Instituto de Química Rosario (CONICET-UNR), Facultad de Ciencias Bioquímicas y Farmacéuticas, Universidad Nacional de Rosario, Suipacha 531, 2000 Rosario, Argentina.
Instituto de Genética Experimental, Facultad de Ciencias Médicas, Universidad Nacional de Rosario, Santa Fe 3100, 2000 Rosario, Argentina.
Org Biomol Chem. 2020 Apr 1;18(13):2475-2486. doi: 10.1039/d0ob00280a.
Propargylamines have gained importance in the area of anticancer research. We synthesized 1-substituted propargylic tertiary amines using the A3-coupling as the key step. Both, solution and solid-phase protocols, were used to provide a library of 1-substituted propargylic tertiary amines with interesting structural diversity. The triple negative breast cancer subtype is the most aggressive and it lacks effective therapeutic options, while pancreatic cancer is one of the neoplasms with worse prognosis and limited therapeutic possibilities. The development of tumor-selective drugs has always been a major challenge in cancer treatment. From our library, two propargylamines displayed a high degree of cytotoxic selectivity. These levels of selectivity give a very interesting perspective for further development of 1-substituted propargylic tertiary amines as new potential chemotherapeutic antitumor agents.
炔丙胺在抗癌研究领域受到重视。我们使用 A3 偶联作为关键步骤合成了 1-取代炔丙基叔胺。我们使用溶液相和固相方案提供了具有有趣结构多样性的 1-取代炔丙基叔胺文库。三阴性乳腺癌亚型是最具侵袭性的，缺乏有效的治疗选择，而胰腺癌是预后最差且治疗选择有限的肿瘤之一。开发肿瘤选择性药物一直是癌症治疗的主要挑战。在我们的文库中，两种炔丙胺表现出很高的细胞毒性选择性。这种选择性水平为进一步开发 1-取代炔丙基叔胺作为新的潜在化疗抗肿瘤药物提供了非常有趣的前景。
