Search results for: Balasubramanian Gopalan

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article

Orally available stilbene derivatives as potent HDAC inhibitors with antiproliferative activities and antitumor effects in human tumor xenografts

Virendra Kachhadia, Sridharan Rajagopal, Thanasekaran Ponpandian, Radhakrishnan Vignesh, more

European Journal of Medicinal Chemistry > 2016 > 108 > C > 274-286

Herein we report the synthesis and activity of a novel class of HDAC inhibitors based on 2, 3-diphenyl acrylic acid derivatives. The compounds in this series have shown to be potent HDAC inhibitors possessing significant antiproliferative activity. Further compounds in this series were subjected to metabolic stability in human liver microsomes (HLM), mouse liver microsomes (MLM), and exhibits promising...

article

Performance Improvement of Average Based Spatial Filters through Multilevel Preprocessing using Wavelets

Balasubramanian Gopalan, A. Chilambuchelvan, S. Vijayan, G. Gowrison

IEEE Signal Processing Letters > 2015 > 22 > 10 > 1698 - 1702

Image denoising filters intended to remove Gaussian noise, principally exploit a procedure called spatial averaging. Quite a lot of averaging approaches have been developed and numerous fall in the class of either pixel-based or patch-based or diffusion-based approach. While the designed filters get rid of the noise, the high frequency information will also be degraded, as the filters fit into a nature...

article

Discovery of adamantane based highly potent HDAC inhibitors

Balasubramanian Gopalan, Thanasekaran Ponpandian, Virendra Kachhadia, Kuppusamy Bharathimohan, more

Bioorganic & Medicinal Chemistry Letters > 2013 > 23 > 9 > 2532-2537

Herein, we report the development of highly potent HDAC inhibitors for the treatment of cancer. A series of adamantane and nor-adamantane based HDAC inhibitors were designed, synthesized and screened for the inhibitory activity of HDAC. A number of compounds exhibited GI ₅₀ of 10-100 nM in human HCT116, NCI-H460 and U251 cancer cells, in vitro. Compound 32 displays efficacy in human tumour...

article

Microwave-assisted Claisen rearrangement of naphthyl 2-propynyl ethers: synthesis of naphthofurans

V.S. Prasada Rao Lingam, Dnyaneshwar H. Dahale, Kagga Mukkanti, Balasubramanian Gopalan, more

Tetrahedron Letters > 2012 > 53 > 42 > 5695-5698

An efficient two-step approach for the synthesis of naphtho[1,2-b]furans and naphtho[2,1-b]furans has been developed. Various functionalized propargyl alcohols were etherified with α- or β-naphthol under Mitsunobu reaction conditions to give naphthyl 2-propynyl ethers, which underwent a facile microwave-assisted Claisen rearrangement and concomitant anionic cyclization to yield naphthofuran derivatives...

article

Synthesis and evaluation of some novel dibenzo[b,d]furan carboxylic acids as potential anti-diabetic agents

N. Lakshminarayana, Y. Rajendra Prasad, Laxmikant Gharat, Abraham Thomas, more

European Journal of Medicinal Chemistry > 2010 > 45 > 9 > 3709-3718

A series of novel dibenzo[b,d]furan mono-carboxylic acid derivatives were synthesized, characterized and evaluated for their ability to inhibit Protein Tyrosine Phosphatase 1B (PTP1B) in vitro in order to use them as potential anti-diabetic agents. Structure–activity relationship study led to the identification of potent compound 5E which inhibited PTP1B with IC ₅₀ value of 82±0.43nM. Compound...

article

Synthesis and evaluation of some novel isochroman carboxylic acid derivatives as potential anti-diabetic agents

N. Lakshminarayana, Y. Rajendra Prasad, Laxmikant Gharat, Abraham Thomas, more

European Journal of Medicinal Chemistry > 2009 > 44 > 8 > 3147-3157

A series of novel isochroman mono-carboxylic acid derivatives were synthesized, characterized and evaluated for their ability to inhibit protein tyrosine phosphatase 1B (PTP1B) in vitro in order to use them as potential anti-diabetic agents. Analysis of structure–activity relationships led to the identification of potent compound 4n which inhibited PTP1B with IC ₅₀ value of 51.63±0.91nM. In...

article

A simple approach to highly functionalized benzo[b]furans from phenols and aryl iodides via aryl propargyl ethers

V.S. Prasada Rao Lingam, Ramanatham Vinodkumar, Khagga Mukkanti, Abraham Thomas, more

Tetrahedron Letters > 2008 > 49 > 27 > 4260-4264

A variety of mono- and disubstituted phenols are alkylated with propargyl bromide to give phenyl 2-propynyl ethers, which were further coupled with aryl iodides under Sonogashira reaction conditions to give 3-phenoxy-1-aryl-1-propyne derivatives. The latter compounds underwent an initial Claisen rearrangement followed by ring closure to give functionalized benzo[b]furans in moderate to good yields.

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ANTI-DIABETIC ACTIVITY (2)
CLAISEN REARRANGEMENT (2)
PTP1B INHIBITION (2)
ADAMANTANE (1)
ANISOTROPIC FILTER (1)
ANTIPROLIFERATIVE ACTIVITY (1)
ARYL PROPARGYL ETHERS (1)
BENZAMIDE (1)
BENZO[B]FURANS (1)
BILATERAL FILTER (1)
CESIUM FLUORIDE (1)
DIBENZO[B,D]FURAN CARBOXYLIC ACID (1)
GAUSSIAN NOISE (1)
HDAC INHIBITORS (1)
HISTONE DEACETYLASES (1)
HYDROXAMATE (1)
IEEE XPLORE (1)
INFORMATION FILTERS (1)
ISOCHROMAN-3-(S)-CARBOXYLIC ACID (1)
MICROWAVE IRRADIATION (1)
MITSUNOBU REACTION (1)
N-HYDROXY-4-AMINOMETHYL CINNAMIDE (1)
NAPHTHO[1,2-B]FURANS (1)
NAPHTHO[2,1-B]FURANS (1)
NAPHTHYL 2-PROPYNYL ETHERS (1)
NOISE (1)
NOISE MEASUREMENT (1)
NOISE REDUCTION (1)
NON LOCAL MEANS FILTER (1)
NOR-ADAMANTANE (1)
PREPROCESSING FILTER (1)
PROBABILISTIC NON LOCAL MEANS FILTER (1)
SONOGASHIRA COUPLING (1)
SPATIAL AVERAGING (1)
STILBENE (1)
TUMOUR XENOGRAFT (1)
WAVELET DOMAIN (1)
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Elsevier (6)
ieee (1)

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Search results for: Balasubramanian Gopalan

Orally available stilbene derivatives as potent HDAC inhibitors with antiproliferative activities and antitumor effects in human tumor xenografts

Performance Improvement of Average Based Spatial Filters through Multilevel Preprocessing using Wavelets

Discovery of adamantane based highly potent HDAC inhibitors

Microwave-assisted Claisen rearrangement of naphthyl 2-propynyl ethers: synthesis of naphthofurans

Synthesis and evaluation of some novel dibenzo[b,d]furan carboxylic acids as potential anti-diabetic agents

Synthesis and evaluation of some novel isochroman carboxylic acid derivatives as potential anti-diabetic agents

A simple approach to highly functionalized benzo[b]furans from phenols and aryl iodides via aryl propargyl ethers

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