scispace - formally typeset
Search or ask a question
Author

S. Reddy

Bio: S. Reddy is an academic researcher from Sri Venkateswara University. The author has contributed to research in topics: Triethylamine & Tetrahydrofuran. The author has an hindex of 4, co-authored 16 publications receiving 59 citations.

Papers
More filters
Journal ArticleDOI
TL;DR: The novel phosphorylated derivatives of Lamivudine (5a-5l) as potential anti colon cancer agents are synthe- sized and among them 5a and 5b emerged as lead compounds with 0.003 μM and 0.0001 μM values.
Abstract: The novel phosphorylated derivatives of Lamivudine (5a-5l) as potential anti colon cancer agents are synthe- sized. These title compounds are designed based on the basic pyrimidine derivative lamivudine as a starting compound and reacted with various phosphorodichloridates followed by the introduction of bioactive groups at the phosphorus. Their structures were characterized by IR, 1 H, 13 C, 31 P NMR and mass spectral analyses. All the compounds were evaluated for their anti colon cancer activity against COLO-205 cell lines in vitro studies. Among them 5a and 5b emerged as lead compounds with 0.003 μM and 0.0001 μM values.

29 citations

Journal ArticleDOI
TL;DR: In this article, the synthesis of 9-substituted naphthalene-9-sulfides/selenides (4,e] naph-thien-naph) was accomplished in three steps.
Abstract: Synthesis of 9-substituted-8, 9 10, 11-tetrahydro-7H-7, 11-diaza-9λ5-phosphacycloocta [d,e] naphthalene-9-sulfides/selenides (4–13) was accomplished in three steps. 1,8-diamino naphthalene (2) was reacted with tris (bromomethyl) phosphine (1) in the presence of triethylamine in dry tetrahydrofuran (THF) under N2 atmosphere to form the corresponding intermediate (3). It was converted to the corresponding sulfide (4) and selenide (5) by the reaction with sulfur and selenium, respectively. The intermediates 4 and 5 were reacted with two achiral alcohols and two achiral amines to obtain the title compounds (6–13). The structures of the title compounds were established by elemental analysis and spectral data (IR, 1H, 13C, 31P NMR, and FAB mass). The antimicrobial activity of these compounds was evaluated and they exhibited significant activity. Synthesis, spectral and antimicrobial evaluation of some new 8-membered phosphorus heterocyclic compounds

7 citations

Journal ArticleDOI
TL;DR: Iminophosphocins 8a-8e and 9a-9e were synthesized in four-step reactions via Staudinger reaction 3-(Bromomethyl)-1,2,3,4,5-pentahydro-3λ5-naphtho[1,8-f,g][1,5,3]diazaphosphocin-3-one (3) as mentioned in this paper.
Abstract: Iminophosphocins 8a–8e and 9a–9e were synthesized in four-step reactions via Staudinger reaction 3-(Bromomethyl)-1,2,3,4,5-pentahydro-3λ5-naphtho[1,8-f,g][1,5,3]diazaphosphocin-3-one (3) was prepared by reacting tris(bromomethyl)phosphineoxide (1) with 1,8-diaminonaphthalene (2) in the presence of triethylamine (TEA) in dry tetrahydrofuran (THF), and treated with L-valine methyl ester (4) and bis(2-chloroethyl)amine (5) in the presence of TEA in dry THF to get 3-methyl-2-[(3-oxo-1,2,3,4,5-pentahydro-3λ5-naphtho[1,8-f,g][1,5,3]diazaphosphocin-3-yl)methylamino]butanoate (6) and 3-[di(2-chloroethyl)aminomethyl]-1,2,3,4,5-pentahydro-3λ5- naphtho[1,8-f,g][1,5,3]diazaphosphocin-3-one (7) The compounds 6 and 7 were treated with trichlorosilane (SiCl3H) in dry tetrahydrofuran (THF) to form the trivalent P(III) intermediates 8 and 9, which were further treated with various alkyl azides in dry THF in 55–60°C to afford the title compounds 8a–8e and 9a–9e Their structures were established by multi-nuclear NMR and mass spectra All the newly synthesized compounds were found to possess moderate anti-microbial activity

6 citations

Journal ArticleDOI
TL;DR: In this article, ribavirin 5-16 was synthesized by the reaction of 4-nitrophenyl phosphorodichloridate with various amino acid esters in the presence of triethylamine in dry tetrahydrofuran through the inter- mediates 3.
Abstract: Novel phosphorylated derivatives of ribavirin 5-16 were synthesized by the reaction of 4-nitrophenyl phosphorodichloridate with various amino acid esters in the presence of triethylamine in dry tetrahydrofuran through the inter- mediates 3. On further reaction of 3 with ribavirin in THF and pyridine in the presence of TEA afforded the title compounds 5-16. Their structures were characterized by IR, 1 H, 13 C, 31 P NMR and mass spectral analyses. All the title compounds were found to exhibit potent in vitro anticancer activity against MCF-7 breast cancer cell lines.

6 citations

Journal Article
TL;DR: In this paper, the synthesis of α-aminophosphonic acid esters (3a-l ) was accomplished by the reaction of equimolar quantities of phenyl ethyl glycine and various aryl aldehydes with diethyl/dimethylphosphite in dry toluene at reflux temperature.
Abstract: Synthesis ofnew-aminophosphonic acid esters ( 3a–l ) was accomplished by the reaction of equimolar quantities of phenyl ethyl glycine and various aryl aldehydes with diethyl/ dimethylphosphite in dry toluene at reflux temperature. All the structures of the newly synthesized α-aminophosphonic acid esters ( 3a–l ) were established by elemental analysis, and IR, 1 H, 13 C, 31 P NMR and mass spectral data. The antimicrobial and antifungal activities of these compounds were evaluated and they exhibited significant activity. Keywords: Phenyl glycine ethyl ester, aryl aldehydes, diethyl/dimethylphosphite, antimicrobial activity

4 citations


Cited by
More filters
Book
01 Jan 1974

439 citations

Journal ArticleDOI
TL;DR: For many decades, the design of new nucleoside analogs as potential therapeutic agents focused on both sugar and nucleobase modifications, but now nucleosides triphosphates cannot be considered as viable drug candidates as they usually have poor chemical stability along with high polarity that hinders them from transporting across cell membranes.
Abstract: For many decades, the design of new nucleoside analogs as potential therapeutic agents focused on both sugar and nucleobase modifications. These nucleoside analogs rely on cellular kinases to undergo stepwise addition of phosphate groups to form the corresponding active nucleoside triphosphate to express their therapeutic effect.1 However, nucleosides triphosphates cannot be considered as viable drug candidates as they usually have poor chemical stability along with high polarity that hinders them from transporting across cell membranes. Within the nucleoside analog phosphate activation process, the first phosphorylation has often been identified as the limiting step, which led medicinal chemists to prepare stable “protected” monophosphate nucleosides capable of delivering nucleoside monophosphates intracellularly. These nucleoside monophosphate prodrugs are designed to efficiently cross the biological barriers (as opposed to nucleoside monophosphates; Figure ​Figure1,1, eq 1) and reach the targeted cells or tissues. Once inside the cell, the biolabile protecting groups are then degraded enzymatically and/or chemically, releasing the free nucleoside analog in the monophosphate form, which can often efficiently express its therapeutical potency by intracellular conversion to the corresponding nucleoside triphosphate (Figure ​(Figure1,1, eq 2). Open in a separate window Figure 1 Mechanism of action of nucleoside monophosphate prodrugs.

420 citations

Journal ArticleDOI
TL;DR: In this paper, a 3D finite element model capable of predicting the velocity, pressure, and temperature fields, as well as the position of the flow fronts is presented, which can be used to optimize the part design and molding conditions.
Abstract: During the molding of industrial parts using injection molding, the molten polymer flows through converging and diverging sections as well as in areas presenting thickness and flow direction changes. A good understanding of the flow behavior and thermal history is important in order to optimize the part design and molding conditions. This is particularly true in the case of automotive and electronic applications where the coupled phenomena of fluid flow and heat transfer determine to a large extent the final properties of the part. This paper presents a 3D finite element model capable of predicting the velocity, pressure, and temperature fields, as well as the position of the flow fronts. The velocity and pressure fields are governed by the generalized Stokes equations. The fluid behavior is predicted through the Carreau Law and Arrhenius constitutive models. These equations are solved using a Galerkin formulation. A mixed formulation is used to satisfy the continuity equation. The tracking of the flow front is modeled by using a pseudo-concentration method and the model equations are solved using a Petrov-Galerkin formulation. The validity of the method has been tested through the analysis of the flow in simple geometries. Its practical relevance has been proven through the analysis of an industrial part.

86 citations

Journal ArticleDOI
TL;DR: In vitro kinase profiling revealed that 7x is a multikinase inhibitor with potent inhibitory activity against the CDK4/CYCLIN D1 and ARK5 kinases, and the synthesis, structure–activity relationship, kinase inhibitory profile, in vitro cytotoxicity, and in vivo tumor regression studies by this lead compound are reported.
Abstract: The success of imatinib, a BCR-ABL inhibitor for the treatment of chronic myelogenous leukemia, has created a great impetus for the development of additional kinase inhibitors as therapeutic agents. However, the complexity of cancer has led to recent interest in polypharmacological approaches for developing multikinase inhibitors with low toxicity profiles. With this goal in mind, we analyzed more than 150 novel cyano pyridopyrimidine compounds and identified structure-activity relationship trends that can be exploited in the design of potent kinase inhibitors. One compound, 8-cyclopentyl-2-[4-(4-methyl-piperazin-1-yl)-phenylamino]-7-oxo-7,8-dihydro-pyrido[2,3-d]pyrimidine-6-carbonitrile (7x), was found to be the most active, inducing apoptosis of tumor cells at a concentration of approximately 30-100 nM. In vitro kinase profiling revealed that 7x is a multikinase inhibitor with potent inhibitory activity against the CDK4/CYCLIN D1 and ARK5 kinases. Here, we report the synthesis, structure-activity relationship, kinase inhibitory profile, in vitro cytotoxicity, and in vivo tumor regression studies by this lead compound.

66 citations

Journal ArticleDOI
TL;DR: These new structurally diversified set of α-aminophosphonates (4a-j) were evaluated for their anti-tumor activity on human chronic myeloid leukemia cells, human colon carcinoma cells along with non-cancerous human embryonic kidney cells.

63 citations