Synthesis and Primary Cytotoxic Screening of Some 3- Sulfonamide Substituted Benzamido-benzimidazolones

Several cycline dependent kinase 2 (cdk2) inhibitors with different chemical structureshave been introduced. the hinge region of cdk2 (residues 81-84) contains a set of hydrogenbond donor and acceptor sites some of which must be satisfied for potent inhibitor binding.the benzimidazolone skeleton may provide such interactions. accordingly, 3-su]fonamidesubstituted benzamido-benzirnidazolones 24-31 were prepared starting from benzoic acid togive the acyl chloride ] which was reacted with different amines to afford the acids 2-9. theacids were changed to their corresponding acyl chlorides ]0-] 7. reaction of ]0-17 with 0nitropheylhydrazine gave the nitro derivatives 18-25 followed by reduction of the nitro groupsto give 26-33 which were then reacted with ethyl chlorofonnate to give the target compounds34-4]. the 3-pyridyl derivative 47 was prepared starting with chlorosulfonyl benzoylchloride to give the acid 43 which was changed to the corresponding acyl, nitro and aminoderivatives 44, 45 and 46, respectively, followed by the final ring closure reaction to give 47.the dibenzimidazolinoe derivative 49 was also obtained from the reaction of isopropcnylbenzimidazolone48 and 3-chloro sulfonyl benzoyl chloride. the target compounds were thentested against the cancer cell lines, ilepa 02, ht-29, cll-5 and aos. results indicated thatthe target compounds did not show reasonable cell growth inhibition comparing to the positiveand negative controls