Synthesis of novel 4,6-disubstituted quinazoline derivatives, their anti-inflammatory and anti-cancer activity (cytotoxic) against U937 leukemia cell lines.

In view of the link between use of NSAIDs and altered cancer incidence and a growing evidence of COX-II implication in angiogenesis, a novel series of 4,6-disubstituted quinazoline derivatives have been synthesized starting from anthranilic acid derivatives 1 through conventional methods. Initially acylation followed by cyclisation to obtain benz-oxazinones 2 which on further treatment with ammonia yielded the crucial intermediate, 2-substituted benzamide (3). The products were subsequently cyclised to obtain quinazolones 4, chlorinated 5, then hooked to various optically pure alpha-amino acids to have 4,6-disubstituted quinazoline derivatives 6. All the derivatives 6 are screened for anti-inflammatory and anti-cancer activity against U937 leukemia cell lines. Some of the compounds exhibited promising anti-cancer activity with reference to standard drug Etoposide.

Anthelmintic activity of leaves of justicia beddomei.

Ethanolic and Chloroform extract of leaves of Justicia beddomei were evaluated separately for anthelmintic activity on adult Indian earthworms Pheretima posthuma, using Piperazine citrate as reference standard. The results indicated that ethanolic extract was more potent than the chloroform extract.

Analgesic activity of Justicia beddomei leaf extract.

The analgesic activity of ethanolic extract of Justicia beddome leaves (Family: Acanthaceae) was evaluated in albino rats using Eddy's hot plate method. The extract at 50 and 100 mg/ kg, (i.p), showed significant analgesic activity at 90 minutes of administration. The analgesic effect of the extract was comparable to that of morphine sulphate.