Synthesis of novel carbazole hydrazine-carbothioamide scaffold as potent antioxidant, anticancer and antimicrobial agents.

Background: Carbazole-based molecules containing thiosemicarbazide functional groups are recognized for their diverse biological activities, particularly in enhancing therapeutic anticancer effects through inhibiting crucial pathways. These derivatives also exhibit noteworthy antioxidant properties.

Objectives: This study aims to synthesize, characterize, and evaluate the antioxidant and anticancer activities of 18 novel carbazole derivatives.

Synthesis and biological studies of pyrimidine derivatives targeting metabolic enzymes.

Novel synthesized pyrimidine derivatives were investigated against carbonic anhydrase isoenzymes I and II (hCA I and II), acetylcholinesterase (AChE), butyrylcholinesterase (BChE), α-glycosidase, and aldose reductase (AR) enzymes associated with some common diseases such as epilepsy, glaucoma, Alzheimer's disease, diabetes, and neuropathy. When the results were examined, novel synthesized pyrimidine derivatives were found to have effective inhibition abilities toward the metabolic enzymes. IC values and K values were calculated for each pyrimidine derivative and compared to positive controls.

Hsp Inhibitor is Affective Against Adenocarcinomic Human Alveolar Basal Epithelial Cells Through Modulating ERK/MAPK Signaling Pathway.

The extracellular signal-regulated kinase (ERK) - mitogen-activated protein kinase (MAPK) pathway regulates cell proliferation, differentiation, and apoptosis. Heat Shock Protein 90 (HSP90) is required to activate proto-oncogenic protein kinases and promotes tumor growth through anti-apoptotic effects on A549-non-small cell lung cancer (NSCLC). Therefore, deregulation of the ERK-MAPK pathway and abnormal expression of HSP90 are reasonably frequent events in NSCLC.

Design, synthesis, molecular docking and biological evaluation of new carbazole derivatives as anticancer, and antioxidant agents.

Background: The carbazole skeleton is an important structural motif occurring naturally or synthesized chemically and has antihistaminic, antioxidant, antitumor, antimicrobial, and anti-inflammatory activities.

Objectives: This study aimed to design and synthesize a novel series of carbazole derivatives and evaluate their antiproliferative and antioxidant activities.

Methods: The synthesized compounds were characterized utilizing HRMS, H-, and C-NMR, and assessed for their anticancer, antifibrotic, and antioxidant effects utilizing reference biomedical procedures.

Triad pyrazole-thiazole-coumarin heterocyclic core effectively inhibit HSP and drive cancer cells to apoptosis.

Intensive studies on hepatocellular carcinoma (HCC), which is spreading rapidly around the world and has a high mortality rate, is due to the lack of adequate preventive or curative treatment methods. Treating patients with HCC has become very challenging because of the heterogeneity in the patient population lead activation of different signaling pathways, and pathway crosstalk for patients. Therefore, understanding these molecular mechanisms and combining drugs with molecular therapies to overcome these drawbacks has become an area of utmost importance.

Synthesis, molecular docking, molecular dynamics and evaluation of Drug-Likeness properties of the fused -Formyl pyrazoline substituted new dehydroepiandrosterone derivatives.

The hybrid molecules bearing heterocyclic structures in the A or D rings of steroids have significant biological activity. 16 ()-Hetereoarylidene steroids were synthesized from the reaction of different heteroaromatic carbaldehydes and -Dehydroepiandrosterone (DHEA) in a basic medium. Then, synthesis of the -formyl pyrazoline substituted new DHEA derivatives were carried out from the reaction of hydrazine hydrate and 16 ()-hetereoarylidene steroids.

Discovery of sulfadrug-pyrrole conjugates as carbonic anhydrase and acetylcholinesterase inhibitors.

Human carbonic anhydrase (hCA) isoenzymes are zinc ion-containing, widespread metalloenzymes and they classically play a role in pH homeostasis maintenance. CA inhibitors suppress the CA activity and their usage has been clinically established as antiglaucoma agents, antiepileptics, diuretics, and in some other disorders. Alzheimer's disease (AD) is a slowly progressive neurodegenerative disorder and a fatal disease of the brain.

Synthesis, dielectric properties, molecular docking and ADME studies of pyrrole-3-ones.

A novel series of pyrrole-3-one derivatives were synthesized using furan-3-one derivatives and various aromatic amines. The synthesized compounds were identified by spectral studies such as IR, NMR and HRMS. Dielectric properties of the target compounds were experimentally determined by dielectric spectroscopy in the frequency range of 20 Hz - 1 MHz.

Designing Specific HSP70 Substrate Binding Domain Inhibitor for Perturbing Protein Folding Pathways to Inhibit Cancer Mechanism.

Background: HSP70 is a survival factor for tumor cells in transformation and in tumor progression as well as in anti-apoptotic response.

Objective: Several inhibitors targeting HSP70 ATPase function displayed off-target effects, but PES, which targets the HSP70 substrate binding domain, prevents tumor cell survival prominently. However, PES may not bind HSP70 in the absence of nucleotide.

The Prevalence of Sarcopenia in Bipolar Disorder.

Background: Sarcopenia (SP) is a syndrome described as generalized and progressive loss of muscle mass and strength that may cause fall, fractures, disability and death. Oxidative stress might be a probable etiologic factor in SP as well. SP is a comorbid syndrome that is seen in chronic illnesses.

The Comparison of the Biological Rhythms of Patients with Fibromyalgia Syndrome with Biological Rhythms of Healthy Controls.

BACKGROUND Fibromyalgia syndrome (FMS) is a rheumatic disease characterized by diffuse body pain and decreased muscle function. The aim of the present study was to compare the biological rhythms of patients with fibromyalgia syndrome with the biological rhythms of healthy controls. MATERIAL AND METHODS This was a cross-sectional, single blind, and single center case-control study.

Recent advances of thiazole hybrids in biological applications.

Thiazoles have attracted much synthetic interest due to their wide variety of biological properties and are important members of heterocyclic compounds. In recent years, studies on the synthesis of thiazole compounds have been increasing because of the properties of this core. In particular, the hybrid structures in which the thiazole ring and the other nuclei are linked have gained popularity.

Design, Synthesis, and Evaluation of Heat Shock Protein 90 Inhibitors in Human Breast Cancer and Its Metastasis.

Background: Despite development of novel cancer drugs, invasive ductal breast carcinoma and its metastasis are still highly morbid. Therefore, new therapeutic approaches are being developed and Hsp90 is an important target for drug design. For this purpose, a series of benzodiazepine derivatives were designed and synthesized as novel Hsp90 inhibitor.

Design and synthesis of pyrimidinyl acyl thioureas as novel Hsp90 inhibitors in invasive ductal breast cancer and its bone metastasis.

Invasive ductal carcinoma is the most common breast malignancies tumors and has tendency to bone metastases. Many oncogenic client proteins involved in formation of metastatic pathways. Stabilization, regulation, and maintenance of these oncogenic client proteins are provided with Heat Shock Protein 90 (Hsp90).

The evaluation in terms of sarcopenia of patients with fibromyalgia syndrome.

Background: Fibromyalgia syndrome (FMS) is an extra-articular rheumatic illness, characterized by widespread body pain and decreased muscle function. Generalized loss of muscle mass and strength is named as sarcopenia. The objective of this study was to evaluate patients with FMS regarding sarcopenia.

A Novel Approach to Inhibit Heat Shock Response as Anticancer Strategy by Coumarine Compounds Containing Thiazole Skeleton.

Inhibition of the Hsp90 function is an essential therapeutic approach and several inhibitors were designed as anti-cancer agents. These inhibitors are ATPases and they aim to deregulate Hsp90 folding function. ATPase proteins are common in human metabolism but they form nonspecific targets.

Evaluation of open and closed kinetic chain exercises in rehabilitation following anterior cruciate ligament reconstruction.

[Purpose] To compare outcomes of anterior cruciate ligament (ACL) reconstruction after open kinetic chain (OKC) exercises and closed kinetic chain (CKC) exercises. [Subjects and Methods] The subjects comprised 11 female and 47 male patients who are randomly divided into two groups: which performed a CKC exercise program Group I and Group II which performed an OKC exercise program. Pain intensity was evaluated using visual analogue scale (VAS).

Effectiveness of a home exercise program in combination with ultrasound therapy for temporomandibular joint disorders.

[Purpose] This study compared the effectiveness of home exercise alone versus home exercise combined with ultrasound for patients with temporomandibular joint disorders. [Subjects and Methods] This study enrolled 23 female and 15 male patients who were divided randomly into two groups. The home exercise group performed a home exercise program consisting of an exercise program and patient education, and the home exercise combined with ultrasound group received ultrasound therapy in addition to the home exercise program.

Relationship among Ocular Diseases, Developmental Levels, and Clinical Characteristics of Children with Diplegic Cerebral Palsy.

[Purpose] The aim of this study was to evaluate the relationships among vision problems, developmental levels, upper extremity functions, and qualities of life of children with cerebral palsy (CP). [Subjects] The study included 32 children, aged 4-15 years, diagnosed with diplegic type CP. [Methods] Hand function was evaluated using the Manual Ability Classification System (MACS) and the Bimanual Fine Motor Function (BFMF) scale, and the severity of CP was assessed using the Gross Motor Function Classification System (GMFCS).

Is There Any Relationship between Joint Destruction and Carotid Intima-media Thickness in Patients with Rheumatoid Arthritis?

[Purpose] The purpose of this study was to investigate the possible relationship between joint destruction and carotid intima-media thickness in patients with rheumatoid arthritis. [Subjects and Methods] Thirty-four RA patients and 31 healthy controls were enrolled in this study. The disease activity for 28 joints was recorded for each patient using the erythrocyte sedimentation rate (DAS28ESR), a visual analog scale (VAS0-10 cm), and a disability index, the health assessment questionnaire (HAQ).

The Relationship between Quadriceps Thickness, Radiological Staging, and Clinical Parameters in Knee Osteoarthritis.

[Purpose] The aim of this study was to investigate the relationship between clinical parameters, radiological staging and evaluated ultrasound results of quadriceps muscle thickness in knee osteoarthritis. [Subjects] The current study comprised 75 patients (51 female, 24 male) with a mean age of 57.9±5.

Changes in spastic muscle stiffness after botulinum toxin A injections as part of rehabilitation therapy in patients with spastic cerebral palsy.

Objective: To investigate changes in stiffness in the gastrocnemius (GCM) muscle following rehabilitation therapy and botulinum toxin type A (BTX-A) injections in patients with spastic cerebral palsy (CP).

Methods: The study included 16 children with spastic CP (Group 1) and 17 healthy children (Group 2). The children with CP received BTX-A injections and underwent rehabilitation therapy.

Adductor longus muscle metastasis of transitional cell carcinoma of the urinary bladder.

Bladder cancer most commonly spreads to the lymph nodes, lungs, bones and adrenal glands. Metastasis of bladder cancer to the skeletal muscle is extremely rare, as is the case in other malignancies. We report a case of a 62-year-old male patient who presented with pain and swelling in the right lower extremity and had difficulty walking, and who was later found to have metastasis in the adductor longus muscle 3 months after the initial diagnosis of transitional cell carcinoma of the urinary bladder.