Lucietto P, de Castiglione R, Gozzini L
Farmitalia Carlo Erba R. & D., Milano, Italy.
Farmaco. 1991 Oct;46(10):1111-20.
Four alkylating bombesin (BN) analogues (two C-terminal and one N-terminal chloromethylketone derivatives, and one chloroethylnitrosourea derivative) were synthesized and tested in Swiss 3T3 fibroblasts for receptor binding and mitogenic activity. Although they bound to the BN receptor with no or very weak mitogenic activity, no one analogue inhibited BN-induced thymidine incorporation in the contemporaneous treatment; only one behaved as a weak receptor antagonist when given 24 h before BN stimulation.
合成了四种烷基化蛙皮素（BN）类似物（两种C末端和一种N末端氯甲基酮衍生物，以及一种氯乙基亚硝基脲衍生物），并在瑞士3T3成纤维细胞中测试其受体结合和促有丝分裂活性。尽管它们与BN受体结合时没有或只有非常微弱的促有丝分裂活性，但在同时处理时没有一种类似物能抑制BN诱导的胸苷掺入；只有一种在BN刺激前24小时给予时表现为弱受体拮抗剂。
