bafilomycin-a1 and sclareol

bafilomycin-a1 has been researched along with sclareol* in 1 studies

Other Studies

1 other study(ies) available for bafilomycin-a1 and sclareol

Article	Year
Design and Synthesis of Antitumor Heck-Coupled Sclareol Analogues: Modulation of BH3 Family Members by SS-12 in Autophagy and Apoptotic Cell Death. Journal of medicinal chemistry, 2015, Apr-23, Volume: 58, Issue:8 Sclareol, a promising anticancer labdane diterpene, was isolated from Salvia sclarea. Keeping the basic stereochemistry-rich framework of the molecule intact, a method for the synthesis of novel sclareol analogues was designed using palladium(II)-catalyzed oxidative Heck coupling reaction in order to study their structure-activity relationship. Both sclareol and its derivatives showed an interesting cytotoxicity profile, with 15-(4-fluorophenyl)sclareol (SS-12) as the most potent analogue, having IC50 = 0.082 μM against PC-3 cells. It was found that SS-12 commonly interacts with Bcl-2 and Beclin 1 BH3 domain proteins and enhances autophagic flux by modulating autophagy-related proteins. Moreover, inhibition of autophagy by autophagy inhibitors protected against SS-12-induced apoptosis. Finally, SS-12 effectively suppressed tumor growth in vivo in Ehrlich's ascitic and solid Sarcoma-180 mouse models. Topics: Animals; Apoptosis; Apoptosis Regulatory Proteins; Autophagy; Beclin-1; Cell Line, Tumor; Diterpenes; Drug Design; Female; Halogenation; Humans; Membrane Proteins; Mice; Proto-Oncogene Proteins c-bcl-2; Salvia; Sarcoma 180; Signal Transduction; TOR Serine-Threonine Kinases	2015

Article

Year

Design and Synthesis of Antitumor Heck-Coupled Sclareol Analogues: Modulation of BH3 Family Members by SS-12 in Autophagy and Apoptotic Cell Death.

Journal of medicinal chemistry, 2015, Apr-23, Volume: 58, Issue:8

Sclareol, a promising anticancer labdane diterpene, was isolated from Salvia sclarea. Keeping the basic stereochemistry-rich framework of the molecule intact, a method for the synthesis of novel sclareol analogues was designed using palladium(II)-catalyzed oxidative Heck coupling reaction in order to study their structure-activity relationship. Both sclareol and its derivatives showed an interesting cytotoxicity profile, with 15-(4-fluorophenyl)sclareol (SS-12) as the most potent analogue, having IC50 = 0.082 μM against PC-3 cells. It was found that SS-12 commonly interacts with Bcl-2 and Beclin 1 BH3 domain proteins and enhances autophagic flux by modulating autophagy-related proteins. Moreover, inhibition of autophagy by autophagy inhibitors protected against SS-12-induced apoptosis. Finally, SS-12 effectively suppressed tumor growth in vivo in Ehrlich's ascitic and solid Sarcoma-180 mouse models.

Topics: Animals; Apoptosis; Apoptosis Regulatory Proteins; Autophagy; Beclin-1; Cell Line, Tumor; Diterpenes; Drug Design; Female; Halogenation; Humans; Membrane Proteins; Mice; Proto-Oncogene Proteins c-bcl-2; Salvia; Sarcoma 180; Signal Transduction; TOR Serine-Threonine Kinases

2015