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: EC:2.3.1.21 (
CPT
)
4,580
document(s) hit in 31,850,051 MEDLINE articles (0.00 seconds)
A series of 10-position substituted nitrogenous heterocyclic aromatic group derivatives of SN-38 were prepared. Most of these compounds possessed lower cytotoxicities than
CPT
. Compound 13 revealed potent cytotoxicity similar to
CPT
, and compounds 17, 18, and 19 showed similar cytotoxic activity to topotecan. All of the pyridine salt derivatives (7-16) revealed comparable or superior topo I inhibitory activity in relation to
CPT
. Ethyl in the 7-position of these compounds can increase the cytotoxicity and inhibitory activity to topo I compared with corresponding pyridine salts
CPT
derivatives (7a-13a) and simultaneously maintain good water solubility. This result is consistent with the
SAR
of
CPT
.
...
PMID:Cytotoxicity and topo I targeting activity of substituted 10--nitrogenous heterocyclic aromatic group derivatives of SN-38. 2039 45
