Synthesis, anticancer activity and mitochondrial mediated apoptosis inducing ability of 2,5-diaryloxadiazole–pyrrolobenzodiazepine conjugates

Synthesis, anticancer activity and mitochondrial mediated apoptosis inducing ability of 2,5-diaryloxadiazole–pyrrolobenzodiazepine conjugates

New class of 2,5-diaryloxadiazole–pyrrolobenzodiazepine conjugates have been prepared and evaluated for their anticancer activity. Further, some of the biological assays related to mechanism aspects have also been carried out. A series of 2,5-diaryloxadiazole linked pyrrolo[2,1-c][1,4]benzodiazepine...

Ausführliche Beschreibung

Gespeichert in:
Bibliographische Detailangaben
Veröffentlicht in:Bioorganic & medicinal chemistry 2010-09, Vol.18 (18), p.6666-6677
Hauptverfasser: Kamal, Ahmed, Dastagiri, D., Ramaiah, M. Janaki, Bharathi, E. Vijaya, Reddy, J. Surendranadha, Balakishan, G., Sarma, Pranjal, Pushpavalli, S.N.C.V.L., Pal-Bhadra, Manika, Juvekar, Aarti, Sen, Subrata, Zingde, Surekha
Format: Artikel
Sprache:eng
Schlagworte:
2,5-Diaryloxadiazoles
Animals
Anticancer activity
Antineoplastic agents
Antineoplastic Agents - chemical synthesis
Antineoplastic Agents - chemistry
Antineoplastic Agents - therapeutic use
Apoptosis
bcl-2-Associated X Protein - metabolism
Benzodiazepines - chemical synthesis
Benzodiazepines - chemistry
Benzodiazepines - therapeutic use
Biological and medical sciences
Caspases
Caspases - metabolism
Cell Cycle - drug effects
Cell Line, Tumor
Cyclin dependent kinase-2 (CDK-2)
Cyclin-Dependent Kinase 2 - metabolism
General aspects
Humans
Male
Medical sciences
Mice
Mice, Inbred NOD
Miscellaneous
Mitochondria - drug effects
Neoplasms - drug therapy
Oxadiazoles - chemical synthesis
Oxadiazoles - chemistry
p53
Pharmacology. Drug treatments
Pyrrolobenzodiazepine
Tumor Suppressor Protein p53 - metabolism
Xenograft Model Antitumor Assays
Online-Zugang:Volltext
Tags: Tag hinzufügen
Keine Tags, Fügen Sie den ersten Tag hinzu!
Beschreibung
Zusammenfassung:New class of 2,5-diaryloxadiazole–pyrrolobenzodiazepine conjugates have been prepared and evaluated for their anticancer activity. Further, some of the biological assays related to mechanism aspects have also been carried out. A series of 2,5-diaryloxadiazole linked pyrrolo[2,1-c][1,4]benzodiazepine conjugates have been prepared and evaluated for their anticancer activity. These conjugates have shown promising activity with GI50 values ranging from
ISSN:0968-0896
1464-3391
DOI:10.1016/j.bmc.2010.07.067