Synthesis and Evaluation of Novel Metacetamol Derivatives with Hydrazone Moiety as Anticancer and Antimicrobial Agents.

By exploiting the wide biological potential of the hydrazone scaffold, a series of hydrazone derivatives were synthesized, starting from N-(3-hydroxyphenyl)acetamide (metacetamol). The structures of the compounds were determined using IR, 1 H and 13 C-NMR, and mass spectroscopic methods. The obtained molecules (3 a-j) were evaluated for their anticancer potential against MDA-MB-231 and MCF-7 breast cancer cell lines. According to the CCK-8 assay, all tested compounds showed moderate to potent anticancer activity. Among them, N-(3-(2-(2-(4-nitrobenzylidene)hydrazinyl)-2-oxoethoxy)phenyl)acetamide (3 e) was found to be the most effective derivative with an IC50 value of 9.89 µM against MDA-MB-231 cell lines. This compound was further tested for its potential effects on the apoptotic pathway. Molecular docking studies was also carried out for 3 e in the colchicine binding pocket of tubulin. Additionally, compound 3 e also demonstrated effective antifungal activity, particularly against Candida krusei (MIC=8 µg/ml), indicating that nitro group at the 4th  position of the phenyl ring was the most preferable substituent for both cytotoxic and antimicrobial activity. Our preliminary findings suggest that compound 3 e could be exploited as a leading structure for further anticancer and antifungal drug development.

Lifestyle Changes and Exacerbation Frequency of COPD in Times of the Pandemic.

OBJECTIVE: The objective of this study is to analyze chronic obstructive pulmonary disease exacerbation rates and the effect of patients' behavioral changes on the exacerbations during the pandemic. MATERIAL AND METHODS: This study was conducted in a reference hospital for chest diseases and patients who were hospitalized with an exacerbation of chronic obstructive pulmonary disease between March 11, 2019, and March 11, 2020, were designated. Patients' chronic obstructive pulmonary disease exacerbations requiring emergency department visits and/or hospitalization were com- pared between the pre-pandemic and pandemic periods. Each patient was surveyed with 25 questions using telemedicine. RESULTS: Of all the 256 patients, 203 (79%) were male and the mean age was 66 ± 10 years. Compared to the previous year, emer- gency department visits and hospitalizations in our hospital were significantly lower and less frequent (P < .0001, for both). Smoking habits decreased in 9% of patients, and 60% had hardly spent time outdoors. Only 3 patients reported to spend time indoors. The household mask-use rate while contacting the patient was 50%. As a chronic obstructive pulmonary disease patient, 33% expressed themselves as "feeling better." Overall, 92(36%) patients were recorded not to have any exacerbation, and 34 (13%) to have no attacks of worsening were managed at home. Novel exacerbation risk was found to independently correlate with younger age (odds ratio: 0.944, CI: 0.904-0.986, P = .010) and having more frequent episodes of exacerbation in the pre-pandemic period (odds ratio: 1.2, CI: 1.025-1.405, P = .023). CONCLUSION: Chronic obstructive pulmonary disease patients specifically benefited from confinements, restrictions, and lifestyle changes. Further studies are needed to better identify the most critical factors leading to these positive outcomes. A permanent patient management guideline for chronic obstructive pulmonary disease patients could be formulated where the weight of lifestyle factors is elevated.

Preliminary study of serum Galectin-1 in breast cancer carcinogenesis [Izmir Oncology Group (IZOG) study].

PURPOSE: Galectin-1 is a lectin involved in the carcinogenesis of many cancers. In the present study, we aimed to investigate the importance of galectin-1 in breast cancer carcinogenesis and its relationship with tumor development. METHODS: Patients who were diagnosed with new breast cancer and a healthy volunteer population were included in the study. Preoperative and postoperative (1 month following visit at the medical oncology outpatient clinic) serum samples were collected from breast cancer patients and the healthy volunteer control group. RESULTS: There was no statistically significant difference between patients' age, height, weight and body mass index (BMI) (p>0.05). The mean galectin-1 value of the preoperative group was 2.16±0.69 ng/ml, in the postoperative group; 1.75±0.31 ng/ml, and the healthy control group 1.64±0.40 ng/ml. A comparison of mean galectin-1 values between the groups showed that the highest galectin-1 level was found in the preoperative patients. When the mean serum galectin-1 levels of preoperative and postoperative patients were compared, a statistically significant difference was found between the two groups (p<0.001). Furthermore, a comparison of the control group and preoperative patients also revealed a statistically significant difference between the groups (p<0.001). When the control group and postoperative patients were compared, no statistically significant difference was found between them (p=0.16). CONCLUSION: Serum galectin-1 levels were higher in breast cancer patients than in the healthy control group. In addition, postoperative galectin-1 levels of breast cancer patients tended to decrease. This suggests that serum galectin-1 levels are important in breast carcinogenesis and positively correlated with the presence of tumors.