Design, synthesis, and evaluation of the anticancer properties of a novel series of carboxamides, sulfonamides, ureas, and thioureas derived from 1,2,4-oxadiazol-3-ylmethyl-piperazin-1-yl substituted with pyrazolo[1,5-a]pyrimidine derivatives
Ajeesh Kumar A.K.,Anthem Biosciences Pvt. Ltd. and 49 |
Nair K.B.,Anthem Biosciences Pvt. Ltd. and 49 |
Bodke Y.D.,Kuvempu University |
Sambasivam G.,Anthem Biosciences Pvt. Ltd. and 49 |
Bhat K.G.,Maratha Mandals Ngh Institute Of Dental Science And Research Center
Monatshefte fur Chemie | Year: 2016
Abstract: A series of novel carboxamides, sulfonamides, ureas, and thioureas derived from 1,2,4-oxadiazol-3-ylmethyl-piperazin-1-yl substituted with pyrazolo[1,5-a]pyrimidine analog were designed and synthesized. The newly synthesized compounds were characterized by 1H NMR, 13C NMR, ESI–MS, and IR and were tested for their in vitro antiproliferative activity by MTT assay. Out of these twenty derivatives, five compounds showed good anticancer activity against HeLa cell line. These are superior with less than 10 µg/cm3 of IC50 when compared to the marketed anticancer drug paclitaxel with 30 µg/cm3 of IC50 against Hela cell line. Graphical abstract: [Figure not available: see fulltext.] © 2016 Springer-Verlag Wien
Kothari S.C.,Gateway Inc. |
Shivarudraiah P.,Anthem Biosciences Pvt. Ltd. and 49 |
Venkataramaiah S.B.,Anthem Biosciences Pvt. Ltd. and 49 |
Gavara S.,Anthem Biosciences Pvt. Ltd. and 49 |
And 2 more authors.
Food and Chemical Toxicology | Year: 2014
In western Cameroon, edible fruits and seeds from the plant Dichrostachys glomerata are commonly used as spices. Extract from the fruit pods has been reported as a good natural source of antioxidants and may provide health benefits. The objective of the present study was to investigate potential adverse effects, if any, of D. glomerata fruit pod extract (Dyglomera™) in a subchronic toxicity study and in genotoxicity studies. In the toxicity study, Sprague Dawley rats (20/sex/group) were gavaged with D. glomerata extract at dose levels of 0, 100, 1000 and 2500. mg/kg body weight (bw)/day for 90-days. Dyglomera™ administration did not result in mortality or show treatmentrelated changes in clinical signs of toxicity, body weights, body weight gain or feed consumption. Similarly, no toxicologically significant treatment-related changes in hematological, clinical chemistry, urine analysis parameters, and organ weights were noted. Macroscopic and microscopic examinations did not reveal treatment-related abnormalities. Mutagenic and clastogenic potentials as evaluated by Ames assay, in vitro and in vivo chromosomal aberration test and in vivo micronucleus test did not reveal any genotoxicity of the extract. The results of subchronic toxicity study supports the no-observed-adverse-effect level (NOAEL) for D. glomerata extract as 2500. mg/kg bw/day, the highest dose tested. © 2014 Elsevier Ltd.
Samant S.,Anthem Biosciences Pvt. Ltd. and 49 |
Gupta G.,Anthem Biosciences Pvt. Ltd. and 49 |
Gupta G.,Apollo Hospitals |
Karthikeyan S.,Anthem Biosciences Pvt. Ltd. and 49 |
And 5 more authors.
Journal of Industrial Microbiology and Biotechnology | Year: 2014
Recombinant proteins can be targeted to the Escherichia coli periplasm by fusing them to signal peptides. The popular pET vectors facilitate fusion of target proteins to the PelB signal. A systematic comparison of the PelB signal with native E. coli signal peptides for recombinant protein expression and periplasmic localization is not reported. We chose the Bacillus stearothermophilus maltogenic amylase (MA), an industrial enzyme widely used in the baking and brewing industry, as a model protein and analyzed the competence of seven, codon-optimized, E. coli signal sequences to translocate MA to the E. coli periplasm compared to PelB. MA fusions to three of the signals facilitated enhanced periplasmic localization of MA compared to the PelB fusion. Interestingly, these three fusions showed greatly improved MA yields and between 18- and 50-fold improved amylase activities compared to the PelB fusion. Previously, non-optimal codon usage in native E. coli signal peptide sequences has been reported to be important for protein stability and activity. Our results suggest that E. coli signal peptides with optimal codon usage could also be beneficial for heterologous protein secretion to the periplasm. Moreover, such fusions could even enhance activity rather than diminish it. This effect, to our knowledge has not been previously documented. In addition, the seven vector platform reported here could also be used as a screen to identify the best signal peptide partner for other recombinant targets of interest. © 2014 Society for Industrial Microbiology and Biotechnology.