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Archive for the ‘SAR studies’ Category

SAR with juvenile hormone analogs

Posted by naturalproductman on November 12, 2011

Tetsuro Shinada and co-workers at Osaka City University have reported in Tetrahedron on some juvenile hormone analogs.

juvenile hormone

Tetrahedron paper

Posted in Methodology, Pesticides, SAR studies | Leave a Comment »

QSAR studies for androgen receptor

Posted by naturalproductman on July 11, 2011

Jose Manuel Garcia de la Vega (Universidad Autonoma de Madrid) and co-workers have reported in the Journal of Steroid Biochemistry and Molecular Biology on some QSAR studiesfor androgen analogs acting on androgen receptors.  If you were ever curious about how drug design works, this paper may illustrate a good example of the computational chemist’s approach.

QSAR

 

JSBMB paper

Posted in Computational, Proteins, Receptors, SAR studies, Strigolactones | Leave a Comment »

Tadalafil Analogs

Posted by naturalproductman on May 5, 2011

Benoit Deprez and co-workers at Universite Lille Nord de France have reported in the Journal of Medicinal Chemistry on the synthesis and activity relationships of tadalafil.

tadalafil

JMC paper

Posted in Named Reactions, Pictet-Spengler, SAR studies | Leave a Comment »

Hoiamides

Posted by naturalproductman on August 6, 2010

William Gerwick and co-workers have published on their studies of hoiamides, which may be a target for voltage gate sodium channels (VGSC).  This channel is a target for the treatment of neurodegenerative disorders – there are neurotoxin sites (at least seven) on VGSCs that are targeted by drugs.

hoiamides


JNP paper

Posted in Macrocycles, Neurodegenerative, Polyketides, Polythio Compounds, SAR studies | Leave a Comment »

Syntheses of Largazole and Analogs

Posted by naturalproductman on June 3, 2010

Angel de Lera and co-workers at Universidade de Vigo (Spain) have published in the Journal of Medicinal Chemistry on the syntheses of largazole and its analogs.  They further tested their HDAC inhibition.

largazole
JMC paper

Posted in Macrocycles, Macrolides, Methodology, Named Reactions, SAR studies | 1 Comment »

Apoptolidin G

Posted by naturalproductman on June 1, 2010

Bachmann, Sulikowski and co-workers at Vanderbilt have published in Organic Letters on the characterization of apoptolidin G.  Apoptolidin A had an EC50 of 50 nM against H292 cells while apoptolidin G had an EC50 of 150 nM.  The difference in the structures is the C2-C3 double bond geometry, which they have obtained via UV light irradiation of apoptolidin A.

apoptolidin

OL paper

Posted in Glycosides, Light Mediated, Macrolides, Methodology, SAR studies | Leave a Comment »

Grecocycline B

Posted by naturalproductman on March 20, 2010

Thomas Paululat and co-workers at the University of Siegen in Germany have recently reported on the isolation of grecocycline B from Streptomyces sp. Acta 1362.  The new polycyclic compound had an IC50 of 0.52 micromolar against tyrosine phosphatase B1.  Interestingly, protein tyrosine phosphatase PTP1B is a target for the treatment of obesity, type 2 diabetes and cancer.
grecocycline B

European JOC paper

Posted in Angucyclines, Aromatic, Diabetes Type 2, Diseases, Obesity, Polycyclic, SAR studies | Leave a Comment »

HDACi Cis-Platin Hybrid

Posted by naturalproductman on November 3, 2009

Celine Marmion and co-workers at the Royal College of Surgeons in Ireland have recently published in Chemical Communications on the synthesis and activity relationship study of a cis-platin/suberoylanilide hydroxamic acid chimera.

hybrid

 

Chem Comm paper

Posted in Chemical Biology, Methodology, SAR studies, Transition Metal | Leave a Comment »

Combretastatin Analogs

Posted by naturalproductman on November 2, 2009

Sylvie Duckie and co-workers at UMIST in Manchester have recently published in Bioorganic and Medicinal Chemistry on biological and synthetic studies of chalcone analogs.  The most amazing properties had to do with the IC50s of the K562 human chronic myelogenous leukemia cell line.  Some of the substrates that were made possessed sub-nanomolar IC50s.  If you look at the substrates carefully, then you should know well enough that these are dienones that are excellent Nazarov cyclization precursors.  These substrates were based off of a natural product, combretastatin A4, that had anti-tubulin polymerization activity by binding to the colchicine binding site belonging to the beta-tubulin subunit.

combretastatin

 

Bioorganic and Medicinal Chemistry Link

Posted in Aromatic, SAR studies | Leave a Comment »

 
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