Studies on cyclin-dependent kinase inhibitors: indolo-[2,3- a ]pyrrolo[3,4- c ]carbazoles versus bis-indolylmaleimides

Autor:	Concha Sanchez-Martinez, Chuan Shih, Richard M. Schultz, Guoxin Zhu, Charles D. Spencer, Tiechao Li, Catherine A. Ogg, Bharvin K. R. Patel, Eileen L. Considine, Jack A. Dempsey, Faming Zhang, Harold B. Brooks, Tammy B. DeHahn, Scott A. Watkins
Rok vydání:	2003
Předmět:	Stereochemistry Clinical Biochemistry Carbazoles Molecular Conformation Pharmaceutical Science Antineoplastic Agents Crystallography X-Ray Biochemistry Chemical synthesis Structure-Activity Relationship chemistry.chemical_compound Polycyclic compound Cyclin-dependent kinase Cell Line Tumor Drug Discovery Humans Structure–activity relationship Pyrroles Enzyme Inhibitors Imide Molecular Biology chemistry.chemical_classification biology Bicyclic molecule Chemistry Organic Chemistry Flow Cytometry Cyclin-Dependent Kinases In vitro Enzyme inhibitor biology.protein Molecular Medicine Drug Screening Assays Antitumor Cell Division
Zdroj:	Bioorganic & Medicinal Chemistry Letters. 13:3841-3846
ISSN:	0960-894X
Popis:	A series of indolo[2,3-a]pyrrolo[3,4-c]carbazoles and their bis-indolylmaleimides precursors have been prepared in order to compare their activity as D1-CDK4 inhibitors. Both enzymatic and antiproliferative assays have shown that the structurally more constrained indolo[2,3-a]pyrrolo[3,4-c]carbazoles are consistently more active (8-42-fold) in head-to-head comparison with their bis-indolylmaleimides counterparts. Cell-cycle analysis using flow cytometry have also shown that the indolocarbazoles are selective G1 blockers while the bis-indolylmaleimides arrest cells in the G2/M phase.
Databáze:	OpenAIRE
Externí odkaz:	https://explore.openaire.eu/search/publication?articleId=doi_dedup___::859dd25d9a43bc2311db2a97d9975f4c https://doi.org/10.1016/s0960-894x(03)00792-3 Zobrazit plný text záznamu Full Text from ScienceDirect