Midtgaardrees1877

5% versus 5.6% in normal conditions. The study shows that normal and regenerating SC are under immune surveillance since early tadpole stages, well in advance of metamorphosis when immune cells determine the degeneration of the SC and the complete reabsorption of the tail. VOCs are the major harmful pollutants released from MSW landfills, which are toxicity to human health. #link# In order to in-situ biodegradation of VOCs released from landfill, two novel laboratory-scale biocovers, including waste-char obtained from MSW pyrolysis (WC), and sewage sludge modified the WC (SWC), are used to degradate VOCs. The removal performances of VOCs as well as the bacterial community in the WC and SWC are investigated in a simulated landfill systems with the contrast experiment of a landfill cover soil (LCS) for 60 days. Meanwhile, the adsorption-biodegradation of VOCs model compounds over the LCS, WC, and SWC are also tested in fixed-bed adsorption reactor and in-situ FTIR. The VOCs removal efficiencies by the SWC are maintained above 85% for a long-term, much higher than that of the LCS and WC. The higher removal efficiencies and long-term stability for VOCs degradation in SWC are attributed to a strongly positive synergistic between adsorption and biodegradation that the gaseous VOCs released from MSW is effectively adsorbed by the SWC due to its higher VOCs adsorption capacity, and then the adsorbed-VOCs is converted into CO2 and H2O by the microorganisms that consuming the adsorbed-VOCs as energy and carbon sources. Subsequently, the decrease of the adsorbed-VOCs in SWC would also promote the transformation of the gaseous VOCs into the adsorbed VOCs and accelerate the growth of microorganisms by taking the adsorbed-VOCs as the energy and carbon source, resulted in a higher adsorption rate and degradation rate for VOCs. Using fragment-based design strategy, new pyridyl-indole hybrids 4a-y and indole intermediates 3a-e were synthesized using multicomponent one pot reaction. The synthesized compounds were subjected to screening for antimalarial activity against chloroquine sensitive (D6) and chloroquine resistant (W2) strains of Plasmodium falciparum. Several compounds exhibited antimalarial activity with IC50 values in the range of 1.47-9.23 μM, and 1.16-7.66 μM, for D6 and W2 strains, respectively. Compounds 4a, 4k and 4u showed the highest selectivity index among all the tested compounds (S.I. ranged 3.8-10). Binding interactions between the active antimalarial compounds and the active site of quadruple mutant Plasmodium falciparum dihydrofolate reductase enzyme have been investigated using molecular docking analysis. Benzodiazepines (BZDs) represent a diverse class of bicyclic heterocyclic molecules. In the last few years, benzodiazepines have emerged as potential therapeutic agents. As a result, several mild, efficient and high yielding protocols have been developed that offer access to various functionalized benzodiazepines (BZDs). They are known to possess a wide array of biological activities such as anxiolytic, anticancer, anticonvulsant, antipsychotics, muscle relaxant, anti-tuberculosis, and antimicrobial activities. The fascinating spectrum of biological activities exhibited by BZDs in various fields has prompted the medicinal chemist to design and discover novel benzodiazepine-based analogs as potential therapeutic candidates with the desired biological profile. In this review, an attempt has been made by to summarize (1) Recent advances in the synthetic chemistry of benzodiazepines which enable their synthesis with desired substitution pattern; (2) Medicinal chemistry of BZDs as therapeutic candidates with promising biological profile including insight of mechanistic studies; (3) The correlation of biological data with the structure i.e. structure-activity relationship studies were also included to provide an insight into the rational design of more active agents. Colchicine belongs to a large group of microtubule polymerization inhibitors. Although the anti-cancer activity of colchicine and its derivatives has been established, none of them has found commercial application in cancer treatment due to side effects. Therefore, we designed and synthesized a series of six triple-modified 4-chlorothiocolchicine analogues with amide moieties and one urea derivative. These novel derivatives were tested against several different cancer cell lines (A549, MCF-7, LoVo, LoVo/DX) and primary acute lymphoblastic leukemia (ALL) cells and they showed activity in the nanomolar range. The obtained IC50 values for novel derivatives were lower than those obtained for unmodified colchicine and common anticancer drugs such as doxorubicin and cisplatin. Further studies of colchicine and selected analogues were undertaken to indicate that they induced apoptotic cell death in ALL-5 cells. We also performed in silico studies to predict binding modes of the 4-chlorothiocolchicine derivatives to different β tubulin isotypes. Elafibranor cell line indicate that select triple-modified 4-chlorothiocolchicine derivatives represent highly promising novel cancer chemotherapeutics. In present study, a new series of 4, 7-disubstituted coumarin derivatives (7a-y) have been synthesized as galectin-1 targeting apoptosis inducing agents and evaluated for their in vitro cytotoxic potentials against a panel of selected human cancer cell lines namely, Brest (MCF7), Ovarian (SKOV3), Prostate (PC-3 & DU145) and normal embryonic kidney (HEK293T) cells, using MTT assay. Most of the compounds exhibited potent growth inhibitory action against the treated cancer cell lines with an IC50 range of 10-30 µM. Compound 7q exhibited a significant growth inhibition against prostate cancer (PC-3 & DU145) cell lines with an IC50 value of 7.45 ± 0.03 µM, 8.95 ± 0.17 µM respectively. Further, the target compound 7q was radiolabeled with fluorine-18 [18F] to be used as a novel PET radiotracer for imaging of tumors via targeting galectin-1, using appropriate reaction conditions in the GE Tracer-lab FX2N synthesis module. The purification of the [18F] radiolabeled compound [18F]-7q was successfully achieved with 60% ethanol.