Clinical studies suggest that NSAIDs, particularly the highly selective cyclooxygenase (COX)-2 inhibitors, are promising anticancer agents. Pyrimidinyl-piperazine fused with heterocyclic benzothiazole derivatives have shown an array of biological activities viz. antimicrobial anticancer and anti-inflammatory. 8 Piperazines attached to benzimidazole and indole were found to have potent anti-inflammatory activity. 9 With this concept of acetamide bridge, N. M. Raghavendra et al, reported the pharmacological activity of N-(benzo[d]thiazol-2-yl)-2-(piperazin-1-yl) acetamide

analogs for their anti-inflammatory activity. 10 and 11 Pyrimidine and fused benzothiazole heterocycles are reported to be effective pharmacophores, Ahmed Kamal et al synthesized pyrazolo[1,5a] pyrimidine linked 2-aminobenzothizole find more conjugate which were evaluated for their anticancer activity against five human cancer cell lines.12 According to quantitative structure–activity

relationship approach Papadopoulou C et al, reported that derivatives of 4-phenyl-piperazine were found to be potent anti-inflammatory agents.13 Literature review showed that benzothiazole substituted at 4 or 5 positions with electron withdrawing groups have significant anti-inflammatory activity.14 In the light of these overall observations, prompted us to synthesize a novel derivatives ZD1839 of substituted N-(1,3-benzothiazol-2-yl)-2-[4-(5-cyano-6-imino-2-oxo-1,2,3,6-tetrahydropyrimidin-4-yl) piperazin-1-yl]acetamide, and to screen for In-vitro anti-inflammatory activity by inhibition of albumin denaturation technique and for anticancer activity at NCI. In present work target compounds were obtained by reaction of starting material of bis (methylthio) methylene malononitrile with molar equivalent Linifanib (ABT-869) amount of urea in presence of toluene and triethylamine for five hrs to give compound 4-imino-6-(methylsulfanyl)-2-oxo-1,2,3,4-tetrahydropyrimidine-5-carbonitrile

(1). Compound (1) posses nucleophilic replaceable active methylthio group at the 6th position, which is activated by the ring 1st position nitrogen atom and the electron withdrawing cyano group at 5th position, which was substituted by piperazine ring by reacting equal molar quantities of compound (1) & piperazine to give 4-imino-2-oxo-6-(piperazin-1-yl)-1,2,3,4-tetrahydropyrimidine-5-carbonitrile (2). The formation of compound (2) was confirmed by spectral data. Substituted 2-amino benzothiazoles reacted independently with chloroacetyl chloride to give substituted 2-chloroacetylamino benzothiazole (3a–3j).