177409-18-6Relevant academic research and scientific papers
DNA sequence-recognizing properties of minor groove alkylating agents / Effects of the replacement of N-methylpyrrole by an N-methylimidazole on tallimustine and its own homologue
Baraldi, Pier Giovanni,Romagnoli, Romeo,Spalluto, Giampiero,Cozzi, Paolo,Mongelli, Nicola,Bianchi, Nicoletta,Gambari, Roberto
, p. 309 - 315 (2007/10/03)
The linkage of an heterocycle, like N-methylimidazole, to minor DNA groove binders containing two or three pyrroles lead to a new class of oligopeptides with reduced antitumor activity both in vitro and in vivo if compared to tallimustine (CAS 115308-98-0) and its tetrapyrrole homologue 9. In the present paper is reported the correlation between the cytoxicity of tallimustine and its derivatives 9-11 with their ability to inhibit polymerase chain reaction (PCR) amplification of oestrogen receptor and Ha- ras gene sequences, containing A+T rich and G+C rich regions, respectively. Tallimustine and its tetrapyrrole homologue 9 were found to have higher sequence selectivity for the human oestrogen receptor (ER) gene with respect to the relative imidazole-containing analogues.
Novel benzoyl nitrogen mustard derivatives of pyrazole analogues of distamycin A: Synthesis and antileukemic activity
Baraldi, Pier Giovanni,Cozzi, Paolo,Geroni, Cristina,Mongelli, Nicola,Romagnoli, Romeo,Spalluto, Giampiero
, p. 251 - 262 (2007/10/03)
The design and synthesis of novel benzoic acid mustard (BAM) derivatives of distamycin A bearing one or more pyrazole rings replacing the pyrrole rings of the latter are described. In vitro and in vivo activities against L1210 leukemia are reported and discussed. Some of these compounds show an activity profile comparable to tallimustine 1. All the compounds bearing the pyrazole ring close to the BAM moiety show reduced cytotoxicity in comparison to derivatives characterized by the BAM linked to a pyrrole: the same effect has not been observed when occurring at the amidine terminus of the oligopeptidic frame. Copyright (C) 1999 Elsevier Science Ltd.
