Preferred Label : Brostacillin Hydrochloride;
NCIt synonyms : 4-(2-Bromoacrylamido)-N'''-(2-guanidinoethyl)-1,1',1',1'''-tetramethyl-N,4':N',4':N',4'''-quater(pyrrole-2-carboxamide)
Hydrochloride;
NCIt related terms : brostallicin hydrochloride;
NCIt definition : The hydrochloride salt form of brostacillin, a synthetic, alpha-bromoacrylic, second-generation
minor groove binder (MGB), related to distamycin A, with potential antineoplastic
activity. Brostallicin binds to DNA minor groove DNA, after having formed a highly
reactive glutathione (GSH)-brostallicin complex in the presence of the enzyme glutathione
S-transferase (GST), which is overexpressed in cancer cells; DNA replication and cell
division are inhibited, resulting in tumor cell death. Compared to typical MGBs, this
agent appears to bind covalently to DNA in a different manner and its activity does
not depend on a functional DNA mismatch repair (MMR) mechanism. Accordingly, brostallicin
may be effective against MMR-defective tumors that are refractory to various anticancer
agents.;
Alternative definition : NCI-GLOSS: A substance being studied in the treatment of cancer. Brostallicin hydrochloride
binds to DNA and may kill cancer cells. It may also help other drugs kill cancer cells.
It is a type of DNA minor groove binding agent.;
UNII : 1DKC476797;
InChIKey : IPKHXIAPPAKHTB-UHFFFAOYSA-N;
CAS number : 203258-38-2;
Molecule name : PNU-166196 Hydrochloride;
NCI Metathesaurus CUI : CL509004;
Codes from synonyms : CDR0000269413;
Origin ID : C128040;
UMLS CUI : C2987714;
Semantic type(s)
- concept_is_in_subset
