Role of the C8 gem-dimethyl group of bryostatin 1 on its unique pattern of biological activity.

Keck, Gary E; Poudel, Yam B; Rudra, Arnab; Stephens, Jeffrey C; Kedei, Noemi; Lewin, Nancy E; Blumberg, Peter M

Keck, Gary E; Poudel, Yam B; Rudra, Arnab; Stephens, Jeffrey C; Kedei, Noemi; Lewin, Nancy E; Blumberg, Peter M.

Affiliation

Keck GE; University of Utah, Department of Chemistry, 315 South 1400 East, RM 2020, Salt Lake City, UT 84112, USA. keck@chem.utah.edu

Bioorg Med Chem Lett ; 22(12): 4084-8, 2012 Jun 15.

Article in En | MEDLINE | ID: mdl-22579485

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.

Subject(s)

Antineoplastic Agents/chemical synthesis; Bryostatins/chemical synthesis; Protein Kinase C/antagonists & inhibitors; Antineoplastic Agents/pharmacology; Bryostatins/pharmacology; Cell Adhesion/drug effects; Cell Line, Tumor; Cell Proliferation/drug effects; Down-Regulation; Humans; Isoenzymes/antagonists & inhibitors; Isoenzymes/metabolism; Molecular Structure; Protein Kinase C/metabolism; Structure-Activity Relationship; Tetradecanoylphorbol Acetate/pharmacology

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Full text: 1 Collection: 01-internacional Database: MEDLINE Main subject: Protein Kinase C / Bryostatins / Antineoplastic Agents Limits: Humans Language: En Journal: Bioorg Med Chem Lett Journal subject: BIOQUIMICA / QUIMICA Year: 2012 Document type: Article Affiliation country: United States Country of publication: United kingdom

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