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香豆素杂合体:乳腺癌治疗中的有前途的支架。

Coumarin Hybrids: Promising Scaffolds in the Treatment of Breast Cancer.

机构信息

Department of Pharmaceutical Chemistry, Indo-Soviet Friendship College of Pharmacy (ISFCP), Moga-142001, India.

Department of Pharmaceutical Sciences, MRSPTU, Bathinda-151001, India.

出版信息

Mini Rev Med Chem. 2019;19(17):1443-1458. doi: 10.2174/1389557519666190308122509.

Abstract

Breast cancer is the most common invasive cancer in women, and the second main cause of deaths in women, after lung cancer. There is continuous advancement in the development of therapeutic agents against breast cancer in recent years and it is still in progress. Development of hybrid molecules by combining different pharmacophores to obtain significant biological activity is an excellent approach. Coupling of coumarin scaffold with other distinct motifs has led to the design of newer compounds against breast cancer. These distinct pharmacophores possess a diverse mode of action as well as selectivity. It has been reported in the literature that coumarin hybrids possess significant potency against breast cancer by binding to various biological targets which are associated with breast cancer. Due to low toxicity profile on various organ systems, coumarin hybrids have nowadays attracted the keen attention of researchers to explore their therapeutic ability against breast cancer. Reported coumarin hybrids include coupling with isoxazole, thiazole, monastrol, chalcone, triazole, sulphonamide, triphenylethylene, benzimidazole, pyran, imidazole, stilbene, oestrogen, phenylsulphonylfuroxan, etc. In the present review, a description of various coumarin hybrid molecules has been presented along with their structural-activity relationships.

摘要

乳腺癌是女性最常见的侵袭性癌症,也是仅次于肺癌的女性死亡的第二大主要原因。近年来,针对乳腺癌的治疗药物不断取得进展,这一进程仍在继续。通过结合不同药效团来开发具有显著生物活性的杂交分子是一种很好的方法。将香豆素支架与其他不同的结构基序结合,设计出了针对乳腺癌的新型化合物。这些不同的药效团具有不同的作用模式和选择性。文献报道,香豆素杂合子通过与各种与乳腺癌相关的生物靶点结合,具有显著的抗乳腺癌活性。由于对各种器官系统的毒性低,香豆素杂合子如今引起了研究人员的极大关注,以探索其针对乳腺癌的治疗能力。报道的香豆素杂合子包括与异噁唑、噻唑、单端孢霉烯、查耳酮、三唑、磺胺、三苯乙烯、苯并咪唑、吡喃、咪唑、二苯乙烯、雌激素、苯磺酰基呋喃二酮等的偶联。在本综述中,介绍了各种香豆素杂合分子,并对其结构-活性关系进行了描述。

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