Naturalproductman’s Blog

Hey, is that a natural product?!

Archive for the ‘Diseases’ Category

(±)-Erythro-7′-methylcarolignan E

Posted by naturalproductman on February 2, 2016

Qiong Gu and co-workers from Sun Yat-sen University and UNC have reported in the Journal of Natural Products on the isolation of (±)-erythro-7′-methylcarolignan E with anti-HIV activity.

 

JNP paper

Posted in Diseases, HIV, Lignans | Leave a Comment »

Erinacine S

Posted by naturalproductman on February 2, 2016

Chien-Chang Shen and co-workers from Hung Kuang University and National Yang-Ming University in Taiwan have reported in the Journal of Natural Products on the isolation of erinacine S, which had increased the expression of an insulin-degrading enzyme in the cerebral cortex.

JNP paper

Posted in Diabetes Type 1, Diabetes Type 2, Diseases, Sesterterpenes | Leave a Comment »

(−)-Jiadifenin synthesis

Posted by naturalproductman on January 26, 2016

Glenn Micalizio and colleague at Dartmouth College have reported in JACS on the synthesis of jiadifenin.

 

JACS paper

Posted in Neurodegenerative, Sesquiterpenes, Total Synthesis | Leave a Comment »

Cipacinoids

Posted by naturalproductman on January 19, 2016

Jian-Min Yue and co-workers from the Chinese Academy of Sciences have reported in Organic Letters on the isolation of cipacinoids A-D, which had protein tyrosine phosphatase 1B inhibition (17 micromolar).

 

OL paper

Posted in Diabetes Type 2, Spirocycles, Spirocyclic centers | Leave a Comment »

Enhancing water solubility of a drug (triptolide)

Posted by naturalproductman on November 25, 2015

Gunda Georg and co-workers at the University of Minnesota reported in the Journal of Medicinal Chemistry on the addition of a phosphonooxymethyl group onto triptolide to increase its water solubility by greater than 3,580 times. (slight mistake: Scheme 2 in the paper has the use of benzoyl peroxide shown as “Bn2O2” when it should be “Bz2O2” – Bn2O2 would be benzyl peroxide). Another interesting point from this paper is that this natural product has multiple modes of action where it can covalently attach to proteins (XPB, xeroderma pigmentosum B) or non-covalently (DCTPP1, dCTP pyrophosphatase). Other modified attempts to form soluble prodrugs of this natural product (e.g. carboxylic acid, amino acid esters) resulted in difficult removal of the prodrug group.

11.25.2015 Naturalproductman

J. Med. Chem. paper

Posted in Alzheimer's, Cancer, Diterpene, Epoxides, Medicinal Chemistry, Prodrug | 1 Comment »

Unciaphenol – Bergman cyclization product of uncialamycin

Posted by naturalproductman on October 16, 2015

Raymond Anderson and co-workers at the University of British Columbia report in Organic Letters on unciaphenol, which has anti-HIV activity.

unciaphenol

OL paper

Posted in Alkynes, Cascade Reactions, Diseases, HIV, Named Reactions, Polyketides | Leave a Comment »

Another validation for natural product research

Posted by naturalproductman on October 5, 2015

The nobel prize in medicine announcement was made and the trio of winners (Satoshi Omura (avermectin), William Campbell (ivermectin), and Youyou Tu) had done natural product isolation work – one was Youyou Tu, the Chinese woman who discovered artemisinin (half of the prize)! An exciting win for natural product research!

Posted in Diseases, Malaria, Random, Unnatural Products | Leave a Comment »

Alpha-bisabolol

Posted by naturalproductman on July 15, 2015

Victoriano Corpas-Lopez and co-workers at Universidad de Granada have reported in Journal of Natural Products on the use of alpha-bisabolol as a treatment for visceral leishmaniasis.

JNP paper

Posted in Diseases | Leave a Comment »

HIV integrase inhibitor synthesis

Posted by naturalproductman on May 12, 2015

Chris Senanayake and co-workers from Boehringer-Ingelheim have reported in ACIE on the synthesis of

HIV

ACIE paper

Posted in Diseases, HIV, Total Synthesis | Leave a Comment »

MAP4K4 for neurodegenerative diseases

Posted by naturalproductman on April 26, 2015

Herbert Waldmann and co-workers at Technische Universität Dortmund have reported in ACIE on MAP4K4 as a target for neurodegenerative diseases.

MAP

ACIE paper

Posted in Diseases, Medicinal Chemistry, Neurodegenerative, Protein Targets, Proteins | Leave a Comment »

 
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