Design, Synthesis and Biological Evaluation of Some 5-Arylthieno[2,3-d]pyrimidines as Potential Anti-cancer Agents
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- El-Ansary Afaf Kamal
- Pharmaceutical Organic Chemistry Department, Faculty of Pharmacy, Cairo University
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- Kamal Aliaa Mohammed
- Pharmaceutical Organic Chemistry Department, Faculty of Pharmacy, Cairo University
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- Al-Ghorafi Mokhtar Abd-Hafiz
- Pharmaceutical Organic Chemistry Department, Faculty of Pharmacy, Cairo University
書誌事項
- タイトル別名
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- Design, Synthesis and Biological Evaluation of Some 5-Arylthieno[2,3-<i>d</i>]pyrimidines as Potential Anti-cancer Agents
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<p>Structure-based design, synthesis and biological evaluation of new small molecules anti-cancer agents were described. On continuation of applying scaffold hopping theory, a series of 5-arylthieno[2,3-d]pyrimidines based on the structural features of lapatinib was designed, synthesized and characterized using IR, 1H-NMR, 13C-NMR, mass and microanalyses. Biological evaluation of the cytotoxic activity against MCF-7 cell line and the inhibition of the enzymatic activity of epidermal growth factor tyrosine kinase were carried out in vitro for the target compounds. Substituting the 4-anilino-5-arylthieno[2,3-d]pyrimidines with different pharmacophoric groups at ortho, meta and/or para positions led to discovery of two potent lead compounds 3b and f with excellent cytotoxic activity and enzymatic inhibition activity.</p>
収録刊行物
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- CHEMICAL & PHARMACEUTICAL BULLETIN
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CHEMICAL & PHARMACEUTICAL BULLETIN 64 (8), 1172-1180, 2016
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
- 1390282679155679232
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- NII論文ID
- 130005253949
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- NII書誌ID
- AA00602100
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- ISSN
- 13475223
- 00092363
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- NDL書誌ID
- 027523024
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- PubMed
- 27477657
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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
- Crossref
- PubMed
- CiNii Articles
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- 抄録ライセンスフラグ
- 使用不可