Network


Latest external collaboration on country level. Dive into details by clicking on the dots.

Hotspot


Dive into the research topics where Preet Mohinder Singh Bedi is active.

Publication


Featured researches published by Preet Mohinder Singh Bedi.


European Journal of Medicinal Chemistry | 2012

Azide-alkyne cycloaddition en route to novel 1H-1,2,3-triazole tethered isatin conjugates with in vitro cytotoxic evaluation.

Pardeep Singh; Pooja Sharma; Amit Anand; Preet Mohinder Singh Bedi; Tandeep Kaur; Ashok Kumar Saxena; Vipan Kumar

1H-1,2,3-triazole tethered isatin conjugates have been synthesized and evaluated for cytotoxicity on four human cancer cell lines. The results revealed 5a, 5c, 5e and 5n proved to be twice as potent as 5-fluorouracil on THP-1 cell line with 5a and 5c being most active exhibiting IC(50) values of <1 against all cell lines except Caco-2. Activity profiles showed dependence on the substituents on isatin rings with a preference for hydrogen while a strong electron withdrawing fluoro as well as nitro substituents on either ring decreased the anticancer activity.


Archiv Der Pharmazie | 2013

Design and Synthesis of Aza‐Flavones as a New Class of Xanthine Oxidase Inhibitors

Rajni Dhiman; Sahil Sharma; Gagandip Singh; Kunal Nepali; Preet Mohinder Singh Bedi

In an attempt to develop non‐purine‐based xanthine oxidase (XO) inhibitors, keeping in view the complications reported with the use of purine‐based XO inhibitors, the flavone framework (a class possessing XO inhibitory potential) was used as lead structure for further optimization. By means of structure‐based classical bioisosterism, quinolone was used as an isoster for chromone (a bicyclic unit present in flavones), owing to the bioactive potential and drug‐like properties of quinolones. This type of replacement does not alter the shape and structural features required for XO inhibition, and also provides some additional interaction sites, without the loss of hydrogen bonding and hydrophobic and arene–arene interactions. In the present study, a series of 2‐aryl/heteroaryl‐4‐quinolones (aza analogs of flavones) was rationally designed, synthesized and evaluated for in vitro XO inhibitory activity. Some notions about structure–activity relationships are presented indicating the influence of the nature of the 2‐aryl ring on the inhibitory activity. Important interactions of the most active compound 3l (IC50 = 6.24 µM) with the amino acid residues of the active site of XO were figured out by molecular modeling.


Bioorganic & Medicinal Chemistry Letters | 2011

Synthesis and in vitro Cytotoxic evaluation of N-alkylbromo and N-alkylphthalimido-isatins

Pardeep Singh; Sharanjeet Kaur; Vipan Kumar; Preet Mohinder Singh Bedi; Mohinder P. Mahajan; Irum Sehar; Harish Chandra Pal; Ajit Kumar Saxena

The manuscript pertains to the synthesis and in vitro cytotoxic evaluation of a series of N-alkylbromo and N-alkylphthalimido-isatins against four different human cancer cell lines namely Colon: HCT-15; Liver: Hep-2; Lung: A-549 and Leukemia: THP-1 at 10 and 100 μM concentrations. The active compounds based on preliminary studies were evaluated for their IC(50) value against six cell lines viz. Colo-205, HCT-15 (Colon), THP-1 (Leukemia), A-549 (Lung), PC-3 (Prostate) and HeLa (Cervix). The active analogue IS-4 exhibited IC(50) values of 4.57, 10.90, 11.75, 12.40 and 54.20 μM against HeLa, PC-3, HCT-15, THP-1 and Colo-205, respectively.


Chinese Journal of Catalysis | 2015

Silica supported Bronsted acids as catalyst in organic transformations: A comprehensive review

Manpreet Kaur; Sahil Sharma; Preet Mohinder Singh Bedi

Abstract Bronsted acid catalysts have been used in a number of organic transformations. To overcome limitations, such as toxicity, volatility, high price and hazardous nature of the conventional methods, the catalysts are adsorbed on silica gel to give the benefits and advantages of ready availability, simple work-up procedure, long catalytic life, environment-friendliness, good to excellent yields and recyclability. The uses of such catalysts have gained importance worldwide. This article describes some of the important silicated catalysts, namely, heteropolyacids, polyphosphoric acid, perchloric acid, fluoroboric acid, and silicated sulphuric acid. These catalysts have been used in a number of organic reactions to yield compounds that are important in the chemical and pharmaceutical industries. We summarize the beneficial effects of these catalysts and the reports that have been published on them in the past several years. In the present review, the description of the catalysts are introduced followed by a recent research history, and a comparison between the silica supported catalysts and other (polymer) supported catalysts. The article ends up giving the advantages of these catalytic systems over the conventional catalyst.


Bioorganic & Medicinal Chemistry Letters | 2014

Synthesis and evaluation of naphthoflavones as a new class of non purine xanthine oxidase inhibitors

Harbinder Singh; Sahil Sharma; Ritu Ojha; Manish K. Gupta; Kunal Nepali; Preet Mohinder Singh Bedi

In view of reported xanthine oxidase inhibitory potential of naphthopyrans and flavones, naphthoflavones as hybrids of the two were designed, synthesized and evaluated for in vitro xanthine oxidase inhibitory activity in the present study. The results of the assay revealed that the naphthoflavones possess promising inhibitory potential against the enzyme with IC50 values ranging from 0.62 to 41.2 μM. Structure activity relationship indicated that the nature and placement of substituents on the phenyl ring at 2nd position remarkably influences the inhibitory activity. Substitution of halo and nitro groups at ortho and para position of the phenyl ring (2nd position) remarkably favored the activity. NF-4 with p-fluoro phenyl ring was the most potent inhibitor with IC50 value of 0.62 μM. Enzyme kinetics study was also performed to investigate the inhibition mechanism and it was found that the naphthoflavones displayed mixed type inhibition. The basis of significant inhibition of xanthine oxidase by NF-4 was rationalized by molecular modeling studies.


Bioorganic & Medicinal Chemistry Letters | 2014

Microwave assisted synthesis of naphthopyrans catalysed by silica supported fluoroboric acid as a new class of non purine xanthine oxidase inhibitors.

Sahil Sharma; Kirti Sharma; Ritu Ojha; Dinesh Kumar; Gagandip Singh; Kunal Nepali; Preet Mohinder Singh Bedi

A series of naphthopyrans was synthesized employing silica supported fluoroboric acid under solvent free conditions in a microwave reactor. The catalytic influence of HBF4-SiO2 was investigated in detail to optimize the reaction conditions. The synthesised compounds were evaluated for in vitro xanthine oxidase inhibitory activity for the first time. Structure-activity relationship analyses have also been presented. Among the synthesised compounds, NP-17, NP-19, NP-20, NP-23, NP-24, NP-25 and NP-26 were the active inhibitors with an IC50 ranging from 4 to 17 μM. Compound NP-19 with a thiophenyl ring at position 1 emerged as the most potent xanthine oxidase inhibitor (IC50=4 μM) in comparison to allopurinol (IC50=11.10 μM) and febuxostat (IC50=0.025 μM). The basis of significant inhibition of xanthine oxidase by NP-19 was rationalized by its molecular docking at MTE binding site of xanthine oxidase.


Recent Patents on Anti-cancer Drug Discovery | 2014

Tubulin inhibitors: a patent survey.

Kunal Nepali; Ritu Ojha; Sahil Sharma; Preet Mohinder Singh Bedi; K.L. Dhar

Tubulin is one of the most useful and strategic molecular targets for anticancer drugs. The dynamic process of microtubule assembly and disassembly can be blocked by various agents that bind to distinct sites in the β-tubulin subunit. By interfering with microtubule function in vitro, these agents arrest cells in mitosis, eventually leading to cell death, by both apoptosis and necrosis. So far, three binding domains have been identified a) the colchicine site close to the α/β interface, b) the area where the vinca alkaloids bind, and c) the taxane-binding pocket. This review compiles the patent literature up to 2013 and offers a detailed account of all the advances on Tubulin inhibitors (lead molecules) along with in depth knowledge about the number of novel scaffolds, modified analogs and derivatives of the lead molecules. Colchicine binding site remains the most explored site indicated by the patent survey as majority of the patents revolves around phenstatin and combretastatin based molecules where the key structural feature for tubulin inhibition is an appropriate arrangement of the two aromatic rings at an appropriate distance and optimal dihedral angle maximizing interactions with tubulin. A brief account of promising tubulin inhibitors in stages of clinical development and some strategies for the development of potent molecules overcoming the problem of drug resistance have also been discussed.


European Journal of Medicinal Chemistry | 2016

Design strategies, structure activity relationship and mechanistic insights for purines as kinase inhibitors.

Sahil Sharma; Jagjeet Singh; Ritu Ojha; Harbinder Singh; Manpreet Kaur; Preet Mohinder Singh Bedi; Kunal Nepali

Kinases control a diverse set of cellular processes comprising of reversible phosphorylation of proteins. Protein kinases play a pivotal role in human tumor cell proliferation, migration and survival of neoplasia. In the recent past, purine based molecules have emerged as significantly potent kinase inhibitors. In view of their promising potential for the inhibition of kinases, this review article focuses on purines which have progressed as kinase inhibitors during the last five years. A detailed account of the design strategies employed for the synthesis of purine analogs exerting inhibitory effects on diverse kinases has been presented. Apart from presenting the design strategies, the article also highlights the structure activity relationship along with mechanistic insights revealed during the biological evaluation of the purine analogs for kinase inhibition. The interactions with the amino acid residues responsible for kinase inhibitory potential of purine based molecules have also been discussed. In this assemblage, purine based protein kinase inhibitors patented in the past have also been summarized in the tabular form. This compilation will be of great interest for the researchers working in the area of protein kinase inhibitors.


Recent Patents on Anti-cancer Drug Discovery | 2014

Anti-Cancer Pyrimidines in Diverse Scaffolds: A Review of Patent Literature

Ramandeep Kaur; Prabhkirat Kaur; Sahil Sharma; G. Singh; Samir Mehndiratta; Preet Mohinder Singh Bedi; Kunal Nepali

Pyrimidine ring is the building unit of DNA and RNA and thus pyrimidine based chemical architectures exhibit diverse pharmacological activities. Among the reported medicinal attributes of pyrimidines, anticancer activity is the most extensively reported. The anticancer potential of pyrimidines in fused scaffolds has also been evidenced through number of research article and patent literature. The pyrimidines based scaffolds have exerted their cell killing effects through varied mechanisms which indicate their potential to interact with diverse enzymes/ targets/receptors. This review article strictly focuses on the patent literature from 2009 onwards. The structure of the potent compounds, their IC50 values, models/assays used for the anticancer evaluation and the enzymes/ receptors/ targets involved have been presented in this compilation. Significant number of patents i.e. 59 have been published on pyrimidine based anticancer agents from 2009-2014 (from 2009 through the present date) which clearly indicate that this heterocycle is an area of focus at present for researchers all over the globe. Moreover, out of the 59 patents published during this period, 32 have been published from 2012 onwards which further highlights the present interest of the researcher towards pyrimidine based anticancer agents. The promising activity displayed by these pyrimidine based scaffolds clearly places them in forefront as potential future drug candidates. The present compilation can be extremely beneficial for the medicinal chemists working on design and synthesis of anticancer drugs.


Archiv Der Pharmazie | 2014

4,6-Diaryl/heteroarylpyrimidin-2(1H)-ones as a new class of xanthine oxidase inhibitors.

Shiwani Shukla; Dinesh Kumar; Ritu Ojha; Manish K. Gupta; Kunal Nepali; Preet Mohinder Singh Bedi

A series of 4,6‐diaryl/heteroarylpyrimidones was synthesized employing silica‐supported fluoroboric acid under solvent‐free conditions in a microwave reactor. The catalytic influence of HBF4‐SiO2 was investigated in detail to optimize the reaction conditions. The synthesized compounds were evaluated for in vitro xanthine oxidase (XO) inhibitory activity for the first time. Structure‐activity relationship analyses are also presented. Among the synthesized compounds, VA‐5, ‐9, ‐10, ‐12, ‐22, ‐23, and ‐25 were the active inhibitors with IC50 values ranging from 6.45 to 13.46 µM. Compound VA‐25 with a pyridinyl ring as ring A and a thiophenyl ring as ring B emerged as the most potent XO inhibitor (IC50 = 6.45 µM) in comparison to allopurinol (IC50 = 12.24 µM). Some of the important interactions of VA‐25 with the amino acid residues of the active site of XO were figured out by molecular modeling studies.

Collaboration


Dive into the Preet Mohinder Singh Bedi's collaboration.

Top Co-Authors

Avatar

Sahil Sharma

Guru Nanak Dev University

View shared research outputs
Top Co-Authors

Avatar

Kunal Nepali

Guru Nanak Dev University

View shared research outputs
Top Co-Authors

Avatar

Manish K. Gupta

The Energy and Resources Institute

View shared research outputs
Top Co-Authors

Avatar

Harbinder Singh

Guru Nanak Dev University

View shared research outputs
Top Co-Authors

Avatar

Ritu Ojha

Guru Nanak Dev University

View shared research outputs
Top Co-Authors

Avatar

Ajit Kumar Saxena

Council of Scientific and Industrial Research

View shared research outputs
Top Co-Authors

Avatar

Jatinder Singh

Guru Nanak Dev University

View shared research outputs
Top Co-Authors

Avatar

K.L. Dhar

Council of Scientific and Industrial Research

View shared research outputs
Top Co-Authors

Avatar
Top Co-Authors

Avatar
Researchain Logo
Decentralizing Knowledge