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Verfasst von:Petersen, Asger B. [VerfasserIn]   i
 Konotop, Gleb [VerfasserIn]   i
 Hanafiah, Nur Hafzan Md [VerfasserIn]   i
 Raab, Marc-Steffen [VerfasserIn]   i
 Krämer, Alwin [VerfasserIn]   i
Titel:Synthesis and formulation studies of griseofulvin analogues with improved solubility and metabolic stability
Verf.angabe:Asger B. Petersen, Nikolaj S. Andersen, Gleb Konotop, Nur Hafzan Md Hanafiah, Marc S. Raab, Alwin Krämer, Mads H. Clausen
E-Jahr:2017
Jahr:22 February 2017
Umfang:8 S.
Fussnoten:Gesehen am 08.08.2018
Titel Quelle:Enthalten in: European journal of medicinal chemistry
Ort Quelle:Amsterdam [u.a.] : Elsevier Science, 1987
Jahr Quelle:2017
Band/Heft Quelle:130(2017), Seite 240-247
ISSN Quelle:1768-3254
Abstract:Griseofulvin (1) is an important antifungal agent that has recently received attention due to its antiproliferative activity in mammalian cancer cells. Comprehensive SAR studies have led to the identification of 2′-benzyloxy griseofulvin 2, a more potent analogue with low micromolar anticancer potency in vitro. Analogue 2 was also shown to retard tumor growth through inhibition of centrosomal clustering in murine xenograft models of colon cancer and multiple myeloma. However, similar to griseofulvin, compound 2 exhibited poor metabolic stability and aqueous solubility. In order to improve the poor pharmacokinetic properties, 11 griseofulvin analogues were synthesized and evaluated for biological activity and physiological stabilities including SGF, plasma, and metabolic stability. Finally, the most promising compounds were investigated in respect to thermodynamic solubility and formulation studies. The 2′-benzylamine analogue 10 proved to be the most promising compound with low μM in vitro anticancer potency, a 200-fold increase in PBS solubility over compound 2, and with improved metabolic stability. Furthermore, this analogue proved compatible with formulations suitable for both oral and intravenous administration. Finally, 2′-benzylamine analogue 10 was confirmed to induce G2/M cell cycle arrest in vitro.
DOI:doi:10.1016/j.ejmech.2017.02.055
URL:Bitte beachten Sie: Dies ist ein Bibliographieeintrag. Ein Volltextzugriff für Mitglieder der Universität besteht hier nur, falls für die entsprechende Zeitschrift/den entsprechenden Sammelband ein Abonnement besteht oder es sich um einen OpenAccess-Titel handelt.

Volltext: http://dx.doi.org/10.1016/j.ejmech.2017.02.055
 Volltext: http://www.sciencedirect.com/science/article/pii/S0223523417301289
 DOI: https://doi.org/10.1016/j.ejmech.2017.02.055
Datenträger:Online-Ressource
Sprache:eng
Sach-SW:Cancer
 Centrosomal clustering
 Formulations
 Griseofulvin
 Pharmacokinetics
 Solubility
K10plus-PPN:1578387930
Verknüpfungen:→ Zeitschrift

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