新型细胞毒性磷脂用于前列腺癌的合成及生物学评价
Synthesis and biological evaluation of novel cytotoxic phospholipids for prostate cancer.
作者信息
Gududuru Veeresa, Hurh Eunju, Durgam Gangadhar G, Hong Seoung Soo, Sardar Vineet M, Xu Huiping, Dalton James T, Miller Duane D
机构信息
Department of Pharmaceutical Sciences, College of Pharmacy, University of Tennessee, Memphis, TN 38163, USA.
出版信息
Bioorg Med Chem Lett. 2004 Oct 4;14(19):4919-23. doi: 10.1016/j.bmcl.2004.07.026.
We describe herein synthesis, SAR, and biological evaluation of a novel series of cytotoxic serine amide phosphates (SAPs) for prostate cancer. These compounds were tested for their cytotoxicity in five human prostate cancer cell lines (DU-145, PC-3, LNCaP, PPC-1, and TSU), and in CHO and RH7777 cells (negative controls). Comparison of anticancer effects of these compounds with a standard chemotherapeutic agent 5-fluorouracil shows that they are very effective in killing prostate cancer cells with low micromolar cytotoxicity and provide us a new lead for the development of drugs for prostate cancer.
我们在此描述了一系列用于前列腺癌的新型细胞毒性丝氨酸酰胺磷酸盐（SAPs）的合成、构效关系（SAR）及生物学评价。这些化合物在五种人前列腺癌细胞系（DU-145、PC-3、LNCaP、PPC-1和TSU）以及CHO和RH7777细胞（阴性对照）中进行了细胞毒性测试。将这些化合物的抗癌效果与标准化疗药物5-氟尿嘧啶进行比较，结果表明它们在低微摩尔细胞毒性下对杀死前列腺癌细胞非常有效，为我们开发前列腺癌药物提供了新的先导化合物。
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