Synthesis and Cytotoxicity Evaluation of N-(۵-(Substituted-benzylthio)-۱,۳,۴-thiadiazole-۲-yl)-۲-p-nitrophenylacetamide Derivatives as Potential Anticancer Agents

Cancer is a big global problem and is one of the top and main causes of mortality in developed countries. Many of the current treatments and anticancer therapeutics have problems with severe side effects and on the other hand, the drug resistance is also another obstacle in the cancer chemotherapy. Hence, there is a strong demand for the discovery and development of effective new antineoplastic therapies. According to the in vitro effectiveness of ۱,۳,۴-thiadiazole based compounds as anticancer agents, new ۱,۳,۴-thiadiazole based derivatives with various electron withdrawing and electron donating moieties were synthesized and tested by MTT assay against three cancerous cell lines. PC۳ (Prostate cancer), U۸۷-C-۵۳۱ (Glioblastoma) and MDA-MB-۲۳۱ (Breast cancer) cell lines were applied for MTT assay and obtained results were compared to imatinib. Study of the structure activity relationship of prepared compounds showed electron withdrawing substituents such as Cl, F and NO۲ enhanced the anticancer properties compared to compound without any substituent (compound ۳l) or compounds with electron donating (methoxy) substituent (compounds ۳j and ۳k). Totally, compound ۳a (IC۵۰ = ۱۰.۶ µM) showed superior activity against PC۳ cell line and compounds ۳d  (IC۵۰ = ۱۰.۳ µM), ۳h (IC۵۰ = ۱۲.۵ µM) and ۳j (IC۵۰ = ۱۱.۳ µM) exhibited higher activity against MDA-MB-۲۳۱ cell line compared to imatinib as reference drug.

کلیدواژه ها:

Synthesis ، ۱ ، ۳ ، ۴-Thiadiazole ، MTT ، Anticancer