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硫代阿糖胞苷在人白血病和淋巴瘤异种移植模型中的临床前抗肿瘤活性。

Preclinical antitumor activity of thiarabine in human leukemia and lymphoma xenograft models.

作者信息

Waud William R, Gilbert Karen S, Secrist John A

机构信息

Cancer Therapeutics and Immunology Department, Southern Research Institute, P. O. Box 55305, Birmingham, AL 35255-5305, USA.

出版信息

Nucleosides Nucleotides Nucleic Acids. 2012;31(9):647-60. doi: 10.1080/15257770.2012.710768.

Abstract

Thiarabine was evaluated for antitumor activity in seven human leukemia, lymphoma, and myeloma xenograft models to explore the activity in hematological malignancies. Thiarabine was active against all of the human leukemia and lymphoma lines tested, being curative against HL-60 leukemia and AS283 lymphoma and effecting tumor regressions in CCRF-CEM, MOLT-4, and K-562 leukemia and RL lymphoma models, but did not exhibit any appreciable activity against RPMI-8226 myeloma. For the leukemia/lymphoma models, thiarabine was more efficacious than ara-C/palmO-ara-C (four models), clofarabine (three models), fludarabine monophosphate (five models), cladribine (four models), and gemcitabine (six models). Thiarabine warrants future clinical trials with leukemias/lymphomas.

摘要

对噻拉滨在七种人类白血病、淋巴瘤和骨髓瘤异种移植模型中的抗肿瘤活性进行了评估,以探索其在血液系统恶性肿瘤中的活性。噻拉滨对所有测试的人类白血病和淋巴瘤细胞系均有活性,可治愈HL-60白血病和AS283淋巴瘤,并使CCRF-CEM、MOLT-4和K-562白血病以及RL淋巴瘤模型中的肿瘤消退,但对RPMI-8226骨髓瘤未表现出任何明显活性。对于白血病/淋巴瘤模型,噻拉滨比阿糖胞苷/棕榈酰阿糖胞苷(四个模型)、氯法拉滨(三个模型)、氟达拉滨单磷酸盐(五个模型)、克拉屈滨(四个模型)和吉西他滨(六个模型)更有效。噻拉滨值得在白血病/淋巴瘤方面开展未来的临床试验。

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