Organo NHC catalyzed aqueous synthesis of 4β-isoxazole-podophyllotoxins: anticancer, caspase activation, tubulin polymerization inhibition and molecular docking studies.

We present, for the first time, the organo--heterocyclic carbene (NHC) catalyzed 1,3-dipolar cycloaddition of 4β--propargyl podophyllotoxin (1) with aromatic nitrile oxides to afford regioselective 4β-isoxazolepodophyllotoxin hybrids (6a-n) in benign aqueous-organic media. Preliminary anticancer activity results showed that compound 6e displayed superior activity against MCF-7, HeLa and MIA PaCa2 human cell lines compared with podophyllotoxin. Compounds 6j and 6n showed greater activity against the MCF-7 cell line than the positive control.

Synthesis of 1,2,3-triazole-piperazin-benzo[][1,4]thiazine 1,1-dioxides: antibacterial, hemolytic and TLR4 protein inhibitory activities.

In this study, we designed and synthesized a number of novel 1,2,3-triazole-piperazin-benzo[][1,4]thiazine 1,1-dioxide derivatives and investigated their antibacterial and hemolytic activity. When compared to the lead chemical, dicloxacillin, the majority of the compounds demonstrated acceptable activity. Among them, the most promising compounds 6e, 6g, 6i, 8d, and 8e exhibited excellent antibacterial activity against the methicillin-susceptible (MSSA), methicillin-resistant (MRSA), and vancomycin-resistant (VRSA) with MIC values of 1.

Antiproliferative, molecular docking, and bioavailability studies of diarylheptanoids isolated from stem bark of Rox B.

Diarylheptanoids are a major class of plant secondary metabolites characterized by 1, 7-diphenyl heptanes in a seven-member carbon frame. In the present study, diarylheptanoids (garuganins 1, 3, 4 and 5) isolated from stem bark were evaluated for cytotoxic activity against MCF-7 and HCT15 cancer cell lines. Among the tested compounds, garuganin and exhibited the highest cytotoxic activity against HCT15 and MCF-7 with IC 2.

Antimicrobial Activities of Salacia oblonga Wall Leaf and Root Extracts Against Different Bacterial Strains and Fungal Isolates.

Antibiotic resistance and the hazardous nature of synthetic drugs is threatening issue in the health sector. The alternative for this problem is to focus on plants that attribute to various compounds that exhibit therapeutic properties. Therefore, the study aims to evaluate the antimicrobial efficacy of Salacia oblonga leaf and root extracts against tested human pathogens.

Fused benzo[1,3]thiazine-1,2,3-triazole hybrids: Microwave-assisted one-pot synthesis, in vitro antibacterial, antibiofilm, and in silico ADME studies.

In this paper, we report an efficient one-pot three-component reaction sequences comprising Cu(I)-catalyzed 1,3-dipolar cycloaddition (CuAAC) followed by Cu-catalyzed arylation of resulting 1,2,3-triazole in the presence of ionic liquid [Emim]BF under microwave conditions involving. The newly synthesized derivatives were screened for in vitro antibacterial inhibition potency against both gram +ve and gram -ve strains. Among the tested compounds, 4f exhibited significant inhibition activity with MIC value 3.

Association of mitochondrial displacement loop polymorphisms with risk of colorectal cancer in south Indian population.

Mitochondrial displacement loop (D-loop) is the hot spot for mitochondrial DNA (mtDNA) alterations which influence the generation of cellular reactive oxygen species. In the present study, we sequenced the entire mitochondrial D-loop region (1124 bp) of colorectal cancer (CRC) patients (n = 174) and controls (n = 170) of south Indian origin to identify significant mutations/polymorphisms. Our results showed 152 polymorphisms in the D-loop region of patients and/or controls.

Synthesis, anti-inflammatory, bactericidal activities and docking studies of novel 1,2,3-triazoles derived from ibuprofen using click chemistry.

Background: Nonsteroidal anti-inflammatory drugs are of vast therapeutic benefit in the treatment of different types of inflammatory conditions. 1,2,3-Triazoles and their derivatives have a wide range of applications as anti-bacterial, anti-fungal, anti-tubercular, cytostatic, anti-HIV, anti-allergic, anti-neoplastic and anti-inflammatory (AI) agents. Considering the individual biological and medicinal importance of ibuprofen and 1,2,3-triazoles, we wanted to explore novel chemical entities based on ibuprofen and triazole moieties towards their biological significance.

Mitochondrial control region alterations and breast cancer risk: a study in South Indian population.

Background: Mitochondrial displacement loop (D-loop) is the hot spot for mitochondrial DNA (mtDNA) alterations which influence the generation of cellular reactive oxygen species (ROS). Association of D-loop alterations with breast cancer has been reported in few ethnic groups; however none of the reports were documented from Indian subcontinent.

Methodology: We screened the entire mitochondrial D-loop region (1124 bp) of breast cancer patients (n = 213) and controls (n = 207) of south Indian origin by PCR-sequencing analysis.