A new class of pyrrolo[l,4lbenzodiazepine (PBD) analogues featuring a pyrazolo[4,3-e]pyrrolo- [l72-al[l,4]diazepinone ring system has been designed and synthesized. These compounds, 2a-0, are characterized by the substitution of the aromatic A ring, characteristic of the PBDs, with a disubstituted pyrazole ring bearing alkyl and benzyl substituents at N6 or N7 and alkyl or carbomethoxy substituents at c8. Biological evaluation revealed an appreciable in vitro cytotoxic activity for compounds 2a,b,f-i.

Synthesis and Antitumor Activity of a New Class of Pyrazolo[4,3-e]pyrrolo[1,2-a][1,4]diazepinone Analogs of Pyrrolo[1,4][2,1-c]benzodiazepines

BARALDI, Pier Giovanni;CACCIARI, Barbara;MANFREDINI, Stefano;SIMONI, Daniele;
1994

Abstract

A new class of pyrrolo[l,4lbenzodiazepine (PBD) analogues featuring a pyrazolo[4,3-e]pyrrolo- [l72-al[l,4]diazepinone ring system has been designed and synthesized. These compounds, 2a-0, are characterized by the substitution of the aromatic A ring, characteristic of the PBDs, with a disubstituted pyrazole ring bearing alkyl and benzyl substituents at N6 or N7 and alkyl or carbomethoxy substituents at c8. Biological evaluation revealed an appreciable in vitro cytotoxic activity for compounds 2a,b,f-i.
1994
Baraldi, Pier Giovanni; Leoni, Alberto; Cacciari, Barbara; Manfredini, Stefano; Simoni, Daniele; Bergomi, Marzia; Menta, Ernesto; Spinelli, Silvano...espandi
File in questo prodotto:
Non ci sono file associati a questo prodotto.

I documenti in SFERA sono protetti da copyright e tutti i diritti sono riservati, salvo diversa indicazione.

Utilizza questo identificativo per citare o creare un link a questo documento: https://hdl.handle.net/11392/460435
 Attenzione

Attenzione! I dati visualizzati non sono stati sottoposti a validazione da parte dell'ateneo

Citazioni
  • ???jsp.display-item.citation.pmc??? ND
  • Scopus 20
  • ???jsp.display-item.citation.isi??? 23
social impact