Driscoll J S, Melnick N R, Quinn F R, Lomax N, Davignon J P, Ing R, Abott B J, Congleton G, Dudeck L
Cancer Treat Rep. 1978 Jan;62(1):45-74.
Compounds with known psychotropic properties were tested for activity in murine ip L1210 leukemia and B 16 melanoma in a protocol designed to obtain leads for new antitumor agents which might also possess central nervous system (CNS) antitumor properties. Barbiturates and hallucinogenic compounds were the only compound types deliberately excluded. Representatives from most of the other known CNS agent classes were included among the 297 psychotropic drugs evaluated. Sixteen of these agents were reproducibly active against the L1210 tumor system with T/C values of 125%. Phenothiazines such as fluphenazine and butyrophenones such as triperidol were prominent among the confirmed active structural types. Dopamine, a beta-phenethylamine neurotrasmitter, was active. While reproducible B16 melanoma activity was not observed among the psychotropic drugs, most of the L1210 confirmed active agents were effective against the ip P388 tumor model and also were active in vitro against KB cells. Ic L1210 activity was not observed among the few compounds chosen for testing in that tumor system. The yield of ip L1210 confirmed actives from this group of psychotropic agents was 18 times that which would have been expected from the random screening of compounds.
对具有已知精神活性的化合物进行了测试，以观察其对小鼠腹腔注射L1210白血病和B16黑色素瘤的活性。该实验方案旨在寻找可能同时具有中枢神经系统（CNS）抗肿瘤特性的新型抗肿瘤药物线索。巴比妥类药物和致幻化合物是特意排除的仅有的化合物类型。在评估的297种精神药物中，包括了大多数其他已知中枢神经系统药物类别的代表药物。其中16种药物对L1210肿瘤系统具有可重复的活性，T/C值为125%。在已确认的活性结构类型中，氟奋乃静等吩噻嗪类药物和三氟哌多等丁酰苯类药物较为突出。多巴胺，一种β-苯乙胺神经递质，具有活性。虽然在精神药物中未观察到对B16黑色素瘤的可重复活性，但大多数对L1210肿瘤已确认有活性的药物对腹腔注射P388肿瘤模型有效，并且在体外对KB细胞也有活性。在为该肿瘤系统选择测试的少数化合物中未观察到对L1210肿瘤的活性。从这组精神药物中获得的对腹腔注射L1210肿瘤有活性的药物产率是化合物随机筛选预期产率的18倍。
