MM-129 as a Novel Inhibitor Targeting PI3K/AKT/mTOR and PD-L1 in Colorectal Cancer

Background and aims: The purpose of the present study was to examine the pharmacodynamics features of MM-129 (1,2,4-triazine derivative) as a novel promising drug candidate against colon cancer. Methods: MM-129 was assessed for antitumor activity through an in vivo study on Cby.Cg-Foxn1nu/cmdb mice. The mechanistic studies investigated cellular affinity of a new 1,2,4-triazine derivative by measuring levels of intracellular/extracellular signal molecules participating in tumorigenesis. Results: The results revealed that MM-129 significantly reduced tumor growth in mice challenged with DLD-1 and HT-29 cells. It exerted the ability to inhibit intracellular molecules promoting tumorigenesis and inducing cell cycle arrest, like Akt, mTOR, and CDK2. Simultaneously, it was able to downregulate PD-L1 expression, which involves immunological self-tolerance. Combined administration of MM-129 and 5-fluorouracil (5-FU) additionally amplified these effects, which were manifest as an increase population of cells in the G0/G1 phase. Conclusions: A novel 1,2,4-triazine derivative with a dual mechanism of antitumor activity—MM-129, may act as a chemosensitizer, overcoming chemoresistance against 5-FU, the first-line agent in the chemotherapy of colon cancer.

Microwave Mediated Synthesis of Novel 1,3,5-Triazine Derivative and their Biological Evaluation

1,3,5-Triazine derivative are synthesized by replacement of chloride ions of Cyanuric chloride and 1,3,5-Triazine derivative are showing promising biologically activity such as Antibacterial, Antifungal, Antimalarial, Antivirus, Anticancer that’s why interest of researches on synthesis of 1,3,5-Triazine derivatives always in focused. The present study reported the synthesis of 2,4,6-Trisubstituted 1,3,5-Triazine derivatives by Microwave mediated Method which gave the desired result in less time with higher yield. The structure of 1,3,5-Triazine derivatives have been elucidated by Spectral of IR, NMR and MASS. The derivative of 1,3,5-Triazine are evaluated for their In vitro Antibacterial activity against Gram Positive and Gram Negative Bacterial species and shown good Antibacterial effect.

The influence of FWA chemical constitution to the whiteness and UV protection of cotton and cotton/polyester blend

It is well known that the optimal concentration of fluorescent whitening agent (FWA) in the bath results in high whiteness of single component textiles. At the same time, due to fluorescence of FWA, the higher UV protection is achieved as well. However, for the textile blends it is not so easy to achieve. Depending on the fabric chemical composition, different FWAs must be applied. Therefore, the influence of FWA chemical constitution to the whiteness and UV protection of cotton and cotton/polyester blend were researched in this paper. For that purpose, cotton and cotton/polyester blended (50%/50%) fabrics was treated with four different FWAs by Huntsman, Uvitex® brand: BHT, RSB, NFW and EBF. Spectral remission before and after FWA treatment was measured on a remission spectrophotometer Spectraflash SF 300, Datacolor. Whiteness degree was calculated according to ISO 105-J02:1997, and the Tint Deviations and its coloristic meanings were determined according to Griesser. The UV protection of cotton and cotton/polyester fabrics treated with FWA was determined according to AS/NZS 4399:2017 using transmission spectrophotometer Cary 50/Solascreen, Varian. Based on the results obtained,the stilbene disulphonic acid triazine derivative (Uvitex® RSB) can be recommended for use on a cotton/polyester blend.