Synthesis and Structure−Activity Relationship of 2-Aminobenzophenone Derivatives as Antimitotic Agents
| Autor: | Ching-Fang Yeh, Jing Ping Liou, Yi Ling Chang, Yung Ning Yang, Hsing Pang Hsieh, Yu Kang Lo, Huan Yi Tseng, Jeng Shin Song, Chungming Chang, Chun Wei Chang |
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| Rok vydání: | 2002 |
| Předmět: |
Stereochemistry
Mitosis Antineoplastic Agents Binding Competitive Chemical synthesis Benzophenones Structure-Activity Relationship chemistry.chemical_compound Biopolymers DU145 Tubulin Drug Discovery Tumor Cells Cultured Humans Structure–activity relationship Cytotoxicity chemistry.chemical_classification Combretastatin Aromatic amine Solubility chemistry Biochemistry Molecular Medicine Antimitotic Agent Drug Screening Assays Antitumor Growth inhibition Colchicine |
| Zdroj: | Journal of Medicinal Chemistry. 45:2556-2562 |
| ISSN: | 1520-4804 0022-2623 |
| Popis: | A new type of inhibitor of tubulin polymerization was discovered on the basis of the combretastatin molecular skeleton. The lead compounds in this series, compounds 6 and 7, strongly inhibited tubulin polymerization in vitro and significantly arrested cells at the G(2)/M phase. Compounds 6 and 7 yielded 50- to 100-fold lower IC(50) values than did combretastatin A-4 against Colo 205, NUGC3, and HA22T human cancer cell lines as well as similar or greater growth inhibitory activities than did combretastain A-4 against DLD-1, HR, MCF-7, DU145, HONE-1, and MES-SA/DX5 human cancer cell lines. Structure-activity relationship information revealed that introduction of an amino group at the ortho position of the benzophenone ring plays an integral role for increased growth inhibition. |
| Databáze: | OpenAIRE |
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