Serpin Peptide 16

Prostate cancer is one of the most prevalent cancers in men leading to second most death causing cancer in men. Despite the availability of multiple treatment still the prevalence is high for prostate cancer. Steroidal antagonists associated with poor bioavailability, side effects while non-steroidal antagonists show serious side effects like gynecomastia. Therefore, there is a need of potential candidate for the treatment of prostate cancer with better bioavailability, good therapeutic effect and minimal side effects. In the same context, we have designed the series, SP1-SP25 based 3-phenyl-5-styryl-1,2,4-oxadiazole as the core structure. We successfully synthesized all 25 molecules in this series and characterized them using ¹H, ¹³C NMR, and mass spectroscopy. Subsequently, we conducted MTT assays using PC-3 cells and observed that all the compounds exhibited a dose-dependent decrease in cell viability. Notably, compounds SP04, SP16, and SP19 demonstrated a significant decrease in cell viability and exhibited potent activity compared to the other synthesized molecules and standard drug bicalutamide. Among them, SP04 emerged as the one of the most potent compounds with an IC₅₀ value of 238.13 nM and an 89.99 % inhibition of PC-3 cells, compared to synthesized molecules and standard drug bicalutamide. Furthermore, we conducted ROS assays and androgen receptor inhibition assays using the potent compound SP04 and bicalutamide. The results indicated that SP04 increased ROS production and decreased androgen receptor expression dose-dependent manner. Additionally, we conducted a docking study to analyse the interaction patterns within the active site of the androgen receptor. ADMET analysis revealed that all the compounds exhibited favorable physicochemical properties and manageable toxicity profiles.

The results of a study of the physicochem. and photomech. properties of mixed Langmuir monolayers based on palmitoyloleoylphosphatidylcholine (POPC), dipalmitoylphosphatidylcholine (DPPC) and amphiphilic spirocompounds are presented.For the first time mixed monolayers based on POPC, DPPC, spiropyran 1',3'-dihydro-1'-hexadecyl-3'3'-dimethyl-6-nitrospiro[2H-benzopyran-2,2'-(2H)indole] and spironaphtoxazine 3,3-dimethyl-1-hexadecyl-1,3-dihydrospiro[indoline-2,3'-naphtho[2,1-b][1,4]oxazine]-9'-ol were formed in various combinations and ratios, and their comparative study was carried out.It has been established that binary mixture of phospholipids and spiro compounds form stable monolayers in which phase transitions can be controlled by UV-light.It has been shown that irradiation of monomol. phosphatidylcholine films containing small amounts of photosensitive compounds (up to 10% by weight) makes it possible to turn them into a liquid-condensed state at pressures above 10 mN/m.The results obtained open broad prospects for using photochromic spirocompounds to control the permeability of biol. membranes using light stimuli.