Synthesis and Biological Evaluation of 16E-Arylidenosteroids as Cytotoxic and Anti-aromatase Agents
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- Bansal Ranju
- University Institute of Pharmaceutical Sciences, Sector-14, Panjab University
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- Guleria Sheetal
- University Institute of Pharmaceutical Sciences, Sector-14, Panjab University
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- Thota Sridhar
- University Institute of Pharmaceutical Sciences, Sector-14, Panjab University
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- Hartmann Rolf Wolfgang
- Pharmaceutical and Medicinal Chemistry, Saarland University
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- Zimmer Christina
- Pharmaceutical and Medicinal Chemistry, Saarland University
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Taking into consideration the structural requirements for cytotoxicity and aromatase inhibition, several new 16E-arylidenosteroidal derivatives have been prepared and evaluated for their cytotoxic and aromatase inhibitory activity. The new steroidal analogues 3, 5—8 and 11 exhibited significant cytotoxic effects when screened against three cancer cell lines, MCF-7 (breast), NCl-H460 (lung) and SF-268 central nervous system (CNS) at 100 μM and sensible cytotoxic effects subsequently in sixty cancer cell lines derived from nine cancers types (leukemia, lung, colon, CNS, melanoma, ovarian, renal, prostate and breast cancers). The imidazolyl substituted steroidal derivatives 5 and 7 exhibited strong inhibition of the aromatase enzyme with 16-[4-{3-(imidazol-1-yl)propoxy}-3-methoxybenzylidene]-5-androstene-3β,17β-diol (7) displaying 13 times more potency in comparison to aminoglutethimide.
収録刊行物
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- ＣＨＥＭＩＣＡＬ ＆ ＰＨＡＲＭＡＣＥＵＴＩＣＡＬ ＢＵＬＬＥＴＩＮ
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ＣＨＥＭＩＣＡＬ ＆ ＰＨＡＲＭＡＣＥＵＴＩＣＡＬ ＢＵＬＬＥＴＩＮ 59 (3), 327-331, 2011
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
- 1390001204172729728
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- NII論文ID
- 130000648940
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- NII書誌ID
- AA00602100
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- ISSN
- 13475223
- 00092363
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- NDL書誌ID
- 10990467
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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
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