Novel tetrakis-phthalocyanines bearing pyrimidine derivative: crystal XRD analysis, enzyme inhibition, molecular docking, and anticancer effects.

In this study, the novel 4-(4-Aminopyrimidin-2-ylthio) phthalonitrile (1) as starting material was synthesized and its 3D structure was verified by the single crystal X-ray diffraction experiment. Then, its peripherally tetra-substituted phthalocyanines (2,3) and the methylated derivatives (2a,3a) containing pyrimidine derivative were synthesized. All these newly synthesized compounds were characterized with various spectroscopic methods such as UV-Vis, FT-IR, 1H-NMR, 13C-NMR and MALDI-TOF MS by obtaining satisfactory results. In addition, these novel phthalocyanines effectively inhibited acetylcholinesterase enzyme, with Ki values in the range of 10.43 ± 2.38 to 41.70 ± 9.32 µM. For the related enzyme, the IC50 values were obtained in the range of 11.68 to 44.28 µM. For α-glycosidase enzyme the most effective Ki values of (3a) and (2) were with Ki values of 92.87 ± 10.70 and 95.18 ± 17.83 µM, respectively. Indeed, the most potent phthalocyanines against both enzymes were recorded for the purpose of investigating interaction modes of these complexes in the active site of the target enzyme. The cytotoxicity potential of these phthalocyanines against human breast, colon, and prostate cancers demonstrated that these compounds had normal cytotoxic effects.Communicated by Ramaswamy H. Sarma.

Surgical and histopathologic outcomes of gastrointestinal stromal tumors.

BACKGROUND: Gastrointestinal stromal tumors are encountered more frequent as a result of increased imaging examinations. The purpose of the study is to define the patient profile, histopathologic and treatment outcomes of cases that underwent surgical treatment for neoplasms of the gastrointestinal tract and diagnosed as gastrointestinal stromal tumor. METHODS: The outcomes of 32 patients operated in our department of general surgery for tumors of the gastrointestinal tract and diagnosed as gastrointestinal stromal tumor between January 2014 and December 2019 are evaluated retrospectively from the medical records and hospital treatment registry. RESULTS: Within the study period a total of 32 patients were operated and diagnosed gastrointestinal stromal tumor. There were 19 male (59.4%) and 13 female (40.6) patients and the average age of the patients was 60.2 11.8 years. The average tumor size was 5.95 3.3 centimeters. The tumor localization was mainly the stomach (n=17) and the small bowel (n=11). Distant metastasis was detected in 6 (18.75%) patients, four of them in the liver and two in the peritoneum and omentum. In half of the cases (n=16) there were reactive lymph nodes and 5 (83.3%) of the metastatic patients were within them. CONCLUSION: Gastrointestinal stromal tumors are more frequently encountered by the surgeons with the help of imaging techniques. The primary treatment is surgery and the results are promising. Patients with reactive lymph nodes should be examined for metastasis. Chemotherapy with imatinib can be used for inoperable patients. Patients should be followed up with computed tomography. KEY WORDS: Gastrointestinal System, Histopathology' Stromal Tumor, Surgery.