Synthesis and Anti-tumor Activities of Novel Methylthio-, Sulfinyl-, and Sulfonyl-8H-thieno[2,3-b]pyrrolizin-8-oximino Derivatives

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, 1H‐NMR, MS, and elemental analysis. The anti‐tumor activities of all the target compounds were test...

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Bibliographic Details
Published in:Archiv der Pharmazie (Weinheim) 2007-08, Vol.340 (8), p.416-423
Main Authors: Guo, Shuchun, Zhao, Yanfang, Zhao, Xianglin, Zhang, Sisi, Xie, Lijun, Kong, Weiyong, Gong, Ping
Format: Article
Language:English
Subjects:
3-b]pyrrolizines
Anti-tumor activities
Antineoplastic Agents - chemical synthesis
Antineoplastic Agents - pharmacology
Cell Line, Tumor
Humans
Pyrroles - chemical synthesis
Pyrroles - pharmacology
Structure-Activity Relationship
Synthesis
Thieno
Thieno[2,3‐b]pyrrolizines
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Summary: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, 1H‐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 (IC50 = 18.2 μM, 8.2 μM), was the most promising compound of all synthesized molecules, it was 2.5‐ and 3.3‐times more active than cisplatin (IC50 = 45.2 μM, 26.7 μM), respectively.
ISSN:0365-6233
1521-4184
DOI:10.1002/ardp.200700044