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3-(3-(取代苯基)丙烯酰基)-2H-色烯-2-酮作为选择性抗乳腺癌药物的设计、合成及抗癌筛选

Design, synthesis and anticancer screening of 3-(3-(substituted phenyl) acryloyl)-2H-chromen-2ones as selective anti-breast cancer agent.

作者信息

Mokale Santosh N, Begum Afreen, Sakle Nikhil S, Shelke Vishakha R, Bhavale Swati A

机构信息

Dr. Rafiq Zakaria Campus, Y.B. Chavan College of Pharmacy, Aurangabad 431001, Maharashtra, India.

Dr. Rafiq Zakaria Campus, Y.B. Chavan College of Pharmacy, Aurangabad 431001, Maharashtra, India.

出版信息

Biomed Pharmacother. 2017 May;89:966-972. doi: 10.1016/j.biopha.2017.02.089. Epub 2017 Mar 9.

DOI:10.1016/j.biopha.2017.02.089
PMID:28292025
Abstract

By utilizing concept of molecular hybridization, involving combination of various Pharmacophore, novel substituted coumarin-chalcone hybrids was synthesized and evaluated for anti-proliferative activity against estrogen receptor-positive MCF-7 and negative MDA-MB-435 breast cancer cell lines. In-vivo study was carried out by N-methyl nitrosourea (MNU) induced mammary carcinoma in virgin female Spraque Dawly (SD) rats. The compound 5b has highest potential than standard drug Adriamycin, comparable against Tamoxifen against ER-positive MCF-7 breast cancer cell lines. Docking study was performed to study the binding orientation and affinity of synthesized compounds on the ER-α enzyme.

摘要

通过利用分子杂交的概念，涉及各种药效团的组合，合成了新型取代香豆素-查尔酮杂化物，并评估了其对雌激素受体阳性MCF-7和阴性MDA-MB-435乳腺癌细胞系的抗增殖活性。通过N-甲基亚硝基脲（MNU）诱导处女雌性斯普拉格-道利（SD）大鼠发生乳腺癌进行体内研究。化合物5b比标准药物阿霉素具有更高的潜力，在抗雌激素受体阳性MCF-7乳腺癌细胞系方面与他莫昔芬相当。进行对接研究以研究合成化合物在雌激素受体-α酶上的结合方向和亲和力。

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