Total Synthesis of the Endocannabinoid Uptake Inhibitor Guineensine and SAR Studies

ChemMedChem ◽  
2019 ◽  
Vol 14 (17) ◽  
pp. 1590-1596 ◽  
Author(s):  
Ruben Bartholomäus ◽  
Simon Nicolussi ◽  
Alice Baumann ◽  
Mark Rau ◽  
Ana Catarina Simão ◽  
...  
Keyword(s):  
Total Synthesis ◽  
Uptake Inhibitor ◽  
Sar Studies

scholarly journals Front Cover: Total Synthesis of the Endocannabinoid Uptake Inhibitor Guineensine and SAR Studies (ChemMedChem 17/2019)

ChemMedChem ◽  
2019 ◽  
Vol 14 (17) ◽  
pp. 1573-1573
Author(s):  
Ruben Bartholomäus ◽  
Simon Nicolussi ◽  
Alice Baumann ◽  
Mark Rau ◽  
Ana Catarina Simão ◽  
...  
Keyword(s):  
Total Synthesis ◽  
Front Cover ◽  
Uptake Inhibitor ◽  
Sar Studies

scholarly journals Mallotojaponins B and C: Total Synthesis, Antiparasitic Evaluation, and Preliminary SAR Studies

2016 ◽  
Vol 18 (4) ◽  
pp. 708-711 ◽  
Author(s):  
Tatyana D. Grayfer ◽  
Philippe Grellier ◽  
Elisabeth Mouray ◽  
Robert H. Dodd ◽  
Joëlle Dubois ◽  
...  
Keyword(s):  
Total Synthesis ◽  
Sar Studies

scholarly journals Total synthesis and biological evaluation of simplified aplyronine analogues as synthetically tractable anticancer agents

2020 ◽  
Vol 56 (10) ◽  
pp. 1529-1532
Author(s):  
Talia R. Pettigrew ◽  
Rachel J. Porter ◽  
Stephen J. Walsh ◽  
Michael P. Housden ◽  
Nelson Y. S. Lam ◽  
...  
Keyword(s):  
Total Synthesis ◽  
Anticancer Agents ◽  
Biological Evaluation ◽  
Sar Studies ◽  
Synthesis And Biological Evaluation

Analysis of bound structures and SAR studies led to the function-oriented simplification of the aplyronines; a convergent and modular synthetic platform then enabled the total synthesis and biological evaluation of four novel analogues.

scholarly journals Total synthesis of griseusins and elucidation of the griseusin mechanism of action

2019 ◽  
Vol 10 (32) ◽  
pp. 7641-7648 ◽  
Author(s):  
Yinan Zhang ◽  
Qing Ye ◽  
Larissa V. Ponomareva ◽  
Yanan Cao ◽  
Yang Liu ◽  
...  
Keyword(s):  
Total Synthesis ◽  
Mechanism Of Action ◽  
Tail Regeneration ◽  
Sar Studies

An efficient divergent synthesis of griseusins enabled SAR studies, mechanistic elucidation and evaluation in an axolotl tail regeneration model.

scholarly journals SAR Studies of the Leupyrrins: Design and Total Synthesis of Highly Potent Simplified Leupylogs

2020 ◽  
Vol 26 (66) ◽  
pp. 15051-15051
Author(s):  
Paul R. Wosniok ◽  
Christopher Knopf ◽  
Sandra Dreisigacker ◽  
J. Manuel Orozco‐Rodriguez ◽  
Bettina Hinkelmann ◽  
...  
Keyword(s):  
Total Synthesis ◽  
Sar Studies

Total synthesis of novel dictyostatin analogs and hybrids as microtubule-stabilizing anticancer agents

2009 ◽  
Vol 81 (2) ◽  
pp. 169-180 ◽  
Author(s):  
Ian Paterson ◽  
Nicola M. Gardner ◽  
Guy J. Naylor
Keyword(s):  
Total Synthesis ◽  
Anticancer Agents ◽  
Human Cancer ◽  
Human Cancer Cell Lines ◽  
Synthetic Strategy ◽  
Sar Studies ◽  
Growth Inhibitory ◽  
Growth Inhibitory Activity ◽  
Microtubule Stabilizing Agent

Structural modification of the dictyostatin macrolide template through adaptation of our total synthesis has led to the identification of a number of potent analogs of this novel microtubule-stabilizing agent. A common synthetic strategy was exploited, employing a (Z)-selective Still-Gennari olefination between various advanced C11-C26 aldehyde and C4-C10 (or C1-C10) β-ketophosphonate intermediates. In vitro evaluation of the growth inhibitory activity of these analogs against both Taxol-sensitive and -resistant human cancer cell lines has provided a foundation for structure-activity relationship (SAR) studies to help define the pharmacophore region.

scholarly journals SAR Studies of the Leupyrrins: Design and Total Synthesis of Highly Potent Simplified Leupylogs

2020 ◽  
Vol 26 (66) ◽  
pp. 15074-15078
Author(s):  
Paul R. Wosniok ◽  
Christopher Knopf ◽  
Sandra Dreisigacker ◽  
J. Manuel Orozco‐Rodriguez ◽  
Bettina Hinkelmann ◽  
...  
Keyword(s):  
Total Synthesis ◽  
Sar Studies

scholarly journals Front Cover: SAR Studies of the Leupyrrins: Design and Total Synthesis of Highly Potent Simplified Leupylogs (Chem. Eur. J. 66/2020)

2020 ◽  
Vol 26 (66) ◽  
pp. 15047-15047
Author(s):  
Paul R. Wosniok ◽  
Christopher Knopf ◽  
Sandra Dreisigacker ◽  
J. Manuel Orozco‐Rodriguez ◽  
Bettina Hinkelmann ◽  
...  
Keyword(s):  
Total Synthesis ◽  
Front Cover ◽  
Sar Studies

The Structural Chemistry, Reactivity, and Total Synthesis of Dolabellane Diterpenes

Tetrahedron ◽  
1998 ◽  
Vol 54 (31) ◽  
pp. 11683-11729 ◽  
Author(s):  
A Rodríguez
Keyword(s):  
Total Synthesis ◽  
Structural Chemistry
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