213844-39-4Relevant academic research and scientific papers
Synthesis and biological evaluation of trans 6-methoxy-1,1-dimethyl-2- phenyl-3-aryl-2,3-dihydro-1H-inden-4-yloxyalkylamine derivatives against drug susceptible, non-replicating M. tuberculosis H37Rv and clinical multidrug resistant strains
Kumar, Shailesh,Dwivedi, Atma P.,Kashyap, Vivek Kr.,Saxena,Dwivedi,Srivastava, Ranjana,Sahu, Devi P.
, p. 2404 - 2407 (2013)
Synthesis of a library of novel trans 6-methoxy-1,1-dimethyl-2-phenyl-3- aryl-2,3-dihydro-1H-inden-4-yloxy alkyl amines and their antimycobacterial activity against drug sensitive and multidrug resistant strains of Mycobacterium tuberculosis have been reported. All the new compounds in the series exhibited MIC between 1.56 and 6.25 μg/ml. Two compounds 1i and 1j with low MIC and low cytotoxicity showed significant reduction in CFU in infected mouse macrophages at 1× MIC concentration. The compound 1i inhibited the growth of M. tuberculosis in mice at 100 mg/kg dose with 1.35 log10 reduction of CFU in lungs tissue and was active against non-replicating Mycobacterium tuberculosis under anaerobic condition.
Design and synthesis of ERα/ERβ selective coumarin and chromene derivatives as potential anti-breast cancer and anti-osteoporotic agents
Hussain, M. Kamil,Ansari, M. Imran,Yadav,Gupta, Puneet K.,Gupta,Saxena,Fatima,Manohar,Kushwaha,Khedgikar,Gautam,Kant, Ruchir,Maulik,Trivedi,Dwivedi,Kumar, K. Ravi,Saxena,Hajela
, p. 8828 - 8845 (2014/03/21)
Several new coumarin and chromene prototype derivatives have been synthesised and evaluated for their ERα and ERβ selective activity. Coumarin prototype compounds 18 & 19 were found to be ERα selective and the most active, exhibiting potential antiproliferative activity against both ER +ve & ER -ve breast cancer cell lines. The surprise finding of the series, however, are the novel prototype III chromenes 45 & 46, with aroyl substitution at the 6th position. Both the compounds have shown potent antiproliferative activity against both the breast cancer cell lines, promote alkaline phosphatase activity, enhance osteoblast mineralization in vitro, significantly decrease ERE-ERα dependent transactivation and induce ERβ activity. This specific upregulation of ERβ isoform activity of compound 45 may be responsible for the antiosteoporotic activity at picomolar concentration. In addition, both the compounds were also devoid of any estrogenic activity, which correlates to their antiestrogenic behaviour in the two breast cancer cell lines. Assessment of selectivity using specific SiRNAs for ERα and ERβ revealed that most of the compounds showed ERα and ERβ-mediated action, except compound 28, which showed selectivity to ERα only. Computational docking analysis of active compounds 18 and 45 was conducted to correlate the interaction with the two receptors and it was found that the docked conformations of the coumarin prototype, compound 18 at ERα and ERβ active sites were more or less superimposable on each other. However, the unique orientation of the aminoalkoxy side chain of novel chromene (prototype III) compound 45 in the ERβ binding cavity may be responsible for its potential biological response. The Royal Society of Chemistry.
AN IMPROVED PROCESS FOR THE PREPARATION OF TRANS 3,4- DIARYLCHROMAN AND THEIR DERIVATIVES
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Page/Page column 12, (2009/07/18)
The invention describes an improved and advantageous process of preparation of trans 3,4-diarylchroman and similar derivatives there of, useful as anti-fertility, anti-osteoporotic and breast cancer drugs. Condensation of arenes with 2,2- dialkyl-3-aryl c
