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Cicenas J.,Swiss Institute of Bioinformatics | Cicenas J.,Vilnius University | Kalyan K.,MAP Kinase Resource | Kalyan K.,Haffkine Institute for Training Research and Testing | And 5 more authors.
Cancers | Year: 2014

Uncontrolled proliferation is the hallmark of cancer and other proliferative disorders and abnormal cell cycle regulation is, therefore, common in these diseases. Cyclin-dependent kinases (CDKs) play a crucial role in the control of the cell cycle and proliferation. These kinases are frequently deregulated in various cancers, viral infections, neurodegenerative diseases, ischemia and some proliferative disorders. This led to a rigorous pursuit for small-molecule CDK inhibitors for therapeutic uses. Early efforts to block CDKs with nonselective CDK inhibitors led to little specificity and efficacy but apparent toxicity, but the recent advance of selective CDK inhibitors allowed the first successful efforts to target these kinases for the therapies of several diseases. Major ongoing efforts are to develop CDK inhibitors as monotherapies and rational combinations with chemotherapy and other targeted drugs. © 2014 by the authors; licensee MDPI, Basel, Switzerland. Source

Mahajan P.,Dr. Babasaheb Ambedkar Marathwada University | Nikam M.,Dr. Babasaheb Ambedkar Marathwada University | Chate A.,Dr. Babasaheb Ambedkar Marathwada University | Nimbalkar U.,Dr. Babasaheb Ambedkar Marathwada University | And 6 more authors.
Phosphorus, Sulfur and Silicon and the Related Elements | Year: 2015

A series of newer 1,3,4-oxadiazole derivatives 3a-h, 5a-h containing a thiophene fused with pyrazole moiety of pharmacological significance have been synthesized. The compounds were characterized by 1H NMR, IR, and mass spectral techniques. The compounds were screened for their in vitro antioxidant, anti-inflammatory and antimicrobial activities. Among them, Compounds 3b (EC50-14.98) and 3f (EC5012.21) showed significant antioxidant activity. Compound 3a (EC50-15.23) showed good anti-inflammatory activity. Compound 3d was found as the most active derivative against bacterial and fungal strains. © 2015 Taylor and Francis Group, LLC. Source

Rohan K.N.,Haffkine Institute for Training Research and Testing | Sweta K.T.,Haffkine Institute for Training Research and Testing | Abhay C.S.,Haffkine Institute for Training Research and Testing
European Journal of Pharmaceutical Sciences | Year: 2014

Delivering a safe and effective topical vaginal contraceptive is the need of present era. We explored the potential of a metal (copper) and herbal moiety (curcumin) for this topical contraceptive prophylaxis. Complex of copper and curcumin (Cu-Cur) was synthesized and the concerns regarding its aqueous solubility was resolved by including it into the hydrophobic cavity of β-cyclodextrin (β-CD) as (Cu-Cur)CD inclusion complex. Dose assessment was made on the basis of in-vitro spermicidal assays and cell cytotoxicity studies. Finally the (Cu-Cur)CD loaded vaginal gel was prepared, characterized and evaluated for in-vitro spermicidal activity and preclinical toxicity studies. Spectral and morphological characterizations confirmed the synthesis of (Cu-Cur) and (Cu-Cur)CD inclusion complex. Spermicidal assays and Hela cell cytotoxic data revealed an optimized 1.5% (Cu-Cur)CD for further studies. 1.5% w/w (Cu-Cur)CD loaded carbopol 974p gel provided 100% motility even at 2-fold dilution and preclinical toxicity studies in Rats and Rabbits revealed its highly safe profile. The hypothesis of considering metal-herbal complex and its cyclodextrin complex has worked and the well planned strategy of including it in (β-CD) cavity provided a preeminent platform for vaginal delivery. In-vitro assays and preclinical toxicity analysis confirmed its potential to be used as highly safe and effective prophylaxis. ©2014 Elsevier Ltd. All rights reserved. Source

Kalyan K.,Haffkine Institute for Training Research and Testing | Jakhia B.,Haffkine Institute for Training Research and Testing | Lele R.D.,Haffkine Institute for Training Research and Testing | Lele R.D.,Jaslok Hospital and Research Center | And 2 more authors.
Advances in Bioinformatics | Year: 2014

The preliminary study presented within this paper shows a comparative study of various texture features extracted from liver ultrasonic images by employing Multilayer Perceptron (MLP), a type of artificial neural network, to study the presence of disease conditions. An ultrasound (US) image shows echo-texture patterns, which defines the organ characteristics. Ultrasound images of liver disease conditions such as "fatty liver," "cirrhosis," and "hepatomegaly" produce distinctive echo patterns. However, various ultrasound imaging artifacts and speckle noise make these echo-texture patterns difficult to identify and often hard to distinguish visually. Here, based on the extracted features from the ultrasonic images, we employed an artificial neural network for the diagnosis of disease conditions in liver and finding of the best classifier that distinguishes between abnormal and normal conditions of the liver. Comparison of the overall performance of all the feature classifiers concluded that "mixed feature set" is the best feature set. It showed an excellent rate of accuracy for the training data set. The gray level run length matrix (GLRLM) feature shows better results when the network was tested against unknown data. © 2014 Karthik Kalyan et al. Source

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