Anticancer and immunomodulatory activities of novel 1,8-naphthyridine derivatives.
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 IC(50) of 0.41 and 0.77 microM on MIAPaCa and K-562 cancer cell lines, respectively while, compound 36 had IC(50) of 1.19 microM on PA-1 cancer cell line. However, one of the unsubstituted 1,8-naphthyridine-C-3'-heteroaryl derivative 29 showed potent cytotoxicity with IC(50) of 0.41 and 1.4 microM 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.
Kumar
Vivek
V
Chemical Research, Dabur Research Foundation, Sahibabad, Ghaziabad, 201 010 UP, India. kumarv@dabur.com
Madaan
Alka
A
Sanna
Vinod K
VK
Vishnoi
Manupriya
M
Joshi
Narendra
N
Singh
Anu T
AT
Jaggi
Manu
M
Sharma
Pramod K
PK
Irchhaiya
Raghuveer
R
Burman
Anand C
AC
D000970:Antineoplastic Agents / Q000138:chemical synthesis* / Q000494:pharmacology*; D045744:Cell Line, Tumor; D002470:Cell Survival / Q000187:drug effects; D004354:Drug Screening Assays, Antitumor; D006801:Humans; D007155:Immunologic Factors / Q000138:chemical synthesis* / Q000494:pharmacology*; D020128:Inhibitory Concentration 50; D015394:Molecular Structure; D009287:Naphthyridines / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology
D000970:Antineoplastic Agents; D007155:Immunologic Factors; D009287:Naphthyridines