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An efficient one-pot synthesis of novel pyrazolo[3,4- b][1,8]naphthyridine and pyrazolo[3,4- d]pyrimido[1,2- a]pyrimidine derivatives has been investigated from the reaction of 2-amino (pyrimidine or pyridine), aromatic aldehydes and 3-methyl-1-phenyl-2-pyrazolin-5-one. All synthesized compounds were evaluated for in vivo anti-inflammatory activity using carrageenan-induced rat paw edema assay. Compounds 4a, 4e, 4g, 5a, 5b (80%) and 5c (86%) showed good to excellent results when compared with the anti-inflammatory active standard drug diclofenac Na (93%). On the basis of the structure-activity relationship, the anti-inflammatory activity of pyrazolo[3,4- d]pyrimido[1,2- a]pyrimidine derivatives has been found to be much better than pyrazolo[3,4- b][1,8]naphthyridine derivatives. [ABSTRACT FROM AUTHOR]

The present study describes the synthesis and in vitro anticancer activity of novel piritrexim analogs against human breast cancer cell line MCF-7 and a normal Vero monkey cell line. The scheme involves the formation of 3-(4-nitrophenyl)-4-phenyl-1,8-naphthyridin-2-amine accomplished by the condensation reaction of 4-nitrophenyl acetonitrile, aromatic aldehyde, and 2-aminopyridine using acetic acid as a catalyst. The selected synthesized compounds have been screened against a human breast cancer cell line MCF-7 and a normal Vero monkey cell line, out of which the compounds 4b, 4e, 4f exhibited higher potency (GI [<10 µg/mL)], and compounds 4a, 4c show moderate to good activity (GI 41.4 and 12.4 µg/mL ) towards human breast cancer cell line MCF-7. Docking study on dihydrofolate reductase enzyme receptor (DHFR) and epidermal growth factor receptor reveals that compounds 4a, 4b, 4c, and 4e show moderate to good binding along with acceptable glide scores. Graphical Abstract: [ABSTRACT FROM AUTHOR]