
- CiNii Articles
-
- 抄録ライセンスフラグ
- 使用不可