About: Silatecan AR-67     Goto   Sponge   NotDistinct   Permalink

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AttributesValues
rdf:type
rdfs:label
  • Silatecan AR-67
rdfs:subClassOf
Has_Target
Semantic_Type
  • Organic Chemical
  • Pharmacologic Substance
Preferred_Name
  • Silatecan AR-67
UMLS_CUI
  • C1955483
PDQ_Open_Trial_Search_ID
  • 522726
PDQ_Closed_Trial_Search_ID
  • 522726
Legacy_Concept_Name
  • _7-Tert-butyldimethylsilyl-10-hydroxycamptothecin
FULL_SYN
  • 7-t-butyldimethylsilyl-10-hydroxycamptothecinSNNCI
  • Silatecan AR-67PTNCI
  • DB-67CNNCI
  • AR-67CNNCI
  • 7-Tert-butyldimethylsilyl-10-hydroxycamptothecinSNNCI
DEFINITION
  • A synthetic, highly lipophilic derivative of camptothecin, with potential antineoplastic and radiosensitizing activities. 7-tert-butyldimethylsilyl-10-hydroxycamptothecin binds to and stabilizes the topoisomerase I-DNA covalent complex. This inhibits the religation of topoisomerase I-mediated single-stranded DNA breaks and produces lethal double-stranded DNA breaks when encountered by the DNA replication machinery, thereby inhibiting DNA replication and inducing apoptosis. Camptothecin readily undergoes hydrolysis at physiological pH, changing its conformation from the active lactone structure to an inactive carboxylate form. Modifications on the E ring of camptothecin prevent binding of human serum albumin, which prefers the inactive carboxylate form, thereby enhancing the stability of the active lactone structure and resulting in prolonged agent activity. In addition, this agent sensitizes tumor cells toward radiation treatment.NCI
code
  • C64618
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