当前位置：
X-MOL 学术
›
ACS Med. Chem. Lett.
›
论文详情
Our official English website, www.x-mol.net, welcomes your
feedback! (Note: you will need to create a separate account there.)
Antiglioma Activity of Aryl and Amido-Aryl Acetamidine Derivatives Targeting iNOS: Synthesis and Biological Evaluation.
ACS Medicinal Chemistry Letters ( IF 3.5 ) Pub Date : 2020-06-19 , DOI: 10.1021/acsmedchemlett.0c00285 Cristina Maccallini 1 , Fabio Arias 2 , Marialucia Gallorini 1 , Pasquale Amoia 1 , Alessandra Ammazzalorso 1 , Barbara De Filippis 1 , Marialuigia Fantacuzzi 1 , Letizia Giampietro 1 , Amelia Cataldi 1 , María Encarnación Camacho 2 , Rosa Amoroso 1
ACS Medicinal Chemistry Letters ( IF 3.5 ) Pub Date : 2020-06-19 , DOI: 10.1021/acsmedchemlett.0c00285 Cristina Maccallini 1 , Fabio Arias 2 , Marialucia Gallorini 1 , Pasquale Amoia 1 , Alessandra Ammazzalorso 1 , Barbara De Filippis 1 , Marialuigia Fantacuzzi 1 , Letizia Giampietro 1 , Amelia Cataldi 1 , María Encarnación Camacho 2 , Rosa Amoroso 1
Affiliation
|
Nitric oxide is an important inflammation mediator with a recognized role in the development of different cancers. Gliomas are primary tumors of the central nervous system with poor prognosis, and the expression of the inducible nitric oxide synthase correlates with the degree of malignancy, changes in vascular reactivity, and neo-angiogenesis. Therefore, targeting the nitric oxide biosynthesis appears as a potential strategy to impair glioma progression. In the present work a set of aryl and amido-aryl acetamidine derivatives were synthesized to obtain new potent and selective inducible nitric oxide synthase inhibitors with improved physicochemical parameters with respect to the previously published molecules. Compound 17 emerged as the most promising inhibitor and was evaluated on C6 rat glioma cell line, showing antiproliferative effects and high selectivity over astrocytes.
中文翻译：
靶向iNOS的芳基和酰胺基-芳基乙酰胺衍生物的抗神经胶质瘤活性：合成和生物学评估。
一氧化氮是重要的炎症介质，在各种癌症的发生中具有公认的作用。胶质瘤是中枢神经系统的原发性肿瘤，预后较差，诱导型一氧化氮合酶的表达与恶性程度，血管反应性变化和新血管生成相关。因此，靶向一氧化氮的生物合成似乎是损害神经胶质瘤进展的潜在策略。在本工作中，合成了一组芳基和酰胺基-芳基乙am衍生物，以获得相对于以前公开的分子而言具有改善的理化参数的新的有效和选择性诱导型一氧化氮合酶抑制剂。化合物17 它是最有希望的抑制剂，并在C6大鼠神经胶质瘤细胞系中进行了评估，显示出抗增殖作用和对星形胶质细胞的高选择性。
更新日期：2020-07-09
中文翻译：
靶向iNOS的芳基和酰胺基-芳基乙酰胺衍生物的抗神经胶质瘤活性：合成和生物学评估。
一氧化氮是重要的炎症介质，在各种癌症的发生中具有公认的作用。胶质瘤是中枢神经系统的原发性肿瘤，预后较差，诱导型一氧化氮合酶的表达与恶性程度，血管反应性变化和新血管生成相关。因此，靶向一氧化氮的生物合成似乎是损害神经胶质瘤进展的潜在策略。在本工作中，合成了一组芳基和酰胺基-芳基乙am衍生物，以获得相对于以前公开的分子而言具有改善的理化参数的新的有效和选择性诱导型一氧化氮合酶抑制剂。化合物17 它是最有希望的抑制剂，并在C6大鼠神经胶质瘤细胞系中进行了评估，显示出抗增殖作用和对星形胶质细胞的高选择性。
京公网安备 11010802027423号