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Your search keyword '"Prakash, Muthuraj"' showing total 23 results
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23 results on '"Prakash, Muthuraj"'

1. Identification of Potent and Selective Inhibitors of Fat Mass Obesity-Associated Protein Using a Fragment-Merging Approach

Author

Prakash, Muthuraj, primary, Itoh, Yukihiro, additional, Fujiwara, Yoshie, additional, Takahashi, Yukari, additional, Takada, Yuri, additional, Mellini, Paolo, additional, Elboray, Elghareeb E., additional, Terao, Mitsuhiro, additional, Yamashita, Yasunobu, additional, Yamamoto, Chika, additional, Yamaguchi, Takao, additional, Kotoku, Masayuki, additional, Kitao, Yuki, additional, Singh, Ritesh, additional, Roy, Rohini, additional, Obika, Satoshi, additional, Oba, Makoto, additional, Wang, Dan Ohtan, additional, and Suzuki, Takayoshi, additional

Published
2021
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2. DHQZ-17, a potent inhibitor of the transcription factor HNF4A, suppresses tumorigenicity of head and neck squamous cell carcinoma in vivo

Author

Ganesh Venkatraman, Kumarswamyreddy Nandarapu, Shilpa Tentu, Prakash Muthuraj, Suresh K. Rayala, and Kesavan Venkitasamy

Subjects
0301 basic medicine, Programmed cell death, Time Factors, Cell cycle checkpoint, Physiology, Clinical Biochemistry, Mice, Nude, Antineoplastic Agents, Apoptosis, Inhibitory Concentration 50, 03 medical and health sciences, 0302 clinical medicine, Cell Line, Tumor, medicine, Animals, Humans, Cytotoxicity, Transcription factor, Cell Proliferation, Quinazolinones, Dose-Response Relationship, Drug, Squamous Cell Carcinoma of Head and Neck, Chemistry, Cell growth, Cell Cycle Checkpoints, Cell Biology, medicine.disease, Xenograft Model Antitumor Assays, Head and neck squamous-cell carcinoma, 030104 developmental biology, Hepatocyte Nuclear Factor 4, Head and Neck Neoplasms, Cell culture, 030220 oncology & carcinogenesis, Carcinoma, Squamous Cell, Cancer research, Female
Abstract

A series of 2, 3-dihydroquinazolinone derivatives were synthesized, characterized and their anticancer activity was determined. Among the compounds synthesized and screened, one compound (17) showed potent anticancer activity against human head and neck squamous cell carcinoma cell line, SCC131 and was non-toxic to normal cells. The compound inhibited the growth of SCC131 cells, with an IC50 of 1.75 μM, triggered apoptotic mode of cell death and caused tumor regression of SCC131 tumor xenografts in athymic mice. To decipher the target for the lead compound, a high throughput qPCR array was performed. Results showed that the compound 17, inhibited the expression of a vital transcription factor HNF4A, involved in regulation of metabolic pathways. Thus, the present work has identified a lead compound 17, with potent anticancer activity, minimal normal cell toxicity and a plausible target and hence definitely holds future prospects as an anticancer agent.

Published
2017
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18. Construction of Polycyclic Fused Pyrrolidines with Three Contiguous Stereocenters via Michael Addition of Vinylmalononitriles to Nitrostyrenes Using L-Proline-Derived Thiourea.

Author

Vishwanath, Manjunatha, Prakash, Muthuraj, Vinayagam, Poopathy, and Kesavan, Venkitasamy

Subjects
*POLYCYCLIC compounds, *PYRROLIDINE, *MICHAEL reaction, *PROLINE, *THIOUREA, *ORGANOCATALYSIS
Abstract

The catalytic efficiency of a bifunctional chiral thiourea derived from L-proline was evaluated in the asymmetric direct vinylogous Michael reaction of α,α-dicyanoolefins to β-nitrostyrenes with an electron- releasing or electron-withdrawing substituent in various positions. The corresponding adducts were isolated in good yields, with excellent diastereo- (>99%) and enantioselectivity (up to 95%). The Michael adducts were further functionalized to achieve the synthesis of polycyclic fused pyrrolidines with three contiguous stereocenters in good enantioselectivities. [ABSTRACT FROM AUTHOR]

Published
2016
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21. Highly Enantioselective Alkylation of Allyl Acetates Using Tartrate-Derived Bioxazoline Ligands.

Author

Jayakumar, Samydurai, Prakash, Muthuraj, Balaraman, Kaluvu, and Kesavan, Venkitasamy

Subjects
*ENANTIOSELECTIVE catalysis, *HETEROGENEOUS catalysis, *ALKYLATION, *CHEMICAL reactions, *ACETATES
Abstract

Tartrate-derived bioxazoline ligands, which form a five-membered chelate ring with metals, were evaluated for use in the asymmetric allylic alkylation (AAA) reactions of various symmetrical and unsymmetrical allyl acetates. Excellent enantioselectivities were achieved by using both symmetrical and unsymmetrical allyl acetates. [ABSTRACT FROM AUTHOR]

Published
2014
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22. Investigation of the Enantioselective Synthesis of 2,3-Dihydroquinazolinones Using Sc(III)-/inda-pybox.

Author

Prakash, Muthuraj, Jayakumar, Samydurai, and Kesavan, Venkitasamy

Subjects
*ENANTIOSELECTIVE catalysis, *QUINAZOLINONES, *PHARMACEUTICAL chemistry, *RACEMIZATION, *SCANDIUM, *CHEMICAL reactions
Abstract

Derivatives of 2,3-dihydroquinazolinones (2,3-DHQZs) are prized for their prevalent pharmaceutical applications. Although there are potential applications, methods available for the enantioselective synthesis of these valuable compounds are scarce, since the chiral aminal center is prone to racemization. We have overcome the difficulties in the catalytic enantioselective synthesis of 2,3- DHQZs using Sc(III)-inda-pybox as a catalyst, in a process with a broad substrate scope [ABSTRACT FROM AUTHOR]

Published
2013
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23. ChemInform Abstract: Investigation of the Enantioselective Synthesis of 2,3-Dihydroquinazolinones Using Sc(III)-inda-Pybox.

Author

Prakash, Muthuraj, Jayakumar, Samydurai, and Kesavan, Venkitasamy

Subjects
*CHEMICAL reactions, *CHEMISTRY charts, *PYRIMIDINE derivatives, *ENANTIOSELECTIVE catalysis
Abstract

A chart is presented related to chemical reaction of fused pyrimidine derivatives which depicts enantioselective synthesis of 2,3-dihydroquinazolinones using Sc(III)-inda-pybox.

Published
2014
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