Bombesin receptor antagonists. 5 new irreversible alkylating analogues.
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.
de Castiglione
R
R
Farmitalia Carlo Erba R & D, Milano, Italy.
Gozzini
L
L
Galantino
M
M
Corradi
F
F
Ciomei
M
M
Roletto
F
F
Bertolero
F
F
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
D000477:Alkylating Agents; D007457:Iodine Radioisotopes; D008934:Mitogens; D018004:Receptors, Bombesin; D017981:Receptors, Neurotransmitter