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Baburaj T.,Anthem Biosciences Pvt. Ltd | Thambidurai S.,Alagappa University
Synlett | Year: 2011

β-Boc-protected aryl and alkyl hydrazines, useful intermediates for azapeptides and N-substituted pyrazoles, were synthesized by electrophylic amination methodology, using less energetic N-Boc-O-tosyl hydroxylamine as an efficient nitrogen source. Also we have demonstrated a two-step, chromatography-free synthesis of N-Boc-O-tosyl hydroxylamine. © Georg Thieme Verlag Stuttgart - New York. Source


Eswaran S.,Anthem Biosciences Pvt. Ltd | Adhikari A.V.,National Institute of Technology Karnataka | Ajay Kumar R.,Rajiv Gandhi Center for Biotechnology Trivandrum
European Journal of Medicinal Chemistry | Year: 2010

A new class of fused oxazoloquinoline derivatives was synthesized starting from 2-bromo-1-phenylethanones 1a-b through multi-step reactions. The newly synthesized compounds were evaluated for their in vitro antibacterial against Escherichia coli (ATTC-25922), Staphylococcus aureus (ATTC-25923), Pseudomonas aeruginosa (ATCC-27853) and Klebsiella pneumoniae (recultured) and antituberculosis activity against Mycobacterium tuberculosis H37Rv (ATCC 27294). Preliminary results indicated that most of the compounds demonstrated very good antibacterial and antituberculosis activities which are comparable with the first line drugs. Compounds 6a, 6c, 6g, 6j, 6k and 6n emerged as the lead antitubercular agents with MIC, 1 μg/mL and 99% bacterial inhibition while eight compounds, viz., 5a, 15k, 6a, 6c, 6g, 6j, 6k and 6n were found to be more potent than INH (MIC: 1.5 μg/mL) with MIC 1 μg/mL. © 2009 Elsevier Masson SAS. All rights reserved. Source


Eswaran S.,Anthem Biosciences Pvt. Ltd | Adhikari A.V.,National Institute of Technology Karnataka
Bioorganic and Medicinal Chemistry Letters | Year: 2010

A series of 26 new quinoline derivatives carrying active pharmacophores has been synthesized and evaluated for their in vitro antituberculosis activity against Mycobacterium tuberculosis H37Rv (MTB), Mycobacterium smegmatis (MC2), and Mycobacterium fortuitum following the broth micro dilution assay method. Compounds 13e, 13i, 13k, 14a, 14c, 14i, and 14k exhibited significant minimum inhibition concentrations, when compared with first line drugs isoniazid (INH) and rifampicin (RIF) and could be ideally suited for further modifications to obtain more efficacious compounds in the fight against multi-drug resistant tuberculosis. © 2009 Elsevier Ltd. All rights reserved. Source


Baburaj T.,Anthem Biosciences Pvt. Ltd | Thambidurai S.,Alagappa University
Tetrahedron Letters | Year: 2012

Terminal tert-butyloxycarbonyl (Boc) protected hydrazino acids, useful intermediates for modified peptides and biologically active heterocyclic derivatives, were synthesized by electrophilic amination methodology using N-Boc-O-tosyl hydroxylamine as an efficient NH-Boc transfer reagent. Also, we have demonstrated the conversion of other amino acid derivatives such as amino esters and amino alcohols into β-Boc-hydrazino derivatives using this reagent. © 2012 Elsevier Ltd. All rights reserved. Source


Silva T.M.,University of Coimbra | Silva T.M.,Lund University | Andersson S.,Lund University | Sukumaran S.K.,Anthem Biosciences Pvt. Ltd | And 3 more authors.
PLoS ONE | Year: 2013

Background: New strategies are needed for breast cancer treatment and one initial step is to test new chemotherapeutic drugs in breast cancer cell lines, to choose candidates for further studies towards clinical use. Methodology and Findings: The cytotoxic effects of a biogenic polyamine analogue - norspermidine - and its trinuclear Pd(II) and Pt(II) complexes - Pd3NSpd2 and Pt3NSpd2, respectively - were investigated in one immortalized normal-like and three breast cancer cell lines. The normal-like MCF-10A cells were least sensitive to the compounds, while growth inhibition and cell death was observed in the cancer cell lines. Norspermidine and its Pd(II) complex were generally shown to have stronger antiproliferative effects than the corresponding Pt(II) complex. Moreover, both norspermidine and the Pd(II) complex reduced the cellular activity of the growth-related enzyme, ornithine decarboxylase (ODC) to a lower level than the Pt(II) complex in most of the cell lines examined. Treatment with norspermidine or the Pd(II) complex reduced the number of colonies formed in a soft agar assay performed with the breast cancer cell lines, indicating that these compounds reduced the malignancy of the breast cancer cells. The effect of norspermidine or the Pd(II) complex on colony formation was much stronger than that observed for the Pt(II) complex. The results from a new mammalian genotoxicity screen together with those of a single cell gel electrophoresis assay indicated that none of the drugs were genotoxic at a 25 μM concentration. Main Conclusions: Overall, norspermidine and its Pd(II) complex were shown to have strong antiproliferative effects. In comparison, the effects obtained with the Pd(II) complex were much stronger than that of the Pt(II) complex. The results obtained in the present study demonstrate that the trinuclear Pd(II) complex of norspermidine (Pd3NSpd2) may be regarded as a potential new metal-based drug against breast cancer, coupling a significant efficiency to a low toxicity. © 2013 Silva et al. Source

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