Abstract:
:In an effort to discover potent antitumor agents, a series of novel C-7-heteroaryl-substituted camptothecin derivatives were designed and synthesized via microwave-promoted Suzuki coupling reaction. These analogs were then assessed for cytotoxicity against three human tumor cell lines, A549, HCT116, HT-29, and inhibitory effects on topoisomerase I. All of the new compounds showed potent inhibition of human tumor cell growth, among which compound 10a showed higher cytotoxic activity than that of SN-38. Furthermore, this series of compounds retained or enhanced Topo I inhibition.
journal_name
Bioorg Med Chem Lettjournal_title
Bioorganic & medicinal chemistry lettersauthors
Wang L,Huang Y,Zhang J,Tong L,Chen Y,Lu W,Huang Qdoi
10.1016/j.bmcl.2014.01.049subject
Has Abstractpub_date
2014-03-15 00:00:00pages
1597-9issue
6eissn
0960-894Xissn
1464-3405pii
S0960-894X(14)00079-1journal_volume
24pub_type
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