n-(5-mercapto-1,3,4-thiadiazol-2-yl)-2-phenylacetamide derivatives: synthesis and in-vitro cytotoxicity evaluation as potential anticancer agents

نویسندگان

ahmad mohammadi-farani department of pharmacology, toxicology and medical services, faculty of pharmacy, kermanshah university of medical sciences, kermanshah, iran

neda heidarian department of medicinal chemistry, faculty of pharmacy, kermanshah university of medical sciences, kermanshah, iran

alireza aliabadi department of medicinal chemsitry, faculty of pharmacy, kermanshah university of medical sciences

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.

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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 ...

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عنوان ژورنال:
iranian journal of pharmaceutical research

جلد ۱۳، شماره ۲، صفحات ۴۸۷-۴۹۲

کلمات کلیدی
[ ' s y n t h e s i s ' , 1 , 3 , 4 , ' t h i a d i a z o l e ' , ' a n t i c a n c e r ' , ' a m i d a t i o n ' ]

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