title: Bombesin receptor antagonists. 5 new irreversible alkylating analogues.
abstract: New alkylating bombesin analogues were synthesized in order to increase their solubility and stability in aqueous solutions. The best compromise between these parameters and the biological properties (receptor binding and antagonistic activity) was achieved with 4-[bis(2-chloro-ethylamino)]benzoyl derivatives of the BN (7-14) octapeptide carrying a (13-14) reduced peptide bond independently of the presence of a His12 residue, either free or protected.
authors.affiliation: Farmitalia Carlo Erba R & D, Milano, Italy.
authors.forename: R
authors.initials: R
authors.lastname: de Castiglione
authors.forename: L
authors.initials: L
authors.lastname: Gozzini
authors.forename: M
authors.initials: M
authors.lastname: Galantino
authors.forename: F
authors.initials: F
authors.lastname: Corradi
authors.forename: M
authors.initials: M
authors.lastname: Ciomei
authors.forename: F
authors.initials: F
authors.lastname: Roletto
authors.forename: F
authors.initials: F
authors.lastname: Bertolero
mesh_terms: D000477:Alkylating Agents / Q000737:chemistry / Q000494:pharmacology*; D000595:Amino Acid Sequence; D055598:Chemical Phenomena; D002627:Chemistry, Physical; D007457:Iodine Radioisotopes; D008934:Mitogens; D008969:Molecular Sequence Data; D018004:Receptors, Bombesin; D017981:Receptors, Neurotransmitter / Q000037:antagonists & inhibitors*; D012995:Solubility
chemical_list: D000477:Alkylating Agents; D007457:Iodine Radioisotopes; D008934:Mitogens; D018004:Receptors, Bombesin; D017981:Receptors, Neurotransmitter