新型吡唑基核苷的合成、结构和抗癌活性评价研究。

Synthetic, Structural, and Anticancer Activity Evaluation Studies on Novel Pyrazolylnucleosides.

机构信息

Bioorganic Laboratory, Department of Chemistry, University of Delhi, Delhi 110 007, India.

Medicinal Chemistry Laboratory, Department of Chemistry, Acadia University, Wolfville, NS B4P 2R6, Canada.

出版信息

Molecules. 2019 Oct 30;24(21):3922. doi: 10.3390/molecules24213922.

DOI:10.3390/molecules24213922

PMID:31671703

原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC6864788/

Abstract

The synthesis of novel pyrazolylnucleosides -, -, -, and - are described. The structures of the regioisomers were elucidated by using extensive NMR studies. The pyrazolylnucleosides - and - were screened for anticancer activities on sixty human tumor cell lines. The compound showed good activity against 39 cancer cell lines. In particular, it showed significant inhibition against the lung cancer cell line Hop-92 (GI 9.3 µM) and breast cancer cell line HS 578T (GI 3.0 µM).

摘要

本文描述了新型吡唑基核苷 - 、 - 、 - 和 - 的合成。通过广泛的 NMR 研究阐明了区域异构体的结构。对吡唑基核苷 - 和 - 进行了 60 个人类肿瘤细胞系的抗癌活性筛选。化合物 - 对 39 种癌细胞系表现出良好的活性。特别是，它对肺癌细胞系 Hop-92（GI9.3µM）和乳腺癌细胞系 HS578T（GI3.0µM）表现出显著的抑制作用。