Gastrointestinal stromal tumor (GIST) is a rare stromal neoplasm, which represents the most common mesenchymal tumor of the gastrointestinal tract. It is characterized by indolent clinical symptoms, although it can present as a life-threatening emergency. Here in, we present a case of primary small bowel GIST treated at our department. A 58-year-old male patient presented to our emergency department with a diffuse abdominal pain of acute onset. Patient presented with symptoms and signs of acute intestinal obstruction. Imaging studies revealed a mass at mid ileum, with multiple air fluid levels. Intra-operatively, a mass of 12×9 cm was found at mid ileum on antimesenteric border with 3600 volvulus of adjacent ileum. En bloc resection was performed. Histopathology report was suggestive of gastrointestinal stromal tumor.

Background: According to the latest global cancer data, cancer burden rises to 18.1 million new cases and 9.6 million cancer deaths in 2018. Among that female breast cancer ranks as the fifth leading cause of death (627000 deaths, 6.6%). The main causative factor involved in breast cancer development and progression is the Estrogen Receptor (ER) which is the essential target for anti-cancer drug discovery. Since millennia ER-α has been considered as an oncology mark for the treatment of breast cancer. Methods: A series of novel 6-methyl-3-(3-oxo-1-phenyl-3-(4-(2-(piperidin-1-yl)ethoxy)phenyl)propyl)-2Hchromen- 2-one was designed, synthesized and screened for their anti-breast cancer activity against estrogen receptor-positive MCF-7, ZR-75-1 and negative MDA-MB-435 human breast cancer cell lines. Estrogen level of all the potent cytotoxic compounds were measured on day 30 of intoxication was compared with the control and N-methyl-N-nitrosourea (MNU) group. The docking study was performed to predict binding orientation towards the estrogen receptor-α. Results: Among the synthesized compounds C-3, C-5 and C-15 were showing potent cytotoxicity against estrogen receptor-positive MCF-7. The potent cytotoxic compounds C-3, C-5 and C-15 were further evaluated for in vivo anti-cancer activity by MNU induced mammary carcinoma in female sprague-dawley rats. The in vivo anticancer activity result shows that the compound C-5 has protuberant affinity towards estrogen receptor as standard TAM (Tamoxifen). The docking of the synthesized chromen derivatives showed interaction modes comparable to that of the co-crystallized ligands. Conclusion: The designed class has very promising starting point for the development and further improvement in anti-breast cancer class of drugs.

A series of novel amide functionalized 1H‐benzo[d]imidazole‐2‐thiol derivatives 4 a‐o were prepared from substituted benzimidazole‐2‐thiol 1 a‐c. All the final compounds were screened for antimicrobial, minimum bactericidal concentration (MBC) and anti‐biofilm activities against Gram‐positive and Gram‐negative bacterial strains. Amongst all the synthesized derivatives, compounds 4 c, 4 e, 4 f, 4 g, 4 k and 4 o exhibiting promising antibacterial activity against various bacterial strains were identified. Moreover, the compound 4 c showed highly significant antimicrobial activity (MIC value of 1.9 μg/mL) and broad‐spectrum anti‐biofilm activity which was identified as a potential lead molecule.

Background: Cancer is a complex disease involving genetic and epigenetic alteration that allows cells to escape normal homeostasis. Kinases play a crucial role in signaling pathways that regulates cell functions. Deregulation of kinases leads to a variety of pathological changes, activating cancer cell proliferation and metastases. The molecular mechanism of cancer is complex and dysregulation of tyrosine kinases like anaplastic lymphoma kinase (ALK), Bcr-Abl (Fusion gene found in patient with chronic myelogenous leukemia (CML), JAK (Janus Activated Kinase), Src family kinases (SFKs), ALK (Anaplastic lymphoma Kinase), c-MET (Mesenchymal- Epithelial Transition), EGFR (Epidermal Growth Factor receptor), PDGFR (Platelet Derived Growth Factor Receptor), RET (Rearranged during Transfection), VEGFR (Vascular Endothelial Growth Factor Receptor) play major role in the process of carcinogenesis. Recently kinase inhibitors have overcome many problems of traditional cancer chemotherapy as they effectively separate out normal, non-cancer cells as well as rapidly multiplying cancer cells. <p> Methods: Electronic databases were searched to explore the small molecule tyrosine kinases by polyphenols with the help of docking study (Glide-7.6 program interfaced with Maestro-v11.3 of Schrödinger 2017) to show the binding energies of polyphenols inhibitor with different tyrosin kinases in order to differentiate between the targets. <p> Results: From the literature survey, it was observed that the number of polyphenols derived from natural sources alters the expression and signaling cascade of tyrosine kinase in various tumor models. Therefore, the development of polyphenols as a tyrosin kinase inhibitor against targeted proteins is regarded as an upcoming trend for chemoprevention. <p> Conclusion: In this review, we have discussed about the role of polyphenols as chemoreceptive which will help in future for the development and discovery of novel semisynthetic anticancer agents coupled with polyphenols.

Objective: The aim of the study is to perform a computational study consisting of molecular docking for polyphenols subjected to in silico studies to identify a new lead for antimicrobial activity which has been reported yet or not been used yet. Methods: The Schrödinger Maestro 11.3 performed molecular docking of the enzyme FabH (β-ketoacyl-acyl carrier protein synthase III) (PDB ID: 5BNR) with polyphenol. The targeted compounds were docked against FabH enzyme and also evaluated for MM-GBSA and ADMET analysis. Results: The top hits shows remarkable results and good binding interactions with a pocket of the enzyme. The best binding score are as-8.6 (kcal/mol) of Geniestein,-8.579 (kcal/mol) of 4-naphthoquinone,-7.651(kcal/mol) of Pelargonidin. All the targeted compounds were found in the given limits of ADMET parameters. They also showed good free-binding energy. Conclusion: The computational study reveals that the targeted polyphenols show good binding interactions and are also compatible with ADMET parameters. So, with this, we can conclude that the reported polyphenols can be potent against bacterial infection. In the future, if we derivatized these polyphenols with different substitutions, it can also lead to a potential drug moiety against bacterial infection.