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161 results on '"Murru, Siva"'

1. Synthesis, inverse docking-assisted identification and in vitro biological characterization of Flavonol-based analogs of fisetin as c-Kit, CDK2 and mTOR inhibitors against melanoma and non-melanoma skin cancers

Author

Roy, Tithi, Boateng, Samuel T., Banang-Mbeumi, Sergette, Singh, Pankaj K., Basnet, Pratik, Chamcheu, Roxane-Cherille N., Ladu, Federico, Chauvin, Isabel, Spiegelman, Vladimir S., Hill, Ronald A., Kousoulas, Konstantin G., Nagalo, Bolni Marius, Walker, Anthony L., Fotie, Jean, Murru, Siva, Sechi, Mario, and Chamcheu, Jean Christopher

Published
2021
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2. Synthesis, in silico modelling, and in vitro biological evaluation of substituted pyrazole derivatives as potential anti-skin cancer, anti-tyrosinase, and antioxidant agents.

Author

Boateng, Samuel T., Roy, Tithi, Torrey, Kara, Owunna, Uchechi, Banang-Mbeumi, Sergette, Basnet, David, Niedda, Eleonora, Alexander, Alexis D., Hage, Denzel El, Atchimnaidu, Siriki, Nagalo, Bolni Marius, Aryal, Dinesh, Findley, Ann, Seeram, Navindra P., Efimova, Tatiana, Sechi, Mario, Hill, Ronald A., Ma, Hang, Chamcheu, Jean Christopher, and Murru, Siva

Subjects
BIOCHEMISTRY, PYRAZOLE derivatives, MOLECULAR docking, NUCLEAR magnetic resonance, ANTIOXIDANTS, MELANINS
Abstract

Twenty-five azole compounds (P1–P25) were synthesised using regioselective base-metal catalysed and microwave-assisted approaches, fully characterised by high-resolution mass spectrometry (HRMS), nuclear magnetic resonance (NMR), and infrared spectra (IR) analyses, and evaluated for anticancer, anti-tyrosinase, and anti-oxidant activities in silico and in vitro. P25 exhibited potent anticancer activity against cells of four skin cancer (SC) lines, with selectivity for melanoma (A375, SK-Mel-28) or non-melanoma (A431, SCC-12) SC cells over non-cancerous HaCaT-keratinocytes. Clonogenic, scratch-wound, and immunoblotting assay data were consistent with anti-proliferative results, expression profiling therewith implicating intrinsic and extrinsic apoptosis activation. In a mushroom tyrosinase inhibition assay, P14 was most potent among the compounds (half-maximal inhibitory concentration where 50% of cells are dead, IC50 15.9 μM), with activity greater than arbutin and kojic acid. Also, P6 exhibited noteworthy free radical-scavenging activity. Furthermore, in silico docking and absorption, distribution, metabolism, excretion, and toxicity (ADMET) simulations predicted prominent-phenotypic actives to engage diverse cancer/hyperpigmentation-related targets with relatively high affinities. Altogether, promising early-stage hits were identified – some with multiple activities – warranting further hit-to-lead optimisation chemistry with further biological evaluations, towards identifying new skin-cancer and skin-pigmentation renormalising agents. [ABSTRACT FROM AUTHOR]

Published
2023
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10. Identification of new fisetin analogs as kinase inhibitors: Data on synthesis and anti-skin cancer activities evaluation

Author

Roy, Tithi, primary, Boateng, Samuel T., additional, Banang-Mbeumi, Sergette, additional, Singh, Pankaj K., additional, Basnet, Pratik, additional, Chamcheu, Roxane-Cherille N., additional, Ladu, Federico, additional, Chauvin, Isabel, additional, Spiegelman, Vladimir S., additional, Hill, Ronald A., additional, Kousoulas, Konstantin G., additional, Nagalo, Bolni Marius, additional, Walker, Anthony L., additional, Fotie, Jean, additional, Murru, Siva, additional, Sechi, Mario, additional, and Chamcheu, Jean Christopher, additional

Published
2021
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16. Copper(I)-catalyzed synthesis of substituted 2-mercapto benzimidazoles

Author

Murru, Siva, Patel, Bhisma K., Le Bras, Jean, and Muzart, Jacques

Subjects
Benzimidazoles -- Chemical properties, Benzimidazoles -- Structure, Copper -- Chemical properties, Copper -- Structure, Biological sciences, Chemistry
Abstract

An efficient method is developed for preparing various substituted 2-mercapto benzimidazoles from their corresponding thioureas. 2-Mercapto benzimidazoles substituted with a p-methoxybenzyl group has allowed access to benzimidazole thiones.

Published
2009

17. Hypervalent iodine(III)-mediated regioselective N-acylation of 1,3-disubstituted thioureas

Author

Singh, C.B., Ghosh, Harisadhan, Murru, Siva, and Patel, Bhisma K.

Subjects
Iodine compounds -- Structure, Iodine compounds -- Chemical properties, Urea -- Structure, Urea -- Chemical properties, X-ray crystallography -- Observations, Acylation -- Analysis, Chemistry
Abstract

The reaction of asymmetrical 1,3-disubstituted thioureas with diacetoxyiodobenzene (DIB) has produced N-acetylurea regioselectively. The correlation is found between the regioselectivity and the p[K.sub.a] of the amine.

Published
2008

22. Synthesis of Novel Oxazolyl Amino Acids and Their Use in the Parallel Synthesis of Disubstituted Oxazole Libraries.

Author

Murru, Siva, Bista, Ramesh, and Nefzi, Adel

Subjects
*AMINO acid synthesis, *OXAZOLES synthesis, *ALANINE, *METHYL formate, *GLUTAMIC acid
Abstract

Novel chiral oxazolyl alanine and homologues are synthesized and utilized as building blocks for the solid-phase parallel synthesis of novel trifunctional oxazole small molecules in good to excellent overall yields and with high purity. The orthogonal deprotection strategy of oxazolyl amino acids, prepared from serine methyl ester and amino acids such as aspartic and glutamic acids, allows multiple sites of diversification to make a variety of pharmacologically relevant small molecules. The general nature of this approach allows the preparation of a large number of small molecules and peptidomimetics. [ABSTRACT FROM AUTHOR]

Published
2018
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27. Newer Strategies for the Synthesis of five and six Membered Heterocycles Containing N, O and S

Author

Murru, Siva

Subjects
CHEMISTRY
Abstract

Supervisor: Bhisma K. Patel, The contents of this thesis have been divided into five chapters based on the results of experimental works performed during the complete course of the research period. The introductory chapter of the thesis presents an overview of different aspects of heterocyclic chemistry with special reference to five and six membered heterocycles and their synthesis using tribromides and copper catalysts. Chapters 2 and 3 describe the syntheses of 1, 4- dithiins and 2-iminothiazolines using a ditribromide reagent (EDPBT). Chapters 4 and 5 illustrate copper-catalyzed syntheses of substituted 2-mercapto benzimidazoles and 2- substituted benzothiazoles via inter and intramolecular hetero-arylations. Each chapter constitute four sections, describing introduction, present work, experimental work and spectral data respectively.CHAPTER I. Introduction to Heterocyclic Chemistry This chapter highlights the nomenclature, definition and importance of heterocycles and literature background for the synthesis of heterocycles using organic ammonium tribromides (OATBs) and copper catalysts. Heterocycles make up an exceedingly important class of compounds. More than half of all known organic compounds are heterocycles. Almost all the compounds we know as drugs, most vitamins and many other natural products are heterocycles. The class also includes many other compounds of biological importance, such as nucleic acids, carbohydrates, hormones, and pigments. Heterocyclic compounds are key components of pharmaceutical chemistry and therefore, they have been a fruitful source of inspiration for the design of structural analogues to be used as pharmacological tools as well as new drugs. One of the reasons for the wide spread use of heterocyclic compounds as shown below, is that their structures can be subtly manipulated to achieve a required modification in function..

Published
2009

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