Diverse Thiophenes as Scaffolds in Anti-cancer Drug Development: A Concise Review.

Thiophenes are one of the abundantly found heterocyclic ring systems in many biologically active compounds. Moreover, various substituted thiophenes exert numerous pharmacological actions on account of their isosteric resemblance with compounds of natural origin, thus rendering them with diverse actions like antibacterial, antifungal, antiviral, anti-inflammatory, analgesic, antiallergic, hypotensives, etc. In this review, we specifically explore the chemotherapeutic potential of a variety of structures consisting of thiophene scaffolds as prospective anticancer agents.

Diversified Synthetic Pathway of 1, 4-Dihydropyridines: A Class of Pharmacologically Important Molecules.

The current review discusses the different synthetic pathways for one of the most important and interesting heterocyclic ring systems, 1,4-dihydropyridine. This cyclic system depicts diverse pharmacological action on several receptors, channels, and enzymes. Dihydropyridine moiety plays an important role in several calcium-channel blockers. Moreover, it has been exploited for the treatment of a variety of cardiovascular diseases due to its potential antihypertensive, anti-angina, vasodilator, and cardiac depressant activities. Furthermore, it also shows antibacterial, anticancer, anti-leishmanial, anticoagulant, anticonvulsant, anti-tubercular, antioxidant, antiulcer, and neuroprotective properties. Several reports have demonstrated dihydropyridine derivatives as a potentiator of cystic fibrosis transmembrane conductance regulator protein, potent antimalarial agent and HIV-1 protease inhibitor. Herein, we have briefly reviewed different novel chemistry and the synthesis of 1,4-dihydropyridine.

Bioanalytical method development and its application to pharmacokinetics studies on Simvastatin in the presence of piperine and two of its synthetic derivatives.

Piperine has been widely used as a bioenhancer. Simvastatin belongs to a group of medicines known as statins. It acts by inhibiting HMG CoA reductase and acts primarily as a hypolipidemic agent. In this study some derivatives of Piperine were synthesized. They were studied for their bioenhencing effect (10 mg kg-1) and this effect was compared with that of Piperine. The pharmacokinectic profile of Simvastatin alone and in combination with Piperine and Piperine derivatives were investigated by validated HPLC method as per USFDA guidelines. It was seen that the two synthesized derivatives of Piperine significantly improved the bioavailability of Simvastatin in Wistar rats. The 5-(benzo) [1,3]dioxol-5-yl)-N-(pyridin-4-yl)penta-2,4-dienamide was better amongst the synthesized in increasing the bioavailability of Simvastatin in Wistar rat.

1, 4-Dihydropyridines: a class of pharmacologically important molecules.

The 1, 4-dihydropyridines (DHPs), a class of drugs possess a wide variety of biological and pharmacological actions. It represents one of the most important groups of calcium-channel modulating agents and has experienced widespread use in the treatment of cardiovascular disease which includes antihypertensive, antianginal, vasodilator and cardiac depressants activities. It also shows antibacterial, anticancer, antileishmanial, anticoagulant, anticonvulsant, antitubercular, antioxidant, antiulcer, CFTR, antimalarials, neuroprotection properties, HIV-1 protease inhibitors, antifertility activities and many more. There are many drugs available in market which contains 1, 4-dihydropyridines ring as basic scaffold. Basic motive of this review is to disclose various therapeutic applications of 1, 4-dihydropyridine derivatives reported by other researchers during their research work in 2001 to 2011.

1,4-Dihydropyridines: A Class of Pharmacologically Important Molecules.

The 1,4-dihydropyridines (DHPs), a class of drugs possess a wide variety of biological and pharmacological actions, have represented one of the most important groups of calcium-channel modulating agents and have experienced widespread use in the treatment of cardiovascular disease which include antihypertensive, antianginal, vasodilator and cardiac depressants activities. It also shows antibacterial, anticancer, antileishmanial, anticoagulant, anticonvulsant, antitubercular, antioxidant, antiulcer, CFTR, antimalarials, neuroprotection properties, HIV-1 protease inhibitors, antifertility activities and many more. There are many marketed drugs which contain 1,4-dihydropyridines ring as basic scaffold. In this review, attempts have been made to disclose various therapeutic applications of 1,4-dihydropyridine derivatives which have been reported during the period of 2001-2011.

Thiazolidinediones : A class of pharmacologically important molecules.

Thiazolidinediones are one of the important chemical class of heterocyclic compounds that can be synthesized from thiourea and chloroacetic acid. Thiazolidinedione ring upon substitution with different scaffolds like benzylidene, methoxynapthalene, ester, benzyl shows wide spectrum of pharmacological activities like antihyperglycemic, anticancer, aldose reductase (ALR) inhibition, anti-inflammatory, PGDH inhibition, Keratin pigmentation, antioxidant and antimicrobial activity. Many drugs are marketed as well as removed amongst thiazolidinediones. Present study includes review on synthesis and various pharmacological activities associated with thaizolidinediones.