Highly efficient antitumor agents of heterocycles containing sulfur atom: linear and angular thiazonaphthalimides against human lung cancer cell in vitro.
A novel series of aminothiazonaphthalimides, A(1-2) and B(1-2), has been regioselectively synthesized. The linear compounds B(1-2) were evaluated to be far more active than their angular isomers A(1-2) in antitumor evaluation. The linear compounds C-F, derived from compound B(1), all showed highly efficient antitumor activities against A549 and P388 cell lines. Also, cytotoxicities of these four analogues against two tumor cells were highly dependent on the length of the side chains. The compound A(1) or B(1), with two methylene units in the side chain, was more cytotoxic than its corresponding homologue A(2) or B(2), with one more methylene unit.
Qian
Xuhong
X
State Key Laboratory of Bioreactor Engineering and Shanghai Key Laboratory of Chemical Biology, School of Pharmacy, East China University of Science and Technology, Shanghai, China. xhqian@ecust.edu.cn
Li
Zhigang
Z
Yang
Qing
Q
D000970:Antineoplastic Agents / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology*; D045744:Cell Line, Tumor; D006571:Heterocyclic Compounds / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology*; D006801:Humans; D008175:Lung Neoplasms / Q000188:drug therapy; D053644:Naphthalimides / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology*; D013329:Structure-Activity Relationship; D013457:Sulfur Compounds / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology*
D000970:Antineoplastic Agents; D006571:Heterocyclic Compounds; D053644:Naphthalimides; D013457:Sulfur Compounds