مورد إلكتروني
Structure-activity relationship analysis of novel derivatives of narciclasine (an Amaryllidaceae isocarbostyril derivative) as potential anticancer agents.
| العنوان: | Structure-activity relationship analysis of novel derivatives of narciclasine (an Amaryllidaceae isocarbostyril derivative) as potential anticancer agents. |
|---|---|
| المؤلفون: | Ingrassia, Laurent, Lefranc, Florence, Dewelle, Janique, Pottier, Laurent, Mathieu, Véronique, Spiegl-Kreinecker, Sabine, Sauvage, Sébastien, El Yazidi, Mohamed, Dehoux, Mischaël, Berger, Walter, Van Quaquebeke, Eric, Kiss, Robert |
| المصدر: | Journal of medicinal chemistry, 52 (4 |
| بيانات النشر: | 2009-02 |
| نوع الوثيقة: | Electronic Resource |
| مستخلص: | Narciclasine (1) is a plant growth regulator that has been previously demonstrated to be proapoptotic to cancer cells at high concentrations (> or = 1 microM). Data generated in the present study show that narciclasine displays potent antitumor effects in apoptosis-resistant as well as in apoptosis-sensitive cancer cells by impairing the organization of the actin cytoskeleton in cancer cells at concentrations that are not cytotoxic (IC(50) values of 30-90 nM). The current study further revealed that any chemical modification to the narciclasine backbone generally led to compounds of variable stability, weaker activity, or even the complete loss of antiproliferative effects in vitro. However, one hemisynthetic derivative of narciclasine, compound 7k, demonstrated by both the intravenous and oral routes higher in vivo antitumor activity in human orthotopic glioma models in mice when compared to narciclasine at nontoxic doses. Narciclasine and compound 7k may therefore be of potential use to combat brain tumors. Journal Article Research Support, Non-U.S. Gov't SCOPUS: ar.j info:eu-repo/semantics/published |
| مصطلحات الفهرس: | Sciences bio-médicales et agricoles, Amaryllidaceae Alkaloids -- chemistry, Amaryllidaceae Alkaloids -- pharmacology, Animals, Antineoplastic Agents -- chemistry, Antineoplastic Agents -- pharmacology, Cell Proliferation, Drug Administration Routes, Drug Stability, Glioma -- drug therapy, Humans, Mice, Phenanthridines -- chemistry, Phenanthridines -- pharmacology, Structure-Activity Relationship, Xenograft Model Antitumor Assays, info:eu-repo/semantics/article, info:ulb-repo/semantics/articlePeerReview, info:ulb-repo/semantics/openurl/article |
| URL: | |
| الإتاحة: | Open access content. Open access content |
| ملاحظة: | No full-text files English |
| أرقام أخرى: | EQY oai:dipot.ulb.ac.be:2013/51195 uri/info:doi/10.1021/jm8013585 uri/info:pii/10.1021/jm8013585 uri/info:pmid/19199649 uri/info:scp/64349093471 764592898 |
| المصدر المساهم: | UNIVERSITE LIBRE DE BRUXELLES From OAIster®, provided by the OCLC Cooperative. |
| رقم الأكسشن: | edsoai.ocn764592898 |
| قاعدة البيانات: | OAIster |
| الوصف غير متاح. |