ABSTRACT
In the recent years, the role of LOX enzymes in the origin of neoplastic diseases such as colorectal, skin, pancreatic and renal cancers has been confirmed. A new series of 1,3,4-thiadiazole derivatives bearing 2-pyridyl moiety was synthesized and the cytotoxicity of the members of this series was assessed using MTT protocol. Enzyme inhibitory activity of the prepared compounds was also tested against 15-lipoxygenase-1 as a novel target for the discovery of anticancer drugs. PC3, HT29 and SKNMC cell lines were utilized and the obtained results were compared with doxorubicin. Overall, nitro containing derivatives exerted a higher cytotoxic activity against PC3 cell line and methoxylated derivatives showed an acceptable activity against SKNMC cell line. Methoxylated derivatives were also the most potent enzyme inhibitors especially at position ortho of the phenyl residue
ABSTRACT
A new series of A-[5-Mercapto-1.3.4-thiadiazol-2-yl]-2-phenylacetamide derivatives [3a-3j] were synthesized via an amidation reaction using EDC and HOBt in acetonitrile solvent at room temperature condition. Chemical structures were characterized by [1]H NMR, IR and MS spectroscopic methods and related melting points were also determined. The anticancer activity was evaluated using MTT procedure in-vitro. All compounds were tested against SKNMC [Neuroblastoma], HT-29 [Colon cancer] and PC3 [Prostate cancer] cell lines. According to the toxicological data, none of the synthesized derivatives exerted superior activity than doxorubicin as reference drug. Derivatives with Ortho chlorine [compound 3d], meta methoxy [compound 3h] and meta fluorine [compound 3b] substituents on the phenyl ring exhibited the best cytotoxic activity against SKNMC [IC[50] = 4.5 +/- 0.035 microM], HT-29 [IC[50] = 3.1 +/- 0.030 microM] and PC3 [IC[50] - 12.6 +/- 0.302 microM] cell lines respectively
ABSTRACT
Cancer is the second leading cause of death in the world. Despite advances in the diagnosis and treatment, overall survival of patients still remains poor. Hence, there is an urgent need for development of new anticancer agents. Considering promising biological activity of 1,3,4-thiadiazole derivatives, in the present study, synthesis and cytotoxicity assessment of new derivatives of this ring was done. All synthesized compounds were characterized by NMR, IR and MS spectroscopic methods. Obtained data from MTT assay showed that all compounds 3a-31 had better anticancer activity against MDA [breast cancer] compared to PC3[prostate cancer] and U87 [Glioblastoma]. Compound 3 g with /w-OCH[3] moiety on the phenyl ring was the most potent one in this series with IC[50] = 9 microM against MDA breast cell line in comparison with imatinib [IC[50] = 20 microM] as reference drug
ABSTRACT
Cancer is a major global problem and is the second leading cause of mortality in the developed countries.Resistance to current chemotherapeutics and high incidence of adverse effects are the two principal reasons for developing new anticancer agents. Phenylacetamide derivatives can act as potential anticancer agents. Synthesis and screening of 2-[4-Fluorophenyl]-N-phenylacetamide derivatives in present study showed that these compounds act as potent anticancer agents especially against PC3[prostate carcinoma] cell line. Compounds 2a-2c with nitro moiety demonstrated a higher cytotoxic effect than compounds 2d-2f with methoxy moiety. All compounds in this series exhibited lower activity than imatinib as reference drug. Compounds 2b [IC[50] = 52 micro M] and 2c [IC[50] = 80 micro M] were the most active compounds against PC3 cell line in comparison with imatinib[IC[50] = 40 micro M]. Compound 2c [IC[50] = 100 micro M] with p-nitro substituent was the most active compound compared to imatinib[IC[50] = 98 micro M] in MCF-7 cell line