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Synthesis and biological activity of some new 1-benzyl and 1-benzoyl-3-heterocyclic indole derivativesStarting from 1-benzyl- (2a) and 1-benzoyl-3-bromoacetyl indoles (2b) new heterocyclic, 2-thioxoimidazolidine (4a, b), imidazolidine-2,4-dione (5a, b), pyrano(2,3-d)imida-zole (8a, band9a, b), 2-substituted quinoxaline (11a, b-17a, b) and triazolo(4,3-a)quinoxaline derivatives (18a, band19a, b) were synthesized and evaluated for their antimicrobial and anticancer activities. Antimicrobial activity screening performed with concentrations of 0.88, 0.44 and 0.22 μg mm-2showed that 3-(1-substituted indol-3-yl)quinoxalin-2(1H)ones (11a, b) and 2-(4-methyl piperazin-1-yl)-3-(1-substituted indol-3-yl) quinoxalines (15a, b) were the most active of all the tested compounds towardsP. aeruginosa, B. cereusandS. aureuscompared to the reference drugs cefotaxime and piperacillin, while 2-chloro-3-(1-substituted indol-3-yl)quinoxalines (12a, b) were the most active against C.albicanscompared to the reference drug nystatin. On the other hand, 2-chloro-3-(1-benzyl indol-3-yl) quinoxaline12adisplay potent efficacy against ovarian cancer xenografts in nude mice with tumor growth suppression of 100.0 ± 0.3 %.

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Positive evidence for anticancer activities of honey is growing and the mechanism on how honey has anticancer characteristics is an area of great interest. Honey has been studied in various cancer cell lines for its ability to induce apoptosis, with several mechanisms of action being suggested. This study aims to evaluate the apoptotic activity of the non cytotoxic Sidr Kashmiry honey and its residue of successive fractionation as well as the cytotoxic chloroform-methanol and ethyl acetate fractions against hepatocellular carcinoma cells in vitro. Apoptosis was assessed by DNA fragmentation, diphenyl amine assay, and ultrastructure investigation. Micronuclei test was carried out to assess genotoxicity. Crude honey, residue, ethyl acetate and chloroform-methanol induced apoptosis, however, the residue and ethyl acetate caused high genotoxicity. Non cytotoxic Sidr Kashmiry honey and its cytotoxic chloroform-methanol fraction could be a powerful pro-apoptotic and non-genotoxic anticancer agent.