Design, synthesis and biological evaluation of triazolo[1,5-a]pyrimidine derivatives as new antiproliferative agents with multikinase inhibitory activity.

Two series of triazolo[1,5-a]pyrimidines were designed and synthesized as antiproliferative agents targeting multi kinase inhibition aiming to increase potency and combat drug resistance. The synthesized compounds were tested for their antiproliferative activity. The triazolopyrimidine derivatives 9b, 9c, 12b and 12c showed promising anticancer activities, in particular, compounds 12b and 12c displayed broad spectrum antiproliferative potential against NCI cancer cell lines with GI mean value of 10.

Novel benzenesulfonamides aryl and arylsulfone conjugates adopting tail/dual tail approaches: Synthesis, carbonic anhydrase inhibitory activity and molecular modeling studies.

New series of benzenesulfonamide and benzoic acid derivatives were designed and synthesized using tail/dual tail approach to improve potency and selectivity as carbonic anhydrase inhibitors. The synthesized compounds evaluated as CAIs against isoforms hCA I, II, IV and IX with acetazolamide (AAZ) as standard inhibitor. The benzenesulfonamide derivatives 7a-d, 8a-h, 12a-c, 13a and 15a-c showed moderate to potent inhibitory activity with selectivity toward isoform hCA II, especially, compound 13a with (K = 7.