Synthesis and biological evaluation of N-heterocyclic indolyl glyoxylamides as orally active anticancer agents
| Autor: | Yue Kan Lo, Der Ren Hwang, Yee Ling Chang, Chi Hung Lin, Shu-Jen Chen, Se Hui Wu, Ching Ping Chen, Chu Chung Lin, Chen Long Huang, Chiung-Tong Chen, Ying Ying Chang, Huan Yi Tseng, Chien Wei Shen, Jeng Shin Song, Tung Wei Chen, Hua Chien Chen, Wen-Tai Li |
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| Rok vydání: | 2003 |
| Předmět: |
Indoles
Administration Oral Antineoplastic Agents Apoptosis chemistry.chemical_compound Mice Structure-Activity Relationship Drug Discovery medicine Tumor Cells Cultured Animals Humans Cytotoxicity Leukemia P388 Cancer Glyoxylates medicine.disease In vitro Drug Resistance Multiple Thiazoles Biochemistry chemistry Cell culture Drug Resistance Neoplasm Mice Inbred DBA Cancer cell Cancer research Molecular Medicine DNA fragmentation Female Growth inhibition Drug Screening Assays Antitumor Cell Division Neoplasm Transplantation |
| Zdroj: | Journal of medicinal chemistry. 46(9) |
| ISSN: | 0022-2623 |
| Popis: | A series of N-heterocyclic indolyl glyoxylamides were synthesized and evaluated for in vitro and in vivo anticancer activities. They exhibited a broad spectrum of anticancer activity not only in murine leukemic cancer cells but also in human gastric, breast, and uterus cancer cells as well as their multidrug resistant sublines with a wide range of IC(50) values. They also induced apoptosis and caused DNA fragmentation in human gastric cancer cells. Among the compounds studied, 7 showed the most potent activity of growth inhibition (IC(50) = 17-1711 nM) in several human cancer cells. Given orally, compounds 7 and 13 dose-dependently prolonged the survival of animals inoculated with P388 leukemic cancer cells. N-Heterocyclic indolyl glyoxylamides may be useful as orally active chemotherapeutic agents against cancer and refractory cancerous diseases of multidrug resistance phenotype. |
| Databáze: | OpenAIRE |
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