Progress in Copper Complexes as Anticancer Agents

The advent of targeted therapies, i.e., small molecules or antibodies that interfere with signaling proteins involved in the etiology of cancer, revolutionized thetreatment of tumors with an addiction to specific oncogenes (e.g., ALK in lung cancer, Bcr-Abl in chronic myeloid leukemia, KIT in GIST, EGFR in lung cancer, HER2 in breast cancer or MET in liver tumors). However, for many cancers, the progressionfree survival of patients treated with targeted therapy is less than one year, which justify for a regain of interest in cytotoxic agents including metallodrugs. 

Indeed, the prevalent success of cisplatin in the treatment of various types of cancers has placed organometallic compounds on the forefront in the development of anticancer drugs. In this quest, copper derivatives hold promising opportunities due to opportunities provided by the hypoxic environment that is a hallmark of cancer cells coupled with the ability of copper complexes to catalyze the formation of Reactive Oxygen and Nitrogen species (ROS and RNS).(Read More)

Synthesis of Cholic Acid-Peptide Conjugates With A Negatively Charged Ester Linkage for Oral Delivery

Advances in biotechnology have provided a wide range of therapeutically active and commercially available biologic large molecules as protein and peptide drugs. However, oral administration of these drugs has been highly limited due to the stability and the difficulties to cross the gastrointestinal membrane. Significant research attempts have been made in recent years to utilize carrier-mediated transport systems for enhancement in the oral bioavailability. Among various intestinal transporters, the intestinal bile acid transporter has a good potential because of its higher capacity and low structural selectivity. The transport system facilitates the daily absorption of 10-20 g bile salts at a more than 95% efficiency rate. 

The system also tolerates significant chemical modifications at the C3 and C24 positions of the sterol nucleus. Thus, the intestinal bile acid transporter has been specifically investigated for its ability to increase the oral absorption of cholic acid conjugates of proteins and small peptides through the carrier-mediated transport mechanism. The fact that the bile acid transporter tolerates the chemical modifications of cholic acid provides a solid rationale for the development of a cholic acid-peptide conjugate for enhanced oral absorption.

Potentiometric and pHmetric Studies of Paracetamol

Paracetamol (acetaminophen) is one of the most popular analgesic and antipyretic drugs. Paracetamol is available in different dosage forms: tablet, capsules, drops, elixirs, suspensions and suppositories. Dosage forms of paracetamol and its combinations with other drugs have been listed in various pharmacopoeias. The combination of paracetamol with dipyrone is used asan antipyretic, analgesic and anti-inflammatory drug. Numerous methods have been reported for the analysis of paracetamol and its combinations in pharmaceuticals or in biological fluids. Paracetamol has been determined in combination with other drugs using titrimetry, voltammetry, fluorimetry, colorimetry, UV-spectrophotometry, quantitative thin-layer chromatography (TLC), high-performance liquid chromatography (HPLC) and gas chromatography (GC) in pharmaceutical preparations. 

Effect of electrophilic and electrodotic groups on the potentiometric titration of amides and other weak bases was studied. Electrodotic groups enhance the potentiometric end point and electrophilicgroups depress it, sometimes to the extent that the compound is not titratable. A combination of chloroform and acetic anhydride is a useful alternative medium for the titration of weak bases. A potentiometric method for determination of p-acetamidophenol was reported.

Conducting Polymers in Biological Systems

Electronics based on π-conjugated organic polymers and molecules have been extensively explored during the last years. The significant interest in the development of organic electronics results in part from the fact that this technology offers new or improved electroactive and opto-electronic features as compared to the inorganic counterparts. The organic electronic materials may be flexible andcan be also fabricated using printing devices. Other characteristics that make organic electronic materials promising as the active material in bioelectronics include:

Functionality which can easily be defined at the materials level, giving that chemical biosignals can be translated into electronics signatures or signals within the material itself.In the thin-layer state organic electronic materials are often transparent, which permits optical transmission imaging and use of various microscopy-based techniques when analyzing biological specimens interacting with the tool.Organic electronic materials are soft and can be (self-)organized to mimic biological structures.Organic conjugated materials conduct electrons as well as ions.Organic conjugated materials can be equipped with (bio-) molecular side-groups to promote cell viability.

Formulation of Catechin Hydrate Nanocapsule and Study of its Bioavailability

Drug delivery refers to approaches, formulations, technologies, and systems for transporting a pharmaceutical compound in the body as needed to safely achieve its desired therapeutic effect. It may involve scientific site targeting within the body, and also facilitating systemic pharmacokinetics; in any case, it is typically concerned with both quantity and duration of drug’s persistence in the system. Drug delivery is often executedvia a drug’s chemical formulation alone, but it may also involve in drug-devicecombination products. Drug delivery is a concept where much emphasis should be given to dosage form and route of administration.

The choice of the delivery systems is to allow the safe application of the drug with minimum losses. This suggests that the drug in theformulation must be chemically, physically and microbiologically stable. Side-effects of the drug and drug interactions should be avoided or minimized by the use of suitable drug delivery systems.

Synthesis of Aryl Tetralone Derivatives by Chalcone Route

Podophyllotoxin is a potent antimitotic agent. Podophyllin is a resinous extract of medicinal plants Podophyllum emodi and Podophyllum peltatum belonging to the family Berbideraceae in which the podophyllotoxin is one of the main constituent. The toxicity of podophyllotoxin liberates as diarrhea, nausea, vomiting. Hence modifications in podophyllotoxin structure are required to reduce its toxicity and to enhance its biological activity. The biologically active and lesscytotoxic new tetralone intermediates of podophyllotoxin have been synthesized. The modification of podophyllotoxin structure might enhance the biological activity with favorable solubility and reduced toxicity. Some synthesized analogues of podophyllotoxin showed better antibacterial activity. The structures of the synthesized new tetralone compounds were confirmed by IR, 1H-NMR, 13C-NMR and Mass spectral data. They will be screened for biological activities.

It was planned to synthesize analogues of podophyllotoxin by modifying lactone ring-A with some linked to ring A is replaced by dimethoxy, methoxy, methyl, H. Chalcones 3a-d were prepared by Claisen-Schmidt reaction of acetophenone 1a-dwith 3, 4, 5-trimethoxybenzaldehyde separately in the presence of potassiumhydroxide in water-ethanol mixture. Cyclopropyl ketones 4a-d was prepared in good yields by the reaction of chalcones 2a-d with diiodomethane in presence of Zn-Cu couple.

Conducting Polymers in Biological Systems

Electronics based on π-conjugated organic polymers and molecules have been extensively explored during the last years. The significant interest in the development of organic electronics results in part from the fact that this technology offers new or improved electroactive and opto-electronic features as compared to the inorganic counterparts. The organic electronic materials may be flexible andcan be also fabricated using printing devices. Other characteristics that make organic electronic materials promising as the active material in bioelectronics include.

Functionality which can easily be defined at the materials level, giving that chemical biosignals can be translated into electronics signatures or signals within the material itself.In the thin-layer state organic electronic materials are often transparent, which permits optical transmission imaging and use of variousmicroscopy-based techniques when analyzing biological specimens interactingwith the tool.Organic electronic materials are soft and can be (self-) organized to mimic biological structures.Organic conjugated materials conduct electrons as well as ions.Organic conjugated materials can be equipped with (bio-) molecular side-groups to promote cell viability.