Preferred Label : Brostallicin;
NCIt synonyms : 4-(2-Bromoacrylamido)-N'''-(2-guanidinoethyl)-1,1',1',1'''-tetramethyl-N,4':N',4':N',4'''-quater(pyrrole-2-carboxamide);
NCIt definition : 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.;
UNII : RPC6R41K4I;
InChIKey : RXOVOXFAAGIKDQ-UHFFFAOYSA-N;
CAS number : 203258-60-0;
Molecule name : PNU-166196;
Chemical formula : C30H35BrN12O5;
Origin ID : C1889;
UMLS CUI : C1122890;
Currated CISMeF NLP mapping
- Semantic type(s)
- UMLS correspondences (same concept)
- concept_is_in_subset
