一锅法合成吡唑啉衍生咔唑类化合物作为抗结核、抗癌药物，及其 DNA 切割和抗氧化活性。
One-pot synthesis of pyrazoline derivatised carbazoles as antitubercular, anticancer agents, their DNA cleavage and antioxidant activities.
机构信息
PG Department of Studies in Chemistry, Karnatak University, Pavate Nagar, Dharwad 580 003, India.
出版信息
Eur J Med Chem. 2011 Sep;46(9):4366-73. doi: 10.1016/j.ejmech.2011.07.007. Epub 2011 Jul 12.
Novel tricyclic carbazoles 4a-k were synthesized in one-pot employing sydnone derivatives 3a-k as masked hydrazines by the ring transformation in presence of conc. HCl and cyclohexanone. The title compounds were screened for anti-tubercular, anti cancer, DNA cleavage, antioxidant activity. MIC, GI50, LC50, TGI were evaluated. The title compounds have exhibited significant antitubercular, DNA cleavage and antioxidant activities and partial anticancer activity.
新型三环咔唑 4a-k 是通过在浓盐酸和环己酮存在下的环转化，以 sydnone 衍生物 3a-k 为掩蔽肼一锅法合成的。对标题化合物进行了抗结核、抗癌、DNA 切割、抗氧化活性筛选。评估了 MIC、GI50、LC50、TGI。标题化合物表现出显著的抗结核、DNA 切割和抗氧化活性以及部分抗癌活性。
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