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羟基亚胺甾体衍生物对乳腺癌细胞的体外合成及生物学评价

Synthesis and biological in vitro evaluation of the effect of hydroxyimino steroidal derivatives on breast cancer cells.

机构信息

Facultad de Ciencias Químicas, Laboratorio de Elucidación y Síntesis en Química Orgánica, Benemérita Universidad Autónoma de Puebla, 72570 Puebla, Mexico.

Herbario y Jardín Botánico Universitario, Benemérita Universidad Autónoma de Puebla, Ciudad Universitaria, 72570 Puebla, Mexico; Centro de Química, Instituto de Ciencias, Benemérita Universidad Autónoma de Puebla, 72570 Puebla, Mexico.

出版信息

Steroids. 2021 Feb;166:108787. doi: 10.1016/j.steroids.2020.108787. Epub 2020 Dec 28.

DOI:10.1016/j.steroids.2020.108787
PMID:33383064
Abstract

Breast cancer is the most common cause of cancer death in women, according to Global Cancer Observatory. This fact forces scientists to continue in the search for effective treatments against this aggressive type of cancer. Breast cancer frequently metastasizes to other organs, most often the bones, lungs, and liver. Breast cancer is normally associated with estrogen and progestogen levels and can be hormone or non-hormone dependent. In current experiments herein reported, some hydroxyimino spirostan derivatives showed great potential against MCF-7 breast cancer, a Luminal-A cancer. On the other hand, a set of synthesized 6-hydroxyimino-22-oxocholestane compounds had excellent activity against the MDA-MB-231 breast cancer cell line. The synthesis of hydroxyamino derivatives from spirostan and 22-oxocholestane compounds was improved. The hydroxyimino compounds enhanced the bioactivity when compared with their parent carbonyl skeletons.

摘要

根据全球癌症观测站的数据,乳腺癌是女性癌症死亡的最常见原因。这一事实迫使科学家继续寻找针对这种侵袭性癌症的有效治疗方法。乳腺癌经常转移到其他器官,最常见的是骨骼、肺部和肝脏。乳腺癌通常与雌激素和孕激素水平有关,可能是激素依赖性或非激素依赖性的。在本报告中进行的当前实验中,一些羟亚氨基螺甾烷衍生物对 MCF-7 乳腺癌(Luminal-A 癌症)显示出巨大的潜力。另一方面,一组合成的 6-羟亚氨基-22-氧代胆甾烷化合物对 MDA-MB-231 乳腺癌细胞系具有极好的活性。改进了螺甾烷和 22-氧代胆甾烷化合物的羟氨基衍生物的合成。与母体羰基骨架相比,羟亚氨基化合物提高了生物活性。

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