设计用于抗增殖活性的新型紫苏基二氢嘧啶酮杂化物的合成。
Synthesis of novel perillyl-dihydropyrimidinone hybrids designed for antiproliferative activity.
作者信息
Vendrusculo Vinicius, de Souza Vanessa P, M Fontoura Luiz Antônio, M D'Oca Marcelo G, Banzato Thais P, Monteiro Paula A, Pilli Ronaldo A, de Carvalho João Ernesto, Russowsky Dennis
机构信息
Instituto de Química , Universidade Federal do Rio Grande do Sul , Porto Alegre , RS , Brazil . Email:
Fundação da Ciência e Tecnologia do Estado do Rio Grande do Sul , Porto Alegre , RS , Brazil.
出版信息
Medchemcomm. 2018 Jul 31;9(9):1553-1564. doi: 10.1039/c8md00270c. eCollection 2018 Sep 1.
Abstract
A series of fifteen novel dihydropyrimidinone hybrid compounds were synthesized in good yields a multicomponent reaction combined with the Huisgen reaction. The antiproliferative activity was investigated against nine tumor cell lines, and four hybrid compounds (TGI < 10 μM) showed promising antiproliferative activity against the tumor cell lines OVCAR-3 (ovarian), UACC-62 (melanoma) and U251 (glioma). Several hybrid compounds assayed have high TGI values (TGI 147.92-507.82) for the human keratinocyte cell line (HaCat), which reveals selectivity to cancer cells.
摘要
通过多组分反应与惠斯根反应相结合，以良好的产率合成了一系列十五种新型二氢嘧啶酮杂化化合物。研究了它们对九种肿瘤细胞系的抗增殖活性，四种杂化化合物（TGI < 10 μM）对肿瘤细胞系OVCAR - 3（卵巢癌）、UACC - 62（黑色素瘤）和U251（胶质瘤）显示出有前景的抗增殖活性。所测定的几种杂化化合物对人角质形成细胞系（HaCat）具有高TGI值（TGI 147.92 - 507.82），这表明对癌细胞具有选择性。
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