title: Role of the C8 gem-dimethyl group of bryostatin 1 on its unique pattern of biological activity.
abstract: The role of the C(8) gem-dimethyl group in the A-ring of bryostatin 1 has been examined through chemical synthesis and biological evaluation of a new analogue. Assays for biological function using U937, K562, and MV4-11 cells as well as the profiles for downregulation of PKC isozymes revealed that the presence of this group is not a critical determinant for the unique pattern of biological activity of bryostatin.
authors.affiliation: University of Utah, Department of Chemistry, 315 South 1400 East, RM 2020, Salt Lake City, UT 84112, USA. keck@chem.utah.edu
authors.forename: Gary E
authors.initials: GE
authors.lastname: Keck
authors.forename: Yam B
authors.initials: YB
authors.lastname: Poudel
authors.forename: Arnab
authors.initials: A
authors.lastname: Rudra
authors.forename: Jeffrey C
authors.initials: JC
authors.lastname: Stephens
authors.forename: Noemi
authors.initials: N
authors.lastname: Kedei
authors.forename: Nancy E
authors.initials: NE
authors.lastname: Lewin
authors.forename: Peter M
authors.initials: PM
authors.lastname: Blumberg
mesh_terms: D000970:Antineoplastic Agents / Q000138:chemical synthesis* / Q000494:pharmacology; D054713:Bryostatins / Q000138:chemical synthesis* / Q000494:pharmacology; D002448:Cell Adhesion / Q000187:drug effects; D045744:Cell Line, Tumor; D049109:Cell Proliferation / Q000187:drug effects; D015536:Down-Regulation; D006801:Humans; D007527:Isoenzymes / Q000037:antagonists & inhibitors / Q000378:metabolism; D015394:Molecular Structure; D011493:Protein Kinase C / Q000037:antagonists & inhibitors* / Q000378:metabolism; D013329:Structure-Activity Relationship; D013755:Tetradecanoylphorbol Acetate / Q000494:pharmacology
chemical_list: D000970:Antineoplastic Agents; D054713:Bryostatins; D007527:Isoenzymes; C046785:bryostatin 1; D011493:Protein Kinase C; D013755:Tetradecanoylphorbol Acetate