具有强大抗肿瘤活性的萘酰亚胺-咪唑并吖啶酮的优化，通向临床候选药物（HKH40A，RTA 502）。
Optimization of naphthalimide-imidazoacridone with potent antitumor activity leading to clinical candidate (HKH40A, RTA 502).
作者信息
Hariprakasha Humcha K, Kosakowska-Cholody Teresa, Meyer Colin, Cholody Wieslaw M, Stinson Sherman F, Tarasova Nadya I, Michejda Christopher J
机构信息
Molecular Aspects of Drug Design Section, Structural Biophysics Laboratory, Center for Cancer Research, NCI-Frederick, Frederick, MD 21702, USA.
出版信息
J Med Chem. 2007 Nov 15;50(23):5557-60. doi: 10.1021/jm7009777. Epub 2007 Oct 16.
Unsymmetrical bifunctional antitumor agent WMC79 was further optimized to generate compound 7b that not only inhibited the growth of many tumor cell lines, but caused rapid apoptosis. Unlike the parent compound, 7b is toxic to both p53 positive and negative cancer cells. It has potent in vivo activity against xenografts of human colon and pancreatic tumors in athymic mice.
不对称双功能抗肿瘤药物WMC79经过进一步优化，生成了化合物7b，该化合物不仅能抑制多种肿瘤细胞系的生长，还能引发快速凋亡。与母体化合物不同，7b对p53阳性和阴性癌细胞均有毒性。它对无胸腺小鼠体内的人结肠癌和胰腺癌异种移植瘤具有强大的体内活性。
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