Synthesis and anticancer activity of novel hydrazone linkage-based aryl sulfonate derivatives as apoptosis inducers

نویسندگان

چکیده

In the present study, various 28 hybrid molecules containing hydrazone and sulfonate moieties were synthesized characterized by FTIR, 1H-NMR, 13C-NMR spectroscopy LC-MS spectrometry, besides elemental analysis. The compounds evaluated for their antiproliferative effects against six cancer cell lines, namely A549 (non-small lung cancer), MCF-7 (breast HT-29 (colorectal adenocarcinoma PC-3 (androgen-independent prostate adenocarcinoma), Hep3B (hepatocellular carcinoma HeLa (epitheloid cervix cancer). Among all target compounds, 4g 4h exhibited more promising on lines (IC50 = 17.8 μM 21.2 μM, respectively) with high selectivity. Further mechanistic studies proposed that induced apoptosis is mediated through intrinsic apoptotic pathway changes in mitochondrial membrane potential finally activating caspase-9 caspase-3. results have been encouraging enough to merit further investigation.

برای دانلود باید عضویت طلایی داشته باشید

برای دانلود متن کامل این مقاله و بیش از 32 میلیون مقاله دیگر ابتدا ثبت نام کنید

اگر عضو سایت هستید لطفا وارد حساب کاربری خود شوید

منابع مشابه

Synthesis and anticancer activity assay of novel chalcone sulfonamide derivatives

Chalcones, or 1,3–diaryl–2–propen–1–ones, one of the major classes of natural products and posses many useful properties like anticancer, antibacterial, antifungal, anti–inflammatory, antimalarial and anti–diabetic activity. We report in this communication the synthesis and anticancer study of a number of novel chalcone sulfonamides. Our results indicate that the synthesis of chalcone sulfonami...

متن کامل

Synthesis and anticancer activity assay of novel chalcone sulfonamide derivatives

Chalcones, or 1,3–diaryl–2–propen–1–ones, one of the major classes of natural products and posses many useful properties like anticancer, antibacterial, antifungal, anti–inflammatory, antimalarial and anti–diabetic activity. We report in this communication the synthesis and anticancer study of a number of novel chalcone sulfonamides. Our results indicate that the synthesis of chalcone sulfonami...

متن کامل

Synthesis, Antiplatelet Activity and Cytotoxicity Assessment of Indole-Based Hydrazone Derivatives

A series of indole-based aryl(aroyl)hydrazone analogs of antiplatelet indole-3-carboxaldehyde phenylhydrazone were synthesized by the Schiff base formation reaction and their antiplatelet activity was assessed using human platelet rich plasma. The platelet concentrate was obtained using a two-step centrifugation protocol and ADP, arachidonic acid and collagen were used as inducers of platelet a...

متن کامل

Synthesis, Antiplatelet Activity and Cytotoxicity Assessment of Indole-Based Hydrazone Derivatives

A series of indole-based aryl(aroyl)hydrazone analogs of antiplatelet indole-3-carboxaldehyde phenylhydrazone were synthesized by the Schiff base formation reaction and their antiplatelet activity was assessed using human platelet rich plasma. The platelet concentrate was obtained using a two-step centrifugation protocol and ADP, arachidonic acid and collagen were used as inducers of platelet a...

متن کامل

Novel Approach Synthesis, Molecular Docking and Cytotoxic Activity Evaluation of N-phenyl-2,2-dichloroacetamide Derivatives as Anticancer Agents

Dichloroacetate (DCA) as a small, cheap and available anticancer agent, is a pyruvate mimetic compound that stimulates the activity of pyruvate dehydrogenase (PDH) enzyme through inhibition of pyruvate dehydrogenase kinases (PDHK1-4). DCA turns on programed cell death (apoptosis) which suppressed in tumor cells and therefore inhibits tumor growth. DCA also interferes with the glucose uses of ca...

متن کامل

ذخیره در منابع من


  با ذخیره ی این منبع در منابع من، دسترسی به آن را برای استفاده های بعدی آسان تر کنید

ژورنال

عنوان ژورنال: Medicinal Chemistry Research

سال: 2022

ISSN: ['1554-8120', '1054-2523']

DOI: https://doi.org/10.1007/s00044-021-02837-z