n-(5-mercapto-1,3,4-thiadiazol-2-yl)-2-phenylacetamide derivatives: synthesis and in-vitro cytotoxicity evaluation as potential anticancer agents
نویسندگان
چکیده
a new series of n-(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 1h 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 (ic50 = 4.5 ± 0.035 µm), ht-29 (ic50 = 3.1 ± 0.030 µm) and pc3 (ic50 = 12.6 ± 0.302 µm) cell lines respectively.
منابع مشابه
N-(5-Mercapto-1,3,4-Thiadiazol-2-yl)-2-Phenylacetamide Derivatives: Synthesis and In-vitro Cytotoxicity Evaluation as Potential Anticancer Agents
A new series of N-(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 1H NMR, IR and MS spectroscopic methods and related melting points were also determined. The anticancer activity was evaluated using MTT procedure ...
متن کاملN-(5-Mercapto-1,3,4-Thiadiazol-2-yl)-2-Phenylacetamide Derivatives: Synthesis and In-vitro Cytotoxicity Evaluation as Potential Anticancer Agents
A new series of N-(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 1H NMR, IR and MS spectroscopic methods and related melting points were also determined. The anticancer activity was evaluated using MTT procedure ...
متن کاملN-(5-Mercapto-1,3,4-Thiadiazol-2-yl)-2-Phenylacetamide Derivatives: Synthesis and In-vitro Cytotoxicity Evaluation as Potential Anticancer Agents
A new series of N-(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 procedur...
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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...
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عنوان ژورنال:
iranian journal of pharmaceutical researchجلد ۱۳، شماره ۲، صفحات ۴۸۷-۴۹۲
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