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AttributesValues
rdf:type
rdfs:label
  • Brostallicin
rdfs:subClassOf
Concept_In_Subset
Semantic_Type
  • Organic Chemical
  • Pharmacologic Substance
Preferred_Name
  • Brostallicin
UMLS_CUI
  • C1122890
CAS_Registry
  • 203258-60-0
In_Clinical_Trial_For
  • Multiple myeloma; soft-tissue sarcoma
FDA_UNII_Code
  • RPC6R41K4I
Contributing_Source
  • FDA
ALT_DEFINITION
  • 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.NCI-GLOSS
PDQ_Open_Trial_Search_ID
  • 590644
PDQ_Closed_Trial_Search_ID
  • 590644
Chemical_Formula
  • C30H35BrN12O5
Legacy_Concept_Name
  • Brostallicin
FULL_SYN
  • BROSTALLICINPTFDARPC6R41K4I
  • 4-(2-Bromoacrylamido)-N'''-(2-guanidinoethyl)-1,1',1',1'''-tetramethyl-N,4':N',4':N',4'''-quater(pyrrole-2-carboxamide)SNNCI
  • BrostallicinPTNCI
  • brostallicin hydrochloridePTNCI-GLOSSCDR0000269413
  • PNU-166196CNNCI
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.NCI
code
  • C1889
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