Jyoti Wadekar

Dr. Vithalrao Vikhe Patil Foundation's College of Pharmacy, Vilad Ghat, Ahmednagar

Background: Cancer is a leading cause of death worldwide. Inhibiting mitosis is the most effective clinical technique for cancer treatment. The most critical field of medicinal chemistry and drug development research is the discovery of innovative anticancer drugs. Thiazolidine is a multifunctional nucleus with anticancer, anti-inflammatory, antiox...

Cancer is a major cause of death all over the globe. Controlling cell division by inhibition of mitosis is the most successful clinical strategy for cancer treatment. The development of novel anticancer agents is the most important area in medicinal chemistry and drug discovery research. Thiazolidine is the multifunctional nucleus which shows a num...

Introduction : Cancer is a major cause of death all over the globe. Controlling cell division by inhibition of mitosis is the most successful clinical strategy for cancer treatment. The development of novel anticancer agents is the most important area in medicinal chemistry and drug discovery research. Thiazolidine is the multifunctional nucleus,...

Polo-like kinase 1(Plk1) plays an essential role in inhibiting cell proliferation and comes under the family of serine/threonine-protein kinase, which is a particular target for cancer therapy. In some clinical studies, Plk1 has been identified as a target for cancer. Currently, so many scientists are developing the Plk1 inhibitors, and they are th...

Background Plumeria obtusa L. (Apocynaceae) is a deciduous, ornamental, tropical plant grown in premises, parks, gardens, graveyards, because of its attractive and fragrant flowers. The different parts of the plant are used traditionally to treat various diseases like diabetes mellitus, wounds and skin disease, diuretic, purgative, abortion and als...

Background: Cancer is a major cause of death all over the globe. Controlling cell division byinhibition of mitosis is the most successful clinical strategy for cancer treatment. The developmentof novel anticancer agents is the most important area in medicinal chemistry and drug discoveryresearch. Thiazolidine is the multifunctional nucleus which sh...

Molecular docking studies of 1, 3- thiazolidin-4-ones as potential human polo like kinase 1 (plk 1) inhibitors

Polo-like kinase 1 (Plk1) belongs to a subfamily of Ser/ Thr protein kinases, collectively termed polo-like kinases (Plks). A growing body of evidence suggests that Plk1 plays important roles during multiple stages of M-phase progression and, as a result, in cell proliferation. In a series of preclinical studies, PLK1 has been validated as a cancer...

Salacia oblonga wall, a native shrub, also known as Saptrangi and Ponkoranti, belongs to the family Celastraceae, is distributed across the world. A large number of chemical constituents such as salacinol, kotalanol, neokotalanol, neosalacinol, and mangiferin are isolated from S. oblonga, which show various pharmacological activities. Salacia oblon...

Structural requirements of 1, 3- thiazolidin-4 one to inhibit polo like kinase 1 (plk 1) as anticancer agents.

A series of thiazolidine derivatives were designed by docking into PPAR-γ active site. The structure of target was obtained from the protein data bank (PDB ID P37231). A library of 200 molecules was prepared on random basis. Molecular docking studies were performed using VLife MDS 4.3 software. After molecular docking studies, the 4-substituted-6-m...

A library of 900 pyrimidine derivatives was screened virtually on vascular endothelial growth factor (VEGF) using Vlife MDS 4.1 software to identify potential candidates with anticancer and anticataract activity. A series of 2,4,6-substituted pyrimidine derivatives were synthesized in good yields from chalcones, where chalcones have been prepared a...

Dalbergia sissoo belonging to family Fabaceae is a widely growing plant and has been reported to possess multiple therapeutic properties like analgesic, anti-inflammatory, analgesic and antipyretic anti-ulcer, antioxidant, anthelmintic, antimicrobial, antidiabetic and is also used to treat syphilis, dysentery, nausea, eye and nose disorder, skin di...

Calotropia gigantea (Asclcpiadacae) is widely growing plant and has been reported to possess multiple therapeutic properties like anti-pyretic, analgesic, anticonvulsant, anxiolytic, sedative, wound healing and antidiabetic. Chemical investigation of Calotropis gigantea report isolation of different type of photochemicals such as flavonoid, glycosi...

Lawsonia inermis L. is a branched glabrous shrub or small tree, cultivated for its leaves although stem bark, roots, flowers and seeds have also been used in traditional medicine. In the present study anticonvulsant, anthelmintic and antibacterial activity of chloroform, ethanol and water extract of Lawsonia inermis has been carried out. Anticonvul...

Rheumatoid Arthritis (RA) is a chronic autoimmune disease of unknown aetiology that affects 0.5% of the population and can result in disability owing to joint destruction, characterized by joint synovial inflammation and progressive cartilage and bone destruction resulting in gradual immobility. The greatest disadvantage in the presently available...

In continuation with our research program, in search of potent enzyme tyrosinase inhibitor, a series of synthesized 2,5-disubstituted 1,3,4-oxadiazoles have been evaluated for enzyme tyrosinase inhibitory activity. Subsequently, 3D QSAR and docking studies were performed to find optimum structural requirements for potent enzyme tyrosinase inhibitor...

A new series of Schiff bases of 1, 3-oxazines were synthesized in three steps. In the first step, 4- bromoacetophenone and substituted aromatic aldehyde reacted in the presence of sodium hydroxide to give substituted chalcones (Claisen-Schmidt condensation). In second step, substituted chalcones reacted with urea to produce 4-(4-bromophenyl)-6-(sub...

Twenty-six different benzylidene oxazolo/thiazolo (3,2-a)-pyrimidine-6-carboxamide derivatives were synthesized and evaluated for their anti-inflammatory potential by protein denaturation method. The structures of title compounds were characterized by IR and NMR spectral data. The SAR studies reveal that compounds containing electron withdrawing po...

Development of new antibacterial agents is increasingly important due to the resistance of microbes to the known antibacterial drugs. A series of benzylidene oxazolo/thiazolo (3,2-a)-pyrimidine-6- carboxamides were synthesized by condensing 2-oxo/thioxo-1,2,3,4-tetrahydropyrimidine carboxamides with various aromatic aldehydes. The structures of new...

A series of Schiff bases of 1, 3-oxazines were synthesized via reaction of 1, 3-oxazine-2-amine with substituted benzaldehyde. The title compounds (3a-3r) were characterized with IR, NMR and screened for their anticoagulant activity by measuring prothombin time by Quick's method. The study revealed that most of the synthesized compounds exhibited s...

The purpose of the present work was to select substituents by using Topliss modified approach to synthesize new 1,3 oxazines with antimicrobial effect. In the series of 6-[4-substitutedphenyl]-4-phenyl-6H-1,3-oxazin-2-amines and N-[6-(4-substitutedphenyl)-4-phenyl-6H-1,3-oxazinyl] acetamides, substituents at fourth position of the phenyl ring were...

A series of 2-methylthio-1,4-dihydropyrimidine derivatives (IIa–IIl) were synthesized in good yields by alkylation of 1,2,3,4-tetrahydropyrimidines (Ia–Il) with methyl iodide in the presence of pyridine. Their structures were confirmed by elemental analysis, IR, and 1H NMR spectra. Molecular docking of title compounds was done using VLife MDS 3.5 o...

A series of structurally similar isatin analogues with antitubercular activity have been subjected for 2D and 3D QSAR analysis using V life MDS 3.5 software. The compounds were divided into training and test set of 44 and 11 each. Best QSAR models were selected on the basis of various statistical parameters like square correlation coefficient (r2),...

Present work describes the potent antidiabetic fraction from flowers of Cassia auriculata Linn. Hydromethanolic extract along with its ethyl acetate and n-butanol fractions were evaluated for antidiabetic activity in alloxan-induced diabetes in rats. The n-butanol fraction exhibited significant reduction (p<0.001) in blood glucose levels and was al...