- Design, synthesis, in silico and in vitro studies of novel 4-methylthiazole-5-carboxylic acid derivatives as potent anti-cancer agents
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Since inhibitors of mucin onco proteins are potential targets for breast cancer therapy, a series of novel 4-methylthiazole-5-carboxylic acid (1) derivatives 3a-k were synthesized by the reaction of 1 with SOCl2followed by different bases/alcohols in the presence of triethylamine. Once synthesized and characterized, their binding modes with MUC1 were studied by molecular docking analysis using Aruglab 4.0.1 and QSAR properties were determined using HyperChem. All synthesized compounds were screened for in vitro anti-breast cancer activity against MDA-MB-231 breast adenocarcinoma cell lines by Trypan-blue cell viability assay and MTT methods. Compounds 1, 3b, 3d, 3e, 3i and 3f showed good anti-breast cancer activity. Since 1 and 3d exhibited high potent activity against MDA-MB-231 cell lines, they show could be effective mucin onco protein inhibitors.
- Kilaru, Ravendra Babu,Valasani, Koteswara Rao,Yellapu, Nanda Kumar,Osuru, Hari Prasad,Kuruva, Chandra Sekhar,Matcha, Bhaskar,Chamarthi, Naga Raju
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supporting information
p. 4580 - 4585
(2015/02/19)
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- PROCESSES FOR THE PREPARATION OF FEBUXOSTAT AND SALTS THEREOF
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There is provided a process for preparing febuxostat of formula (I) or a pharmaceutically acceptable salt thereof, the process comprising: condensing a compound of formula (A) with a compound of formula (B) to form an ester of febuxostat; hydrolyzing the ester of febuxostat to febuxostat, and optionally converting the febuxostat to a pharmaceutically acceptable salt thereof, wherein: R' is an activating group selected from boronic acid or lithium; R is selected from optionally substituted C1-4 alkyl or optionally substituted aryl; L is a leaving group selected from diazo, halo, -OSO2R", -OCOR" or -O-Si(R")3; and R" is selected from optionally substituted C1-4 alkyl or optionally substituted aryl.
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Page/Page column 29
(2011/07/07)
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