Document Detail

Substitution on the A-ring confers to bryopyran analogues the unique biological activity characteristic of bryostatins and distinct from that of the phorbol esters.
MedLine Citation:
PMID:  19113896     Owner:  NLM     Status:  MEDLINE    
A close structural analogue of bryostatin 1, which differs from bryostatin 1 only by the absence of the C(30) carbomethoxy group (on the C(13) enoate of the B-ring), has been prepared by total synthesis. Biological assays reveal a crucial role for substitution in the bryostatin 1 A-ring in conferring those responses which are characteristic of bryostatin 1 and distinct from those observed with PMA.
Gary E Keck; Yam B Poudel; Dennie S Welch; Matthew B Kraft; Anh P Truong; Jeffrey C Stephens; Noemi Kedei; Nancy E Lewin; Peter M Blumberg
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Publication Detail:
Type:  Journal Article; Research Support, N.I.H., Extramural; Research Support, N.I.H., Intramural    
Journal Detail:
Title:  Organic letters     Volume:  11     ISSN:  1523-7052     ISO Abbreviation:  Org. Lett.     Publication Date:  2009 Feb 
Date Detail:
Created Date:  2009-01-29     Completed Date:  2009-02-26     Revised Date:  2014-09-16    
Medline Journal Info:
Nlm Unique ID:  100890393     Medline TA:  Org Lett     Country:  United States    
Other Details:
Languages:  eng     Pagination:  593-6     Citation Subset:  IM    
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MeSH Terms
Antineoplastic Agents / chemical synthesis*,  chemistry*,  pharmacology
Bryostatins / chemical synthesis,  chemistry*,  pharmacology
Dose-Response Relationship, Drug
Drug Screening Assays, Antitumor
Molecular Structure
Phorbol Esters / chemistry*,  pharmacology
Structure-Activity Relationship
Grant Support
GM28961/GM/NIGMS NIH HHS; R01 GM028961/GM/NIGMS NIH HHS; R01 GM028961-18/GM/NIGMS NIH HHS; R01 GM028961-19/GM/NIGMS NIH HHS; R01 GM028961-20/GM/NIGMS NIH HHS; R01 GM028961-21/GM/NIGMS NIH HHS; R01 GM028961-22/GM/NIGMS NIH HHS; R01 GM028961-23/GM/NIGMS NIH HHS; R01 GM028961-24/GM/NIGMS NIH HHS; R01 GM028961-25A1/GM/NIGMS NIH HHS; R01 GM028961-26/GM/NIGMS NIH HHS
Reg. No./Substance:
0/Antineoplastic Agents; 0/Bryostatins; 0/Phorbol Esters; 37O2X55Y9E/bryostatin 1

From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine

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