Jindal Dharam Paul, Chattopadhaya Raja, Guleria Sheetal, Gupta Ranju
University Institute of Pharmaceutical Sciences, Panjab University, Chandigarh 160014, India.
Eur J Med Chem. 2003 Nov-Dec;38(11-12):1025-34. doi: 10.1016/j.ejmech.2003.09.002.
Various steroidal oxime ether derivatives in androstene and estrane series have been synthesized and evaluated for the antineoplastic activity at National Cancer Institute, Bethesda, Maryland, USA. O-alkylation of the oximes by various alkylaminoethyl halides gave the oxime ether derivatives. The 17alpha-ethynylandrostene derivatives 29 (DPJ-684), 30 (DPJ-685), 31 (DPJ-686) and estrane derivatives 35 (DPJ-531) and 36 (DPJ-532) were among the small percentage of compounds, which have been screened by NCI for in vivo hollow fiber assay by virtue of their activity against one or more human tumour cell lines in 60 cell line in vitro prescreen. The preliminary in vivo reports of hollow fiber assays have been referred to the Biological Evaluation Committee for Cancer Drugs for considering these compounds for further detailed in vivo testing.
在美国马里兰州贝塞斯达的国家癌症研究所，已经合成了雄甾烯和雌甾烷系列中的各种甾体肟醚衍生物，并对其抗肿瘤活性进行了评估。通过各种卤代烷基氨基乙基对肟进行O-烷基化反应，得到了肟醚衍生物。17α-乙炔基雄甾烯衍生物29（DPJ-684）、30（DPJ-685）、31（DPJ-686）以及雌甾烷衍生物35（DPJ-531）和36（DPJ-532）是一小部分化合物，它们凭借在60种细胞系体外预筛选中对一种或多种人类肿瘤细胞系的活性，被美国国家癌症研究所筛选用于体内中空纤维试验。中空纤维试验的初步体内报告已提交给癌症药物生物学评估委员会，以考虑对这些化合物进行进一步详细的体内测试。
