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EnglishThe 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
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| Data di pubblicazione: | 2000 | |
| Titolo: | 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 | |
| Autori: | BARALDI P G; R. ROMAGNOLI; SPALLUTO G; COZZI P; MONGELLI N; BIANCHI N; GAMBARI R | |
| Rivista: | ARZNEIMITTEL-FORSCHUNG | |
| Abstract: | 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 | |
| Handle: | http://hdl.handle.net/11392/517096 | |
| Appare nelle tipologie: | 03.1 Articolo su rivista |
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