Biological activity of the bryostatin analog Merle 23 on mouse epidermal cells and mouse skin

JS Kelsey, C Cataisson, J Chen… - Molecular …, 2016 - Wiley Online Library
Bryostatin 1, a complex macrocyclic lactone, is the subject of multiple clinical trials for cancer
chemotherapy. Although bryostatin 1 biochemically functions like the classic mouse skin …

Charge density influences C1 domain ligand affinity and membrane interactions

JS Kelsey, T Geczy, NE Lewin, N Kedei, CS Hill… - …, 2014 - Wiley Online Library
The C1 domain, which represents the recognition motif on protein kinase C for the lipophilic
second messenger diacylglycerol and its ultrapotent analogues, the phorbol esters, has …

Syntheses of C17–C27 fragments of 20-deoxybryostatins for assembly using Julia and metathesis reactions

M Ball, T Gregson, H Omori, EJ Thomas - Organic & Biomolecular …, 2017 - pubs.rsc.org
Two approaches to the synthesis of compounds corresponding to the C17–C27 fragment of
the 20-deoxybryostatins are described. The first approach is based on the palladium (0) …

Total synthesis of 7-des-O-pivaloyl-7-O-benzylbryostatin 10

AP Green, S Hardy, ATL Lee, EJ Thomas - Organic & Biomolecular …, 2017 - pubs.rsc.org
The first total synthesis of a derivative of a 20-deoxybryostatin, namely 7-des-O-pivaloyl-7-O-
benzylbryostatin 10 is described. Preliminary studies demonstrated that the modified Julia …

Deletion of the C26 methyl substituent from the Bryostatin analogue Merle 23 has negligible impact on its biological profile and potency

X Zhao, N Kedei, A Michalowski, NE Lewin… - …, 2018 - Wiley Online Library
Important strides are being made in understanding the effects of structural features of
bryostatin 1, a candidate therapeutic agent for cancer and dementia, in conferring its …

Marine organisms and their prospective use in therapy of human diseases

SS Ebada, P Proksch - Nature Helps... How Plants and Other Organisms …, 2011 - Springer
Marine ecosystems show remarkable chemical, biological, and ecological diversities which
have inspired marine natural product chemists for many years to identify novel chemical …

Synthesis of the C1–C16 fragment of bryostatin for incorporation into 20, 20-fluorinated analogues

PR Mears, EJ Thomas - Tetrahedron, 2021 - Elsevier
The stereoselective synthesis of a carboxylic acid ester corresponding to the C1–C16
fragment of bryostatin, with 4-methoxybenzyl (PMB) protection for the 7-hydroxyl group, is …

Synthesis of vinylic iodides for incorporation into the C17-C27 fragment of bryostatins

T Gregson, EJ Thomas - Tetrahedron, 2017 - Elsevier
Vinylic iodides were identified as useful intermediates for the synthesis of the C17-C27
fragment of the bryostatins with control of the geometry of the exocyclic …

Design and synthesis of protein kinase Cα activators based on 'out of pocket'interactions

G Hirai, M Ohkubo, Y Tamura, M Sodeoka - Bioorganic & medicinal …, 2011 - Elsevier
Novel types of PKCα activators based on isobenzofuranone bearing a myo-inositol moiety
were designed and synthesized. The derivatives with bulky substituents on the myo-inositol …

Synthetic approaches to the C11–C27 fragments of bryostatins

AP Green, S Hardy, EJ Thomas - Organic & Biomolecular Chemistry, 2017 - pubs.rsc.org
The modified Julia reaction and acyl carbanion chemistry, especially reactions of 2-lithiated
dithianes, have been investigated for the synthesis of intermediates that are the synthetic …