Gene/Protein
Disease
Symptom
Drug
Enzyme
Compound
Pivot Concepts:
Gene/Protein
Disease
Symptom
Drug
Enzyme
Compound
Target Concepts:
Gene/Protein
Disease
Symptom
Drug
Enzyme
Compound
Query: UMLS:C0684249 (
lung carcinoma
)
23,830
document(s) hit in 31,850,051 MEDLINE articles (0.00 seconds)
Tetrahydrolipstatin
(
THL
), its enantiomer, and an additional six diastereomers were evaluated as inhibitors of the hydrolysis of
p
-nitrophenyl butyrate by porcine pancreatic lipase. IC
50
s were found for all eight stereoisomers ranging from a low of 4.0 nM for
THL
to a high of 930 nM for the diastereomer with the inverted stereocenters at the 2,3,2'-positions. While the enantiomer of
THL
was also significantly less active (77 nM) the remaining five stereoisomers retained significant inhibitory activities (IC
50
s = 8.0 to 20 nM). All eight compounds were also evaluated against three human cancer cell lines (human breast cancers MCF-7 and MDA-MB-231, human large-cell
lung carcinoma
H460). No appreciable cytotoxicity was observed for
THL
and its seven diastereomers, as their IC
50
s in a MTT cytotoxicity assay were all greater than 3 orders of magnitude of camptothecin.
...
PMID:Stereochemical Structure Activity Relationship Studies (S-SAR) of Tetrahydrolipstatin. 2954 73
