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Nowadays there are several limitations in cancer treatment. One of these is the use of conventional medicines which not only target cancer cells and thus also cause high toxicity precluding effective treatment. Recent elucidation of mechanisms that cause cancer has led to discovery of novel key molecules and pathways which have have become successful targets for the treatments that eliminate only cancer cells. These so-called targeted therapies offer new hope for millions of cancer patients, as briefly reveiwed here focusing on different types of agents, like PARP, CDK, tyrosine kinase, farnysyl transferase and proteasome inhibitors, monoclonal antibodies and antiangiogenic agents.

In the light of these findings, 5-chloro-1H-indole-2,3-dione 3-thiosemicarbazone derivatives were synthesized in order to obtain more potent and less toxic compounds. The structures of the ABSTRACT: A series of 5-chloro-1H-indole-2,3-dione 3-thiosemicarbazones 3a-g were synthesized to investigate the chemotherapeutic activities. The structures of 3a-g were confirmed by the spectral data (IR, 1 H NMR, 13 C NMR-APT, 13 C NMR-DEPT, HSQC, HMBC) and elemental analysis. Anticancer activities of the compounds were evaluated using cell kinetic parameters on HeLa cells derived from human cervix carcinoma. The preliminary screening results indicated that alkyl substituted compounds 3a, 3b and 3d were more effective in mitosis phase when compared to the synthesis phase. 3a-g were tested against some DNA and RNA viruses in CRFK, HeLa, HEL, MDCK and Vero cells. None of the compounds was active against any of the RNA or DNA viruses at 100 μM. All compounds were also evaluated for antimicrobial activity against selected strains. Methyl substituted 3a and allyl substituted 3c were found to be active against S. aureus and C. albicans.

In the present study, the in vitro cytotoxic effect of a novel transforming growth factor-β receptor inhibitor, LY2109761, was investigated in the human cervix carcinoma HeLa cell lines. For the purpose of the present study, cell index values obtained using the xCELLigence Real-Time Cell Analysis DP instrument, and mitotic, labelling and apoptotic index analysis were used. The results of the present study indicated that LY2109761 affected the cytoskeleton of HeLa cells, decreased the mitotic and labelling index values of the HeLa cell line, and increased the apoptotic index values. Significant differences were observed between the control group which was not treated with LY2109761 and the experimental groups, which were treated with LY2109761 (P<0.01). The results of the present study suggest that LY2109761 may serve as a promising treatment option for cervix carcinoma.