GVK Biosciences Private Ltd

Hyderabad andhra Pradesh, India

GVK Biosciences Private Ltd

Hyderabad andhra Pradesh, India

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Saha S.,GVK Biosciences Private Ltd | Saha S.,Jawaharlal Nehru University | Venkata Ramana Reddy C.,Jawaharlal Nehru University | Chiranjeevi T.,Jawaharlal Nehru Technological University Anantapur | And 4 more authors.
Bioorganic and Medicinal Chemistry Letters | Year: 2013

We have developed the first total syntheses of marine natural products ma'edamines A (18) and B (20). Structurally, they contain a pyrazine-2-(1H)-one core and were screened for antiproliferative activity on several cancer cell lines. Out of the six cell lines tested, ma'edamines A and B showed significant cytotoxicity against human colon cancer line COLO 205 (IC50 7.9 and 10.3 μM, respectively), breast cancer cell line MCF-7 (IC50: 6.9 and 10.5 μM, respectively) and human lung adenocarcinoma cell line A549 (IC50: 12.2 and 15.4 μM, respectively). The apoptotic effect of ma'edamines was confirmed by comet assay. Hence ma'edamines are likely to be useful as leads for development of a new class of anti-cancer agents. © 2012 Elsevier Ltd. All rights reserved.

Yanamandra M.,GVK Biosciences Private Ltd | Yanamandra M.,Jawaharlal Nehru University | Mitra S.,GVK Biosciences Private Ltd | Giri A.,Jawaharlal Nehru University
Expert Opinion on Drug Discovery | Year: 2015

Introduction: Phosphoinositide 3-kinases (PI3Ks) constitute one of the most important signaling pathways, playing a vital role in cellular differentiation and proliferation with a key function in cellular receptor triggered signal transduction downstream of tyrosine kinase receptors and/or G-protein coupled receptors. PI3K promotes cell survival proliferation, protein synthesis and glucose metabolism by generating secondary messengers phospholipid phosphatidyl 3,4,5-triphosphate and signaling via AKT/mTOR regulation. Deregulation of PI3K pathways have been observed in cancer, diabetes, neurological and inflammatory diseases and is an attractive target for pharmaceutical industries. Areas covered: In this review, the authors explain different PI3K assay methodologies. Furthermore, the authors summarize the techno-scientific principles and their utility in profiling novel chemical entities against PI3Ks. Specifically, the authors compare different PI3K assay formats explaining their mode of detection as well as their advantages and limitations for drug discovery efforts. Expert opinion: Developing lipid (PI3K) kinase assays involves significant effort and a rational understanding is needed due to the intrinsic lipidic nature of phospholipid phosphatidyl 4,5-biphosphate, which is used as an in vitro substrate for assays with PI3K isoforms. The assay of choice should be versatile, homogenous and definitely adaptable for high-throughput screening campaigns. Additionally, these assays are expected to dissect the mechanism of action of novel compounds (inhibitor characterization) against PI3K. Existing methods provide the versatility to medicinal chemists such that they can choose one or more assay platform to progress their compounds while profiling and/or inhibitor characterization. © 2014 Informa UK, Ltd.

Saha S.,GVK Biosciences Private Ltd | Saha S.,Jawaharlal Nehru University | Venkata Ramana Reddy C.,Jawaharlal Nehru University | Patro B.,GVK Biosciences Private Ltd
Tetrahedron Letters | Year: 2011

The synthesis of 4 and 8 is reported. These intermediates are obtained by a one-pot tandem cyclization of 1 and 6, respectively, via Bischler Napieralski reaction followed by cyclopropylimine rearrangement. Compounds 4 and 8 were reduced by sodium borohydride in methanol to afford cytotoxic alkaloid (±)-crispine A and antileishmania compound (±)-harmicine. © 2011 Elsevier Ltd. All rights reserved.

PubMed | GVK Biosciences Private Ltd and Temple University
Type: Journal Article | Journal: Bioorganic & medicinal chemistry letters | Year: 2016

Metabolic Syndrome, also referred to as Syndrome X or Insulin Resistance Syndrome, remains a major, unmet medical need despite over 30years of intense effort. Recent research suggests that there may be a causal link between this condition and abnormal glucocorticoid processing. Specifically, dysregulation of the hypothalamic-pituitary-adrenocortical (HPA) axis leads to increased systemic cortisol concentrations. Cushing syndrome, a disorder that is also typified by a marked elevation in levels of cortisol, produces clinical symptomology that is similar to those observed in MetS, and they can be alleviated by decreasing circulating cortisol concentrations. As a result, it has been suggested that decreasing systemic cortisol concentration might have a positive impact on the progression of MetS. This could be accomplished through inhibition of enzymes in the cortisol synthetic pathway, 11-hydroxylase (Cyp11B1), 17-hydroxylase-C17,20-lyase (Cyp17), and 21-hydroxylase (Cyp21). We have identified a series of novel sulfonamide analogs of (2S,4R)-Ketoconazole that are potent inhibitors of these enzymes. In addition, selected members of this class of compounds have pharmacokinetic properties consistent with orally delivered drugs, making them well suited to further investigation as potential therapies for MetS.

Saha S.,GVK Biosciences Private Ltd | Saha S.,University of Hyderabad | Reddy C.V.R.,University of Hyderabad | Xu S.,University of Southern California | And 3 more authors.
Bioorganic and Medicinal Chemistry Letters | Year: 2013

The synthesis of several analogues of ma'edamines A and B are reported. The synthesized compounds were tested on hormone receptor positive and HER2 positive breast cancer cell lines, by MTT assay. MED-114, 115, 117, 119, 120, 124, 128 and 131 were found to be equally active as Lapatinib on HER2 +ve cell line SKBR3. © 2013 Elsevier Ltd. All rights reserved.

Sanaboina C.,GVK Biosciences Private Ltd | Sanaboina C.,Sreenidhi Institute of Science and Technology Autonomous | Jana S.,GVK Biosciences Private Ltd | Chidara S.,GVK Biosciences Private Ltd | And 3 more authors.
Tetrahedron Letters | Year: 2012

Synthesis of indole alkaloid related compounds using Schiff base formation, intramolecular cyclization (or N-alkylation), and Pictet-Spengler reaction as a cascade one pot condensation has been reported. The cascade chemistry has been applied to the synthesis of (±)-harmicine as a key step. © 2012 Elsevier Ltd. All rights reserved.

Sorra K.,GVK Biosciences Private Ltd | Sorra K.,Jawaharlal Nehru Technological University Anantapur | Mukkanti K.,Jawaharlal Nehru Technological University Anantapur | Pusuluri S.,GVK Biosciences Private Ltd
Tetrahedron | Year: 2012

A concise synthesis of enantiopure quinazolino [1,4] benzodiazepine was accomplished by palladium-catalyzed N-arylation of amidines with o-bromobenzoates followed by intra molecular cyclization. The strategy was successfully applied to the total synthesis of pyrrolo quinazolino [1,4] benzodiazepine alkaloids such as circumdatin H, J and other analogues. © 2011 Elsevier Ltd. All rights reserved.

Chowdhury A.R.,Johns Hopkins Hospital | Chowdhury A.R.,GVK Biosciences Private Ltd | Bakshi R.,Johns Hopkins Hospital | Wang J.,Johns Hopkins Hospital | And 9 more authors.
PLoS Pathogens | Year: 2010

Introduced in the 1950s, ethidium bromide (EB) is still used as an anti-trypanosomal drug for African cattle although its mechanism of killing has been unclear and controversial. EB has long been known to cause loss of the mitochondrial genome, named kinetoplast DNA (kDNA), a giant network of interlocked minicircles and maxicircles. However, the existence of viable parasites lacking kDNA (dyskinetoplastic) led many to think that kDNA loss could not be the mechanism of killing. When recent studies indicated that kDNA is indeed essential in bloodstream trypanosomes and that dyskinetoplastic cells survive only if they have a compensating mutation in the nuclear genome, we investigated the effect of EB on kDNA and its replication. We here report some remarkable effects of EB. Using EM and other techniques, we found that binding of EB to network minicircles is low, probably because of their association with proteins that prevent helix unwinding. In contrast, covalently-closed minicircles that had been released from the network for replication bind EB extensively, causing them, after isolation, to become highly supertwisted and to develop regions of left-handed Z-DNA (without EB, these circles are fully relaxed). In vivo, EB causes helix distortion of free minicircles, preventing replication initiation and resulting in kDNA loss and cell death. Unexpectedly, EB also kills dyskinetoplastic trypanosomes, lacking kDNA, by inhibiting nuclear replication. Since the effect on kDNA occurs at a.10-fold lower EB concentration than that on nuclear DNA, we conclude that minicircle replication initiation is likely EB's most vulnerable target, but the effect on nuclear replication may also contribute to cell killing. ©2010 Roy Chowdhury et al.

Vegi S.R.,GVK Biosciences Private Ltd | Vegi S.R.,Jawaharlal Nehru Technological University Anantapur | Boovanahalli S.K.,GVK Biosciences Private Ltd | Patro B.,GVK Biosciences Private Ltd | Mukkanti K.,Jawaharlal Nehru Technological University Anantapur
European Journal of Medicinal Chemistry | Year: 2011

We report herein an efficient enantioselective synthesis of SPF32629A and SPF32629B through one-pot enantioselective reduction and protecting-group-free regioselective O-acylation strategy. The absolute configuration of the enantiomerically pure isomers was established by Mosher ester analysis. The inhibitory potencies of the synthesized compounds were assayed in vitro against a panel of microorganisms and against A549 human lung adenocarcinoma cell line. Compounds 2, 11 and 12 displayed moderate to potent antibacterial activity against all the tested strains and compounds 7, 8, 2, 11 and 12 exhibited significant cytotoxicity in a dose-dependent manner with an IC 50 values ranging from 2.92 to 4.14 μg/ml and 8-11 μM. © 2011 Elsevier Masson SAS. All rights reserved.

Sorra K.,GVK Biosciences Private Ltd | Sorra K.,Jawaharlal Nehru Technological University Anantapur | Mukkanti K.,Jawaharlal Nehru Technological University Anantapur | Pusuluri S.,GVK Biosciences Private Ltd
Synthesis (Germany) | Year: 2014

The first total synthesis of (-)-auranomide C has been achieved. The short synthetic strategy involves a reductive dehydrocyclization and the nucleophilic ring opening of a fused γ-lactam. The route allows for ease in synthesizing diverse derivatives in the side chain of the natural product. © 2014 Georg Thieme Verlag Stuttgart New York.

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