論文 - 詳細
| RRC ID | 62197 |
|---|---|
| 著者 | Galal SA, Hegab KH, Hashem AM, Youssef NS. |
| タイトル | Synthesis and antitumor activity of novel benzimidazole-5-carboxylic acid derivatives and their transition metal complexes as topoisomerease II inhibitors. |
| ジャーナル | Eur J Med Chem |
| Abstract |
N-aminomethyl-1H-benzimidazole-5-carboxylic acid derivatives 2-5 and the ligand, 1-(5 (or 6-)-carboxy-1H-benzimidazol-2-ylmethyl)pyridinium chloride (6; H2L1) have been synthesized. New benzimidazole complexes 7-9 of the ligand 6; H2L1 with Cu2+, Co2 and Zn2+ were prepared. The growth-inhibitory against a panel of 21 human cancer cell lines of the synthesized compounds 1-9 was studied. Compounds 6-9 showed potent growth-inhibitory activity against the studied cell lines. The correlation coefficients according to COMPARE analysis of the National Cancer Institute screening protocol showed that the pattern of the growth-inhibitory effect of the compounds 6-9 was similar to that of etoposide and doxorubicin but different from that of SN-38 and cisplatin. The topoisomerase II inhibitory activity of the tested compounds 6-9 was studied. Compounds 6 and 8 inhibited topoisomerase II activity at 10 times lower concentration than etoposide in relaxation assay. |
| 巻・号 | 45(12) |
| ページ | 5685-91 |
| 公開日 | 2010-12-1 |
| DOI | 10.1016/j.ejmech.2010.09.023 |
| PII | S0223-5234(10)00671-9 |
| PMID | 20884089 |
| MeSH | Animals Antineoplastic Agents / chemical synthesis Antineoplastic Agents / chemistry Antineoplastic Agents / pharmacology* Benzimidazoles / chemical synthesis Benzimidazoles / chemistry Benzimidazoles / pharmacology* Carboxylic Acids / chemical synthesis Carboxylic Acids / chemistry Carboxylic Acids / pharmacology* Cell Line, Tumor Cell Proliferation / drug effects DNA Topoisomerases, Type II / metabolism* Drug Screening Assays, Antitumor Enzyme Inhibitors / chemical synthesis Enzyme Inhibitors / chemistry Enzyme Inhibitors / pharmacology* Humans Mice Molecular Structure Organometallic Compounds / chemical synthesis Organometallic Compounds / chemistry Organometallic Compounds / pharmacology* Stereoisomerism Structure-Activity Relationship |
| IF | 5.573 |
| リソース情報 | |
| ヒト・動物細胞 | HGC-27(RCB0500) |