Screening of the Sigma-Aldrich Library of Pharmacologically Active Compounds (LOPAC) against cultured Trypanosoma brucei, the causative agent of African sleeping sickness, resulted in the identification of a number of compounds with selective antiproliferative activity over mammalian cells. These included (+)-(1R,2R)-U50488, a weak opioid agonist with an EC50 value of 59 nm as determined in our T. brucei in vitro assay reported previously. This paper describes the modification of key structural elements of U50488 to investigate structure-activity relationships (SAR) and to optimise the antiproliferative activity and pharmacokinetic properties of this compound.</p
From a whole-organism high throughput screen of approximately 87000 compounds against Trypanosoma br...
A previous publication from our laboratory reported the identification of a new class of 2-(1H-imida...
Human African trypanosomiasis (sleeping sickness) is a devastating disease which is endemic in parts...
Screening of the Sigma-Aldrich Library of Pharmacologically Active Compounds (LOPAC) against culture...
AbstractA resazurin-based cell viability assay was developed for phenotypic screening of the LOPAC 1...
A resazurin-based cell viability assay was developed for phenotypic screening of the LOPAC 1280 'lib...
Human African Trypanosomiasis (HAT) is a disease caused by the parasite Trypanosoma brucei and is cl...
This thesis describes the synthesis and structure activity relationship (SAR) of oxazolopyridine an...
The development of drugs for neglected infectious diseases often uses parasite-specific enzymes as t...
ABSTRACT: Compound NVP-BEZ235 (1) is a potent inhibitor of human phospoinositide-3-kinases and mamma...
Insect-borne parasite Trypanosoma brucei plagues humans and other animals, eliciting the disease Hum...
Human African trypanosomiasis (HAT), more commonly known as African sleeping sickness is caused by t...
Human African Trypanosomiasis (HAT) is caused by two trypanosome sub-species, Trypanosoma brucei rho...
The compound NVP-BEZ235 (1) is a potent inhibitor of human phospoinositide-3-kinases (PI3Ks) and mam...
The drugs in clinical use against African sleeping sickness are toxic, costly, or inefficient. We sh...
From a whole-organism high throughput screen of approximately 87000 compounds against Trypanosoma br...
A previous publication from our laboratory reported the identification of a new class of 2-(1H-imida...
Human African trypanosomiasis (sleeping sickness) is a devastating disease which is endemic in parts...
Screening of the Sigma-Aldrich Library of Pharmacologically Active Compounds (LOPAC) against culture...
AbstractA resazurin-based cell viability assay was developed for phenotypic screening of the LOPAC 1...
A resazurin-based cell viability assay was developed for phenotypic screening of the LOPAC 1280 'lib...
Human African Trypanosomiasis (HAT) is a disease caused by the parasite Trypanosoma brucei and is cl...
This thesis describes the synthesis and structure activity relationship (SAR) of oxazolopyridine an...
The development of drugs for neglected infectious diseases often uses parasite-specific enzymes as t...
ABSTRACT: Compound NVP-BEZ235 (1) is a potent inhibitor of human phospoinositide-3-kinases and mamma...
Insect-borne parasite Trypanosoma brucei plagues humans and other animals, eliciting the disease Hum...
Human African trypanosomiasis (HAT), more commonly known as African sleeping sickness is caused by t...
Human African Trypanosomiasis (HAT) is caused by two trypanosome sub-species, Trypanosoma brucei rho...
The compound NVP-BEZ235 (1) is a potent inhibitor of human phospoinositide-3-kinases (PI3Ks) and mam...
The drugs in clinical use against African sleeping sickness are toxic, costly, or inefficient. We sh...
From a whole-organism high throughput screen of approximately 87000 compounds against Trypanosoma br...
A previous publication from our laboratory reported the identification of a new class of 2-(1H-imida...
Human African trypanosomiasis (sleeping sickness) is a devastating disease which is endemic in parts...