Synthesis and Antitumor Activities of Novel Methylthio-, Sulfinyl-, and Sulfonyl-8H-thieno[2,3-b]pyrrolizin-8-oximino Derivatives
| Autor: | Sisi Zhang, Lijun Xie, Shuchun Guo, Xianglin Zhao, Yanfang Zhao, Weiyong Kong, Ping Gong |
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| Rok vydání: | 2007 |
| Předmět: |
Antitumor activity
Cisplatin Sulfonyl chemistry.chemical_classification Stereochemistry Chemistry Mtt method Pharmaceutical Science Antineoplastic Agents General Medicine medicine.disease Thiophene derivatives Combinatorial chemistry In vitro Human liver cancer Structure-Activity Relationship Cell culture Cell Line Tumor Drug Discovery medicine Humans Pyrroles Sarcoma medicine.drug |
| Zdroj: | ChemInform. 38 |
| ISSN: | 1522-2667 0931-7597 |
| DOI: | 10.1002/chin.200748109 |
| Popis: | A series of novel methylthio-, sulfinyl-, and sulfonyl-8H-thieno[2,3-b]pyrrolizin-8-oximino derivatives 7A-12P was designed and synthesized as anti-tumor agents. Their structures were confirmed by IR, (1)H-NMR, MS, and elemental analysis. The anti-tumor activities of all the target compounds were tested by the MTT method in vitro against Bel-7402 (human liver cancer) and HT-1080 (human fibro sarcoma) cell lines. Among them, compound 11N (IC(50) = 18.2 microM, 8.2 microM), was the most promising compound of all synthesized molecules, it was 2.5- and 3.3-times more active than cisplatin (IC(50) = 45.2 microM, 26.7 microM), respectively. |
| Databáze: | OpenAIRE |
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