Design and synthesis of caffeoyl-anilides as portmanteau inhibitors of HIV-1 integrase and CCR5

Bodiwala, Hardik S.; Sabde, Sudeep; Gupta, Pawan; Mukherjee, Ruchira; Kumar, Rajender; Garg, Prabha; Bhutani, K. K.; Mitra, Debashis; Singh, Inder Pal

doi:10.1016/j.bmc.2010.12.031

Cited by 19 publications

(10 citation statements)

References 48 publications

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“…In fact, assays for detecting anti‐HIV activity utilized in the recent years by many authors actually involve CEM‐GFP as target cells. However, p24 release in supernatants [Ahmed et al, ; Brahmbhatt et al, ; Chauthe et al, ; Bodiwala et al, , ], fluorimetric detection of the absorbance of the samples in black optiplate [Kumari et al, ], both these two [Gruber et al, ; Modi et al, , ] or fluorescence values expressed as mean fluorescence intensity [Gruber et al, ], but in no case % of GFP positive cells, were used to calculate IC 50 values. Thus, all the above‐mentioned methods do not give information on number/percentage of cells in which HIV‐1 replication is impeded by the drug.…”

Section: Discussionmentioning

confidence: 99%

“…Following infection, the effect of HIV‐Tat on HIV‐LTR was responsible for GFP up‐regulation [Ramautar et al, ]. Several recent reports demonstrated that variants of this method could be useful to investigate the effects of compounds on HIV infection [Gruber et al, ; Ahmed et al, ; Brahmbhatt et al, ; Chauthe et al, ; Bodiwala et al, , ; Kumari et al, ; Modi et al, , ]. Surprisingly, however, inhibition of infection in no case was evaluated by flow cytometry analysis, expressed as % of GFP positive cells.…”

Section: Introductionmentioning

confidence: 99%

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Testing anti‐HIV activity of antiretroviral agents in vitro using flow cytometry analysis of CEM‐GFP cells infected with transfection‐derived HIV‐1 NL4‐3

Frezza

Grelli

Federico

et al. 2015

Journal of Medical Virology

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An assay, specifically optimized to evaluate the anti-HIV activity of antiretrovirals by flow cytometry analysis, is described. As widely used anti-HIV agents, zidovudine (AZT), abacavir (ABC), 2',3'-dideoxyinosine (DDI), lamivudine (3TC), nevirapine (NVP), and efavirenz (EFV), and as drugs of recent approval raltegravir (RAL), etravirine (ETR), and rilpivirine (RPV), were utilized as reference drugs. HIV-1 NL4-3 virus was prepared by transfection of HEK293T cells with purified plasmid DNA and quantified by p24 antigen-capture assay. For infection, CEM-GFP cells were exposed to vehicle or to several concentrations of the drugs for 2 hr at 37 °C before HIV-1 NL4-3 was added to each sample. The adsorption was prolonged for 3 hr at 37 °C. After 72 hr of incubation, HIV-induced GFP expression in infected CEM-GFP cells was assessed by flow cytometry analysis and expressed as % positive cells. For comparison, p24 production in supernatants was assessed by a commercial ELISA kit. On the basis of IC50 values, the anti-HIV activity, as assayed by this method, was EFV > 3TC > AZT > NVP > DDI > ABC and ETR > RPV > RAL. The comparison between the IC50 values calculated through flow cytometry and p24 production revealed overlapping results, showing that the optimized protocol of CEM-GFP infection with HIV NL4-3 is a suitable method to perform quantitative, rapid and low-expensive screening tests to evaluate the in vitro effect of new candidate anti-HIV drugs.

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Section: Discussionmentioning

confidence: 99%

Section: Introductionmentioning

confidence: 99%

Testing anti‐HIV activity of antiretroviral agents in vitro using flow cytometry analysis of CEM‐GFP cells infected with transfection‐derived HIV‐1 NL4‐3

Frezza

Grelli

Federico

et al. 2015

Journal of Medical Virology

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“…The basic focus of all gene recognition algorithm is to measure a 'typical ' exonic DNA which is responsible for the building of protein. Bioinformatics is the emerging field with the requirement of managing and extracting a huge amount of information which can be used in solving many common problems, especially related to drug design [4,5]. Three research communities mainly Biologists, Mathematicians and Computer Scientists joined their hands to solve these interesting problems.…”

Section: Literature Surveymentioning

confidence: 99%

Splice Site Recognition Using Lower Dimensional LHMM Features and SVM Classifier

Sahu¹

2017

IJRASET

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“…One emerging strategy in the development of new drugs involves combining key pharmacophores from existing natural products to generate novel chimeric compounds with improved biological properties. [45][46][47][48][49]…”

Section: Introductionmentioning

confidence: 99%

Design, synthesis and antiproliferative activity of urocanic-chalcone hybrid derivatives

et al. 2011

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Inspired by biologically active natural products, a hybrid analogue that combines the N-Me urocanic side chain of the sarcodictyin family of compounds with the chalcone motif has been proposed, synthesised and examined for antiproliferative activity in three cancer cell lines and one normal primary cell line. The analogues are all synthesised in one or two steps from commercially available materials and, of the compounds examined, the proposed hybrid analogue displays the most active and selective inhibition of cell proliferation in human colon cancer cell line HT29 (IC 50 2.9 µM) and highly metastatic human breast carcinoma MDA-MB-231 (IC 50 4.8 µM).

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Design and synthesis of caffeoyl-anilides as portmanteau inhibitors of HIV-1 integrase and CCR5

Cited by 19 publications

References 48 publications

Testing anti‐HIV activity of antiretroviral agents in vitro using flow cytometry analysis of CEM‐GFP cells infected with transfection‐derived HIV‐1 NL4‐3

Testing anti‐HIV activity of antiretroviral agents in vitro using flow cytometry analysis of CEM‐GFP cells infected with transfection‐derived HIV‐1 NL4‐3

Splice Site Recognition Using Lower Dimensional LHMM Features and SVM Classifier

Design, synthesis and antiproliferative activity of urocanic-chalcone hybrid derivatives

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