FRINK Linked Data Fragments server

Matches in SemOpenAlex for { <https://semopenalex.org/work/W2081184475> ?p ?o ?g. }

• W2081184475 endingPage "2623" @default.
• W2081184475 startingPage "2611" @default.
• W2081184475 abstract "The mechanism of action of many antitumor agents involves DNA damage, either by direct binding of the drug to DNA or to DNA-binding proteins. However, most of the DNA-interacting agents have only a limited degree of sequence specificity, which implies that they may hit all the cellular genes. DNA minor groove binders, among which the derivatives of distamycin A play an important role, could provide significant improvement in cancer management, increasing gene specificity, due to high selectivity of interaction with thymine-adenine (TA) rich sequences. We now report and discuss the synthesis, the in vitro and in vivo activities, and some mechanistic features of α-halogenoacrylamido derivatives of distamycin A. The final result of this work was the selection of brostallicin 17 (PNU-166196). Brostallicin, presently in phase II clinical trials, shows a broad spectrum of antitumor activity and an apoptotic effect higher than distamycin derivative tallimustine. An important in vitro toxicological feature of brostallicin is the very good ratio between myelotoxicity on human haematopoietic progenitor cells and cytotoxicity on tumor cells, in comparison with clinically tested DNA minor groove binders. A peculiarity of brostallicin is its in vitro reactivity in the DNA alkylation assays only in the presence of glutathione. Moreover brostallicin's antitumor activity, both in in vitro and in vivo tumor models, is higher in the presence of increased levels of glutathione/glutathione-S-tranferases. These findings contribute to the definition of brostallicin as a novel anticancer agent that differs from other minor groove binders and alkylating agents for both the profile of activity and the mechanism of action and to classify the α-bromoacrylamido derivatives of distamycin as a new class of cytotoxics. Moreover, due to its interaction with glutathione, brostallicin may have a role for the tailored treatment of tumors characterized by constitutive or therapy-induced overexpression of glutathione/glutathione-S-tranferase levels." @default.
• W2081184475 created "2016-06-24" @default.
• W2081184475 creator A5000499660 @default.
• W2081184475 creator A5022738573 @default.
• W2081184475 creator A5041567500 @default.
• W2081184475 creator A5058402482 @default.
• W2081184475 creator A5063804577 @default.
• W2081184475 creator A5067286039 @default.
• W2081184475 creator A5069986334 @default.
• W2081184475 creator A5075508318 @default.
• W2081184475 date "2004-04-06" @default.
• W2081184475 modified "2023-10-04" @default.
• W2081184475 title "Cytotoxic α-Halogenoacrylic Derivatives of Distamycin A and Congeners" @default.
• W2081184475 cites W1699367618 @default.
• W2081184475 cites W1974375149 @default.
• W2081184475 cites W1984785998 @default.
• W2081184475 cites W1990262711 @default.
• W2081184475 cites W1996163469 @default.
• W2081184475 cites W1999923210 @default.
• W2081184475 cites W2004748824 @default.
• W2081184475 cites W2014524176 @default.
• W2081184475 cites W2018996043 @default.
• W2081184475 cites W2028917872 @default.
• W2081184475 cites W2045489285 @default.
• W2081184475 cites W2052897849 @default.
• W2081184475 cites W2068075238 @default.
• W2081184475 cites W2079867467 @default.
• W2081184475 cites W2081237805 @default.
• W2081184475 cites W2092514160 @default.
• W2081184475 cites W2093628877 @default.
• W2081184475 cites W2093728648 @default.
• W2081184475 cites W2259395139 @default.
• W2081184475 cites W2949262277 @default.
• W2081184475 cites W2950390751 @default.
• W2081184475 cites W4245957869 @default.
• W2081184475 doi "https://doi.org/10.1021/jm031051k" @default.
• W2081184475 hasPubMedId "https://pubmed.ncbi.nlm.nih.gov/15115402" @default.
• W2081184475 hasPublicationYear "2004" @default.
• W2081184475 type Work @default.
• W2081184475 sameAs 2081184475 @default.
• W2081184475 citedByCount "38" @default.
• W2081184475 countsByYear W20811844752012 @default.
• W2081184475 countsByYear W20811844752013 @default.
• W2081184475 countsByYear W20811844752014 @default.
• W2081184475 countsByYear W20811844752015 @default.
• W2081184475 countsByYear W20811844752017 @default.
• W2081184475 countsByYear W20811844752019 @default.
• W2081184475 countsByYear W20811844752020 @default.
• W2081184475 countsByYear W20811844752021 @default.
• W2081184475 countsByYear W20811844752022 @default.
• W2081184475 countsByYear W20811844752023 @default.
• W2081184475 crossrefType "journal-article" @default.
• W2081184475 hasAuthorship W2081184475A5000499660 @default.
• W2081184475 hasAuthorship W2081184475A5022738573 @default.
• W2081184475 hasAuthorship W2081184475A5041567500 @default.
• W2081184475 hasAuthorship W2081184475A5058402482 @default.
• W2081184475 hasAuthorship W2081184475A5063804577 @default.
• W2081184475 hasAuthorship W2081184475A5067286039 @default.
• W2081184475 hasAuthorship W2081184475A5069986334 @default.
• W2081184475 hasAuthorship W2081184475A5075508318 @default.
• W2081184475 hasConcept C109316439 @default.
• W2081184475 hasConcept C143425029 @default.
• W2081184475 hasConcept C181199279 @default.
• W2081184475 hasConcept C185592680 @default.
• W2081184475 hasConcept C202751555 @default.
• W2081184475 hasConcept C207001950 @default.
• W2081184475 hasConcept C2776120743 @default.
• W2081184475 hasConcept C538909803 @default.
• W2081184475 hasConcept C54355233 @default.
• W2081184475 hasConcept C552990157 @default.
• W2081184475 hasConcept C55493867 @default.
• W2081184475 hasConcept C71240020 @default.
• W2081184475 hasConcept C86803240 @default.
• W2081184475 hasConceptScore W2081184475C109316439 @default.
• W2081184475 hasConceptScore W2081184475C143425029 @default.
• W2081184475 hasConceptScore W2081184475C181199279 @default.
• W2081184475 hasConceptScore W2081184475C185592680 @default.
• W2081184475 hasConceptScore W2081184475C202751555 @default.
• W2081184475 hasConceptScore W2081184475C207001950 @default.
• W2081184475 hasConceptScore W2081184475C2776120743 @default.
• W2081184475 hasConceptScore W2081184475C538909803 @default.
• W2081184475 hasConceptScore W2081184475C54355233 @default.
• W2081184475 hasConceptScore W2081184475C552990157 @default.
• W2081184475 hasConceptScore W2081184475C55493867 @default.
• W2081184475 hasConceptScore W2081184475C71240020 @default.
• W2081184475 hasConceptScore W2081184475C86803240 @default.
• W2081184475 hasIssue "10" @default.
• W2081184475 hasLocation W20811844751 @default.
• W2081184475 hasLocation W20811844752 @default.
• W2081184475 hasOpenAccess W2081184475 @default.
• W2081184475 hasPrimaryLocation W20811844751 @default.
• W2081184475 hasRelatedWork W1982027601 @default.
• W2081184475 hasRelatedWork W1998842974 @default.
• W2081184475 hasRelatedWork W200909032 @default.
• W2081184475 hasRelatedWork W2049529530 @default.
• W2081184475 hasRelatedWork W2071952937 @default.
• W2081184475 hasRelatedWork W2416964709 @default.
• W2081184475 hasRelatedWork W2464301138 @default.

• next