Synthesis of some anticancer agent conjugated to am
inoacids through amide 
bond with expected biological activity

Abbas Abdulridha; Kawkab Y. Saour

Abstract

Synthesis of some anticancer agent conjugated to am inoacids through amide bond with expected biological activity

Author(s): Abbas Abdulridha * and Kawkab Y. Saour

purines are an important group of organic compounds where several compounds containing a purine residu e are known to possess useful biological activity and use d as antibacterial, antifungal and antitumor agents . These pharmacological properties of purines aroused our i nterest in synthesizing several new 6-mercaptopurin e(6-MP) derivatives linked to amino acid via peptide bond w ith expected biological activity. 6-MP was S-alkyla ted by the methyl bromoacetate and then hydrolyzed with an al kaline sodium hydroxide solution to librate the fre e carboxylic group side chain. Also the alkylated 6-MP reacted w ith hydrazine hydrate to get hydrazide of 6-MP. Conventional solution method for peptide synthesis used as a cou pling method between the free carboxyl and amine gr oups. The proposed analogues were successfully synthesized an d their structural formulas were consistent with th e proposed structures as they were characterized and proved by thin layer chromatography (TLC), melting point, in frared spectroscopy (IR) and elemental microanalysis. All tested analogues showed an improved antistaphylococ cus activity in comparison with ofloxacin. Also the ana logues showed cytotoxic activity on the HeLa cell l ine ( cervical cancer cells) with inhibitory concentration percent of (IC %) range (16.79 % -39.28 %). It can be conc luded from the results that the synthesized compounds are prom ising as new anticancer candidates in future.

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