Cihan-Üstündağ Gökçe, Şatana Dilek, Özhan Gül, Çapan Gültaze
a Department of Pharmaceutical Chemistry , Faculty of Pharmacy .
b Department of Microbiology and Clinical Microbiology , Istanbul Faculty of Medicine , and.
J Enzyme Inhib Med Chem. 2016;31(3):369-80. doi: 10.3109/14756366.2015.1024673. Epub 2015 Apr 24.
A new series of indolylhydrazones (6) and indole-based 4-thiazolidinones (7, 8) have been designed, synthesized and screened for in vitro antitubercular activity against Mycobacterium tuberculosis H37Rv. 4-Thiazolidinone derivatives 7g-7j, 8g, 8h and 8j displayed notable antituberculosis (anti-TB) activity showing 99% inhibition at MIC values ranging from 6.25 to 25.0 µg/ml. Compounds 7g, 7h, 7i, 8h and 8j demonstrated anti-TB activity at concentrations 10-fold lower than those cytotoxic for the mammalian cell lines. The indolylhydrazone derivative 6b has also been evaluated for antiproliferative activity against human cancer cell lines at the National Cancer Institute (USA). Compound 6b showed an interesting anticancer profile against different human tumor-derived cell lines at sub-micromolar concentrations with obvious selectivity toward colon cancer cell line COLO 205.
设计、合成了一系列新型吲哚腙（6）和基于吲哚的4-噻唑烷酮（7、8），并对其针对结核分枝杆菌H37Rv的体外抗结核活性进行了筛选。4-噻唑烷酮衍生物7g - 7j、8g、8h和8j表现出显著的抗结核活性，在6.25至25.0µg/ml的最低抑菌浓度（MIC）值下显示出99%的抑制率。化合物7g、7h、7i、8h和8j在比其对哺乳动物细胞系具有细胞毒性的浓度低10倍的浓度下表现出抗结核活性。吲哚腙衍生物6b也在美国国立癌症研究所针对人癌细胞系进行了抗增殖活性评估。化合物6b在亚微摩尔浓度下对不同的人肿瘤衍生细胞系显示出有趣的抗癌谱，对结肠癌细胞系COLO 205具有明显的选择性。
