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Items: 1 to 50 of 208

1.

Differentiation of human neuroblastoma cell line IMR-32 by sildenafil and its newly discovered analogue IS00384.

Dar MI, Jan S, Reddy GL, Wani R, Syed M, Dar MJ, Sawant SD, Vishwakarma RA, Syed SH.

Cell Signal. 2020 Jan;65:109425. doi: 10.1016/j.cellsig.2019.109425. Epub 2019 Nov 2.

PMID:
31689507
2.

Corrigendum to "Design, synthesis and biological evaluation of pyrazolopyrimidinone based potent and selective PDE5 inhibitors for treatment of erectile dysfunction" [Bioorg. Chem. 89 (2019) 103022].

Reddy GL, Dar MI, Hudwekar AD, Mahajan P, Nargotra A, Baba AM, Nandi U, Wazir P, Singh G, Bharate SS, Vishwakarma RA, Syed SH, Sawant SD.

Bioorg Chem. 2019 Nov;92:103257. doi: 10.1016/j.bioorg.2019.103257. Epub 2019 Sep 13. No abstract available.

PMID:
31525521
3.

Binary and ternary solid dispersions of an anticancer preclinical lead, IIIM-290: In vitro and in vivo studies.

Kumar V, Mintoo MJ, Mondhe DM, Bharate SB, Vishwakarma RA, Bharate SS.

Int J Pharm. 2019 Oct 30;570:118683. doi: 10.1016/j.ijpharm.2019.118683. Epub 2019 Sep 9.

PMID:
31513869
4.

Preclinical Development of Crocus sativus-Based Botanical Lead IIIM-141 for Alzheimer's Disease: Chemical Standardization, Efficacy, Formulation Development, Pharmacokinetics, and Safety Pharmacology.

Bharate SS, Kumar V, Singh G, Singh A, Gupta M, Singh D, Kumar A, Vishwakarma RA, Bharate SB.

ACS Omega. 2018 Aug 20;3(8):9572-9585. doi: 10.1021/acsomega.8b00841. eCollection 2018 Aug 31.

5.

Glycyrrhizic Acid Prevents Oxidative Stress Mediated DNA Damage Response through Modulation of Autophagy in Ultraviolet-B-Irradiated Human Primary Dermal Fibroblasts.

Umar SA, Tanveer MA, Nazir LA, Divya G, Vishwakarma RA, Tasduq SA.

Cell Physiol Biochem. 2019;53(1):242-257. doi: 10.33594/000000133.

6.

Preclinical development of gastro-protective botanical candidate from Woodfordia fruticosa (Linn.) Kurz: Chemical standardization, efficacy, pharmacokinetics and safety pharmacology.

Khan IA, Singh A, Mindala DP, Meena S, Vij B, Yadav AK, Roy S, Nandi U, Katare AK, Jaglan S, Singh D, Gupta AP, Gupta P, Singh S, Tikko MK, Singh G, Vishwakarma RA.

J Ethnopharmacol. 2019 Sep 15;241:112023. doi: 10.1016/j.jep.2019.112023. Epub 2019 Jun 11.

PMID:
31195031
7.

Design, synthesis and biological evaluation of pyrazolopyrimidinone based potent and selective PDE5 inhibitors for treatment of erectile dysfunction.

Reddy GL, Dar MI, Hudwekar AD, Mahajan P, Nargotra A, Baba AM, Nandi U, Wazir P, Singh G, Vishwakarma RA, Syed SH, Sawant SD.

Bioorg Chem. 2019 Aug;89:103022. doi: 10.1016/j.bioorg.2019.103022. Epub 2019 May 31. Erratum in: Bioorg Chem. 2019 Nov;92:103257.

PMID:
31181491
8.

Transformation of Santonin to a Naproxen Analogue with Anti-Inflammatory Activity.

Singh R, Mandrah K, Asati A, Patel DK, Goel B, Vishwakarma RA, Roy SK, Jain SK.

J Nat Prod. 2019 Jun 28;82(6):1710-1713. doi: 10.1021/acs.jnatprod.8b00318. Epub 2019 May 24.

PMID:
31125226
9.

Trichoderma lixii (IIIM-B4), an endophyte of Bacopa monnieri L. producing peptaibols.

Katoch M, Singh D, Kapoor KK, Vishwakarma RA.

BMC Microbiol. 2019 May 16;19(1):98. doi: 10.1186/s12866-019-1477-8.

10.

Isolation of depsipeptides and optimization for enhanced production of valinomycin from the North-Western Himalayan cold desert strain Streptomyces lavendulae.

Singh VP, Sharma R, Sharma V, Raina C, Kapoor KK, Kumar A, Chaubey A, Singh D, Vishwakarma RA.

J Antibiot (Tokyo). 2019 Aug;72(8):617-624. doi: 10.1038/s41429-019-0183-y. Epub 2019 May 9.

PMID:
31073236
11.

Discovery and preclinical development of IIIM-160, a Bergenia ciliata-based anti-inflammatory and anti-arthritic botanical drug candidate.

Bharate SB, Kumar V, Bharate SS, Singh B, Singh G, Singh A, Gupta M, Singh D, Kumar A, Singh S, Vishwakarma RA.

J Integr Med. 2019 May;17(3):192-204. doi: 10.1016/j.joim.2019.03.001. Epub 2019 Mar 6.

PMID:
30898582
12.

Discovery of Quinazolin-4(3 H)-ones as NLRP3 Inflammasome Inhibitors: Computational Design, Metal-Free Synthesis, and in Vitro Biological Evaluation.

Abdullaha M, Mohammed S, Ali M, Kumar A, Vishwakarma RA, Bharate SB.

J Org Chem. 2019 May 3;84(9):5129-5140. doi: 10.1021/acs.joc.9b00138. Epub 2019 Apr 2.

PMID:
30896160
13.

Alborixin clears amyloid-β by inducing autophagy through PTEN-mediated inhibition of the AKT pathway.

Wani A, Gupta M, Ahmad M, Shah AM, Ahsan AU, Qazi PH, Malik F, Singh G, Sharma PR, Kaddoumi A, Bharate SB, Vishwakarma RA, Kumar A.

Autophagy. 2019 Oct;15(10):1810-1828. doi: 10.1080/15548627.2019.1596476. Epub 2019 Apr 2.

PMID:
30894052
14.

Introducing Oxo-Phenylacetyl (OPAc) as a Protecting Group for Carbohydrates.

Kumar A, Gannedi V, Rather SA, Vishwakarma RA, Ahmed QN.

J Org Chem. 2019 Apr 5;84(7):4131-4148. doi: 10.1021/acs.joc.9b00126. Epub 2019 Mar 28.

PMID:
30888192
15.

Analyzing the role of cannabinoids as modulators of Wnt/β-catenin signaling pathway for their use in the management of neuropathic pain.

Nalli Y, Dar MS, Bano N, Rasool JU, Sarkar AR, Banday J, Bhat AQ, Rafia B, Vishwakarma RA, Dar MJ, Ali A.

Bioorg Med Chem Lett. 2019 May 1;29(9):1043-1046. doi: 10.1016/j.bmcl.2019.03.013. Epub 2019 Mar 11.

PMID:
30871771
16.

Impurity profiling of anticancer preclinical candidate, IIIM-290.

Kumar V, Bhurta D, Sharma A, Kumar P, Bharate SB, Vishwakarma RA, Bharate SS.

J Pharm Biomed Anal. 2019 Mar 20;166:1-5. doi: 10.1016/j.jpba.2018.12.027. Epub 2018 Dec 18.

PMID:
30590350
17.

Orally Effective Aminoalkyl 10H-Indolo[3,2-b]quinoline-11-carboxamide Kills the Malaria Parasite by Inhibiting Host Hemoglobin Uptake.

Mudududdla R, Mohanakrishnan D, Bharate SS, Vishwakarma RA, Sahal D, Bharate SB.

ChemMedChem. 2018 Dec 6;13(23):2581-2598. doi: 10.1002/cmdc.201800579. Epub 2018 Nov 13.

PMID:
30358112
18.

Room Temperature Metal-Catalyzed Oxidative Acylation of Electron-Deficient Heteroarenes with Alkynes, Its Mechanism, and Application Studies.

Sharma S, Kumar M, Vishwakarma RA, Verma MK, Singh PP.

J Org Chem. 2018 Oct 19;83(20):12420-12431. doi: 10.1021/acs.joc.8b01475. Epub 2018 Oct 9.

PMID:
30238752
19.

Soluble Aβ1-42 suppresses TNF-α and activates NLRP3 inflammasome in THP-1 macrophages.

Gupta M, Wani A, Ul Ahsan A, Chopra M, Vishwakarma RA, Singh G, Kumar A.

Cytokine. 2018 Nov;111:84-87. doi: 10.1016/j.cyto.2018.07.026. Epub 2018 Aug 17.

PMID:
30125779
20.

Selection of a Water-Soluble Salt Form of a Preclinical Candidate, IIIM-290: Multiwell-Plate Salt Screening and Characterization.

Kumar V, Bharate SB, Vishwakarma RA, Bharate SS.

ACS Omega. 2018 Jul 31;3(7):8365-8377. doi: 10.1021/acsomega.8b00801. Epub 2018 Jul 27.

21.

Why Are the Majority of Active Compounds in the CNS Domain Natural Products? A Critical Analysis.

Bharate SS, Mignani S, Vishwakarma RA.

J Med Chem. 2018 Dec 13;61(23):10345-10374. doi: 10.1021/acs.jmedchem.7b01922. Epub 2018 Jul 20. Review.

PMID:
29989814
22.

Porostereum sp., Associated with Saffron (Crocus sativus L.), is a Latent Pathogen Capable of Producing Phytotoxic Chlorinated Aromatic Compounds.

Wani ZA, Ahmad T, Nalli Y, Ali A, Singh AP, Vishwakarma RA, Ashraf N, Riyaz-Ul-Hassan S.

Curr Microbiol. 2018 Jul;75(7):880-887. doi: 10.1007/s00284-018-1461-9. Epub 2018 Feb 28.

PMID:
29492649
23.

Design and synthesis of 1,4-substituted 1H-1,2,3-triazolo-quinazolin-4(3H)-ones by Huisgen 1,3-dipolar cycloaddition with PI3Kγ isoform selective activity.

Srinivas M, Singh Pathania A, Mahajan P, Verma PK, Chobe SS, Malik FA, Nargotra A, Vishwakarma RA, Sawant SD.

Bioorg Med Chem Lett. 2018 Apr 1;28(6):1005-1010. doi: 10.1016/j.bmcl.2018.02.032. Epub 2018 Feb 16.

PMID:
29486969
24.

Lipovelutibols A-D: Cytotoxic Lipopeptaibols from the Himalayan Cold Habitat Fungus Trichoderma velutinum.

Singh VP, Yedukondalu N, Sharma V, Kushwaha M, Sharma R, Chaubey A, Kumar A, Singh D, Vishwakarma RA.

J Nat Prod. 2018 Feb 23;81(2):219-226. doi: 10.1021/acs.jnatprod.6b00873. Epub 2018 Jan 26.

PMID:
29373791
25.

Corrigendum: Mannitol Stress Directs Flavonoid Metabolism toward Synthesis of Flavones via Differential Regulation of Two Cytochrome P450 Monooxygenases in Coleus forskohlii.

Awasthi P, Gupta AP, Bedi YS, Vishwakarma RA, Gandhi SG.

Front Plant Sci. 2018 Jan 8;8:2222. doi: 10.3389/fpls.2017.02222. eCollection 2017.

26.

Discovery and Preclinical Development of IIIM-290, an Orally Active Potent Cyclin-Dependent Kinase Inhibitor.

Bharate SB, Kumar V, Jain SK, Mintoo MJ, Guru SK, Nuthakki VK, Sharma M, Bharate SS, Gandhi SG, Mondhe DM, Bhushan S, Vishwakarma RA.

J Med Chem. 2018 Feb 22;61(4):1664-1687. doi: 10.1021/acs.jmedchem.7b01765. Epub 2018 Feb 6.

PMID:
29370702
27.

Present drug-likeness filters in medicinal chemistry during the hit and lead optimization process: how far can they be simplified?

Mignani S, Rodrigues J, Tomas H, Jalal R, Singh PP, Majoral JP, Vishwakarma RA.

Drug Discov Today. 2018 Mar;23(3):605-615. doi: 10.1016/j.drudis.2018.01.010. Epub 2018 Jan 9. Review.

PMID:
29330127
28.

Establishment of LCMS Based Platform for Discovery of Quorum Sensing Inhibitors: Signal Detection in Pseudomonas aeruginosa PAO1.

Kushwaha M, Jain SK, Sharma N, Abrol V, Jaglan S, Vishwakarma RA.

ACS Chem Biol. 2018 Mar 16;13(3):657-665. doi: 10.1021/acschembio.7b00875. Epub 2018 Jan 18.

PMID:
29303546
29.

Physicochemical, pharmacokinetic, efficacy and toxicity profiling of a potential nitrofuranyl methyl piperazine derivative IIIM-MCD-211 for oral tuberculosis therapy via in-silico-in-vitro-in-vivo approach.

Magotra A, Sharma A, Singh S, Ojha PK, Kumar S, Bokolia N, Wazir P, Sharma S, Khan IA, Singh PP, Vishwakarma RA, Singh G, Nandi U.

Pulm Pharmacol Ther. 2018 Feb;48:151-160. doi: 10.1016/j.pupt.2017.11.006. Epub 2017 Nov 21.

PMID:
29174840
30.

Glycyrrhiza glabra extract and quercetin reverses cisplatin resistance in triple-negative MDA-MB-468 breast cancer cells via inhibition of cytochrome P450 1B1 enzyme.

Sharma R, Gatchie L, Williams IS, Jain SK, Vishwakarma RA, Chaudhuri B, Bharate SB.

Bioorg Med Chem Lett. 2017 Dec 15;27(24):5400-5403. doi: 10.1016/j.bmcl.2017.11.013. Epub 2017 Nov 7.

PMID:
29150398
31.

Design of Novel 3-Pyrimidinylazaindole CDK2/9 Inhibitors with Potent In Vitro and In Vivo Antitumor Efficacy in a Triple-Negative Breast Cancer Model.

Singh U, Chashoo G, Khan SU, Mahajan P, Nargotra A, Mahajan G, Singh A, Sharma A, Mintoo MJ, Guru SK, Aruri H, Thatikonda T, Sahu P, Chibber P, Kumar V, Mir SA, Bharate SS, Madishetti S, Nandi U, Singh G, Mondhe DM, Bhushan S, Malik F, Mignani S, Vishwakarma RA, Singh PP.

J Med Chem. 2017 Dec 14;60(23):9470-9489. doi: 10.1021/acs.jmedchem.7b00663. Epub 2017 Dec 5.

PMID:
29144137
32.

Synthesis, pH dependent, plasma and enzymatic stability of bergenin prodrugs for potential use against rheumatoid arthritis.

Singh R, Kumar V, Bharate SS, Vishwakarma RA.

Bioorg Med Chem. 2017 Oct 15;25(20):5513-5521. doi: 10.1016/j.bmc.2017.08.011. Epub 2017 Aug 10.

PMID:
28843845
33.

Biotransformation of Chrysin to Baicalein: Selective C6-Hydroxylation of 5,7-Dihydroxyflavone Using Whole Yeast Cells Stably Expressing Human CYP1A1 Enzyme.

Williams IS, Chib S, Nuthakki VK, Gatchie L, Joshi P, Narkhede NA, Vishwakarma RA, Bharate SB, Saran S, Chaudhuri B.

J Agric Food Chem. 2017 Aug 30;65(34):7440-7446. doi: 10.1021/acs.jafc.7b02690. Epub 2017 Aug 15.

PMID:
28782952
34.

Synthesis and biological evaluation of pyrrole-based chalcones as CYP1 enzyme inhibitors, for possible prevention of cancer and overcoming cisplatin resistance.

Williams IS, Joshi P, Gatchie L, Sharma M, Satti NK, Vishwakarma RA, Chaudhuri B, Bharate SB.

Bioorg Med Chem Lett. 2017 Aug 15;27(16):3683-3687. doi: 10.1016/j.bmcl.2017.07.010. Epub 2017 Jul 4.

PMID:
28711350
35.

Natural alkaloids as P-gp inhibitors for multidrug resistance reversal in cancer.

Joshi P, Vishwakarma RA, Bharate SB.

Eur J Med Chem. 2017 Sep 29;138:273-292. doi: 10.1016/j.ejmech.2017.06.047. Epub 2017 Jun 27. Review.

PMID:
28675836
36.

Chemical chaperone 4-phenyl butyric acid (4-PBA) reduces hepatocellular lipid accumulation and lipotoxicity through induction of autophagy.

Nissar AU, Sharma L, Mudasir MA, Nazir LA, Umar SA, Sharma PR, Vishwakarma RA, Tasduq SA.

J Lipid Res. 2017 Sep;58(9):1855-1868. doi: 10.1194/jlr.M077537. Epub 2017 Jun 27.

37.

Development and validation of a highly sensitive LC-ESI-MS/MS method for estimation of IIIM-MCD-211, a novel nitrofuranyl methyl piperazine derivative with potential activity against tuberculosis: Application to drug development.

Magotra A, Sharma A, Gupta AP, Wazir P, Sharma S, Singh PP, Tikoo MK, Vishwakarma RA, Singh G, Nandi U.

J Chromatogr B Analyt Technol Biomed Life Sci. 2017 Aug 15;1060:200-206. doi: 10.1016/j.jchromb.2017.06.015. Epub 2017 Jun 8.

PMID:
28623772
38.

Revelation and cloning of valinomycin synthetase genes in Streptomyces lavendulae ACR-DA1 and their expression analysis under different fermentation and elicitation conditions.

Sharma R, Jamwal V, Singh VP, Wazir P, Awasthi P, Singh D, Vishwakarma RA, Gandhi SG, Chaubey A.

J Biotechnol. 2017 Jul 10;253:40-47. doi: 10.1016/j.jbiotec.2017.05.008. Epub 2017 May 18.

PMID:
28528783
39.

Identification of Potent and Selective CYP1A1 Inhibitors via Combined Ligand and Structure-Based Virtual Screening and Their in Vitro Validation in Sacchrosomes and Live Human Cells.

Joshi P, McCann GJP, Sonawane VR, Vishwakarma RA, Chaudhuri B, Bharate SB.

J Chem Inf Model. 2017 Jun 26;57(6):1309-1320. doi: 10.1021/acs.jcim.7b00095. Epub 2017 May 22.

PMID:
28489395
40.

Crocus sativus Extract Tightens the Blood-Brain Barrier, Reduces Amyloid β Load and Related Toxicity in 5XFAD Mice.

Batarseh YS, Bharate SS, Kumar V, Kumar A, Vishwakarma RA, Bharate SB, Kaddoumi A.

ACS Chem Neurosci. 2017 Aug 16;8(8):1756-1766. doi: 10.1021/acschemneuro.7b00101. Epub 2017 May 15.

41.

Exploring Derivatives of Quinazoline Alkaloid l-Vasicine as Cap Groups in the Design and Biological Mechanistic Evaluation of Novel Antitumor Histone Deacetylase Inhibitors.

Ahmad M, Aga MA, Bhat JA, Kumar B, Rouf A, Capalash N, Mintoo MJ, Kumar A, Mahajan P, Mondhe DM, Nargotra A, Sharma PR, Zargar MA, Vishwakarma RA, Shah BA, Taneja SC, Hamid A.

J Med Chem. 2017 Apr 27;60(8):3484-3497. doi: 10.1021/acs.jmedchem.7b00322. Epub 2017 Apr 13.

PMID:
28368585
42.

Functional Characterization of CsBGlu12, a β-Glucosidase from Crocus sativus, Provides Insights into Its Role in Abiotic Stress through Accumulation of Antioxidant Flavonols.

Baba SA, Vishwakarma RA, Ashraf N.

J Biol Chem. 2017 Mar 17;292(11):4700-4713. doi: 10.1074/jbc.M116.762161. Epub 2017 Jan 31.

43.

Metal-free Cross-Dehydrogenative Coupling of HN-azoles with α-C(sp3)-H Amides via C-H Activation and Its Mechanistic and Application Studies.

Aruri H, Singh U, Kumar M, Sharma S, Aithagani SK, Gupta VK, Mignani S, Vishwakarma RA, Singh PP.

J Org Chem. 2017 Jan 20;82(2):1000-1012. doi: 10.1021/acs.joc.6b02448. Epub 2017 Jan 9.

PMID:
28013543
44.

Development and mechanistic insight into enhanced cytotoxic potential of hyaluronic acid conjugated nanoparticles in CD44 overexpressing cancer cells.

Saneja A, Nayak D, Srinivas M, Kumar A, Khare V, Katoch A, Goswami A, Vishwakarma RA, Sawant SD, Gupta PN.

Eur J Pharm Sci. 2017 Jan 15;97:79-91. doi: 10.1016/j.ejps.2016.10.028. Epub 2016 Oct 29.

PMID:
27989859
45.

An Insight into the Secondary Metabolism of Muscodor yucatanensis: Small-Molecule Epigenetic Modifiers Induce Expression of Secondary Metabolism-Related Genes and Production of New Metabolites in the Endophyte.

Qadri M, Nalli Y, Jain SK, Chaubey A, Ali A, Strobel GA, Vishwakarma RA, Riyaz-Ul-Hassan S.

Microb Ecol. 2017 May;73(4):954-965. doi: 10.1007/s00248-016-0901-y. Epub 2016 Dec 6.

PMID:
27924400
46.

(Z)-2-(3-Chlorobenzylidene)-3,4-dihydro-N-(2-methoxyethyl)-3-oxo-2H-benzo[b][1,4]oxazine-6-carboxamide as GSK-3β inhibitor: Identification by virtual screening and its validation in enzyme- and cell-based assay.

Joshi P, Gupta M, Vishwakarma RA, Kumar A, Bharate SB.

Chem Biol Drug Des. 2017 Jun;89(6):964-971. doi: 10.1111/cbdd.12913. Epub 2017 Feb 16.

PMID:
27896926
47.

Production of Gentisyl Alcohol from Phoma herbarum Endophytic in Curcuma longa L. and Its Antagonistic Activity Towards Leaf Spot Pathogen Colletotrichum gloeosporioides.

Gupta S, Kaul S, Singh B, Vishwakarma RA, Dhar MK.

Appl Biochem Biotechnol. 2016 Nov;180(6):1093-1109. Epub 2016 Jun 11.

PMID:
27288000
48.

Diapolic acid A-B from an endophytic fungus, Diaporthe terebinthifolii depicting antimicrobial and cytotoxic activity.

Yedukondalu N, Arora P, Wadhwa B, Malik FA, Vishwakarma RA, Gupta VK, Riyaz-Ul-Hassan S, Ali A.

J Antibiot (Tokyo). 2017 Feb;70(2):212-215. doi: 10.1038/ja.2016.109. Epub 2016 Sep 7. No abstract available.

PMID:
27599766
49.

Functional induction of P-glycoprotein efflux pump by phenyl benzenesulfonamides: Synthesis and biological evaluation of T0901317 analogs.

Padala AK, Wani A, Vishwakarma RA, Kumar A, Bharate SB.

Eur J Med Chem. 2016 Oct 21;122:744-755. doi: 10.1016/j.ejmech.2016.07.005. Epub 2016 Jul 6.

PMID:
27497733
50.

6-Aryl substituted 4-(4-cyanomethyl) phenylamino quinazolines as a new class of isoform-selective PI3K-alpha inhibitors.

Yadav RR, Guru SK, Joshi P, Mahajan G, Mintoo MJ, Kumar V, Bharate SS, Mondhe DM, Vishwakarma RA, Bhushan S, Bharate SB.

Eur J Med Chem. 2016 Oct 21;122:731-743. doi: 10.1016/j.ejmech.2016.07.006. Epub 2016 Jul 12.

PMID:
27479483

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