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Research Article

Anticancer and immunomodulatory activities of novel 1,8-naphthyridine derivatives

, , , , , , , , & show all
Pages 1169-1178 | Received 27 Aug 2008, Accepted 12 Nov 2008, Published online: 21 Apr 2009
 

Abstract

A number of 1,8-naphthyridine derivatives (22–62) have been synthesized and screened for their in vitro cytotoxicity against eight tumors and two non-tumor cell lines. Halogen substituted 1,8-naphthyridine-3-caboxamide derivatives showed potent activity with compound 47 having IC50 of 0.41 and 0.77 μM on MIAPaCa and K-562 cancer cell lines, respectively while, compound 36 had IC50 of 1.19 μM on PA-1 cancer cell line. However, one of the unsubstituted 1,8-naphthyridine-C-3’-heteroaryl derivative 29 showed potent cytotoxicity with IC50 of 0.41 and 1.4 μM on PA-1 and SW620 cancer cell lines, respectively. These compounds were also evaluated for anti-inflammatory activity as suggested by downregulation of proinflammaotory cytokines.

Acknowledgment

Declaration of interest: The authors report no conflicts of interest. The authors alone are responsible for the content and writing of the paper.

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