Tenidap

Arylmethylene derivatives, chromenes and aminothiophenes were synthesized from 2‐cyano‐N‐(4‐(3‐(thiophen‐2‐yl)acryloyl)phenyl)acetamide 2. The anticancer activity of most synthetic compounds was assessed in breast cancer (MCF‐7), hepatocellular carcinoma (HepG‐2) and cervical cancer (HeLa), with five of arylmethylene and chromene derivatives showing highest cytotoxic activity. Further, treatment of breast cancer (MCF‐7) cell lines with 4 d and 6 b, the most cytotoxic compounds; revealed down regulation for ERK‐2 protein with expression concentration; 527.7±6.61 and 427.7±8.39 pg/ml, respectively compared to staurosporine; 440.9±5.02 pg/ml. Moreover, cell death induction was assessed by Annexin V‐ FITC/PI assay and these compounds caused cell death by apoptosis, besides the DNA fragmentation was assessed by gel electrophoresis and ELISA and the data showed increase in the percentage of fragmentation in treated MCF‐7 of values; 30.49 % and 28.19 % in 4 d and 6 b, respectively confirming the same effect as staurosporine. The DNA‐flow cytometric cell cycle analysis showed that 4 d and 4 g arrested the cell cycle at S phase and 8 b arrested it at G1/S phase. Molecular docking was carried out together with physicochemical properties prediction using DruLiTo program.

Despite the fact that the oxindole has long been thought to be the best structural scaffold, research shows that oxindole derivatives are being studied the least against tuberculosis (TB), a historically airborne illness.The present research focuses on the development of 3-substituted-2-oxindole derivatives with a combination of structural and functional alterations in order to create dual-active new chem. entities with anti-TB, anti-oxidant, and radical-scavenging properties.The physicochem. properties of these compounds are in line with the theories of Lipinski, Veeber, and Leeson.SWISSADME was used to assess the drug-like mol. nature and pharmacokinetics features.Multistep synthetic procedures were used to synthesize the chems.Based on in vitro anti-TB and radical scavenging property analyses, the synthesized 3-substituted-2-oxindole derivatives were confirmed as dual-active compoundsThe synthesized 3-substituted-2-oxindole derivatives were confirmed to possess the dual therapeutics action.The discovery of radical scavengers 4d, 4a, 4c, 3d, 3c, 3f, 3e, 3h, 3g, and 3j that are more potent than Ascorbic acid, the standardThe mols., 3c, 3j, 3b, and 4b have exhibited moderate to active anti-TB properties with a % reduction values of 46.42%, 40.89%, 39.76% and 39.32%, resp.The findings suggest that fine-tuning mols. might result in compounds with better anti-TB and radical-scavenging properties.