Synthesis of Substituted 1,2,4-Triazole Containing Novel Small Molecules by Using Microwave

Green chemistry finds its most promising use in the synthesis of compounds using ecologically friendly, non-hazardous, non-irritant, gentle, and reproducible catalysts and solvents. The adoption of green chemistry approaches has recently been shown to significantly reduce chemical waste and reaction times in a number of organic synthesis processes. The objective of this research work is to develop an eco-friendly method for the Substituted 1,2,4-Triazole containing novel small molecules. The approach makes use of acid as starting material on reaction with hydrazine forms Acetyl-hydrazide. On condensation with nitrile and subsequent ring closure forms substituted 1,2,4-Triazole derivatives.  This research work describes the synthesis of thirty-two unique 1,2,4-triazole containing novel small molecules. It has been shown that this technique is superior to other synthetic methods in terms of reaction time, yield, and energy efficiency along with use of green chemistry and microwave. &nbsp

Natural sources as potential anti-cancer agents: A review

Natural products remain an important source of new drugs, new drug leads and new chemical entities. The plant based drug discovery resulted mainly in the development of anticancer agents including plants (vincristine, vinblastine, etoposide, paclitaxel, camptothecin, topotecan and irinotecan), marine organisms (citarabine, aplidine and dolastatin 10) and micro-organisms (dactinomycin, bleomycin and doxorubicin). Beside this there is numerous agents identified from fruits and vegetables can used in anticancer therapy. The agents include curcumin (turmeric), resveratrol (red grapes, peanuts and berries), genistein (soybean), diallyl sulfide (allium), S-allyl cysteine (allium), allicin (garlic), lycopene (tomato), capsaicin (red chilli), diosgenin (fenugreek), 6-gingerol (ginger), ellagic acid (pomegranate), ursolic acid (apple, pears, prunes), silymarin (milk thistle), anethol (anise, camphor, and fennel), catechins (green tea), eugenol (cloves), indole-3-carbinol (cruciferous vegetables), limonene (citrus fruits), beta carotene (carrots), and dietary fiber. In this review active principle derived from natural products are offering a great opportunity to evaluate not only totally new chemical classes of anticancer agents, but also novel lead compound and potentially relevant mechanisms of action. Keywords: Cancer, vincristin, vinblastin, fruit, vegetables

Natural sources as potential anti-cancer agents: A review

Natural products remain an important source of new drugs, new drug leads and new chemical entities. The plant based drug discovery resulted mainly in the development of anticancer agents including plants (vincristine, vinblastine, etoposide, paclitaxel, camptothecin, topotecan and irinotecan), marine organisms (citarabine, aplidine and dolastatin 10) and micro-organisms (dactinomycin, bleomycin and doxorubicin). Beside this there is numerous agents identified from fruits and vegetables can used in anticancer therapy. The agents include curcumin (turmeric), resveratrol (red grapes, peanuts and berries), genistein (soybean), diallyl sulfide (allium), S-allyl cysteine (allium), allicin (garlic), lycopene (tomato), capsaicin (red chilli), diosgenin (fenugreek), 6-gingerol (ginger), ellagic acid (pomegranate), ursolic acid (apple, pears, prunes), silymarin (milk thistle), anethol (anise, camphor, and fennel), catechins (green tea), eugenol (cloves), indole-3-carbinol (cruciferous vegetables), limonene (citrus fruits), beta carotene (carrots), and dietary fiber. In this review active principle derived from natural products are offering a great opportunity to evaluate not only totally new chemical classes of anticancer agents, but also novel lead compound and potentially relevant mechanisms of action. Keywords: Cancer, vincristin, vinblastin, fruit, vegetables

Development and Validation of Stability Indicating Reverse Phase High Performance Liquid Chromatographic Method for estimation of Donepezil HCl from bulk drug

Stability of Donepezil Hydrochloride(DONE) was investigated using stability indicating Reverse phase high performance liquid chromatography (RP-HPLC) utilizing C-18 column and mobile phase containing Acetonitrile:Water (pH 3.5)  in ratio of 40:60 at flow rate of 1 ml min-1. Peaks of donepezil and degradation products were well resolved at retention times < 7 min. Stability was performed in 0.1N hydrochloric acid, 0.1N sodium hydroxide, 3 % hydrogen peroxide, neutral, photolytic and dry heat conditions. Fast hydrolysis was seen in alkaline condition as compared to oxidative and neutral conditions. Methods was validated with respect to linearity, precision, accuracy, specificity and robustness LOQ and LOD. It was also found to be stability indicating, and therefore suitable for the routine analysis of Donepezil hydrochloride in the pharmaceutical formulation

Synthesis of new 2,2-dimethyl-2H-chromen derivatives as potential anticancer agents

874-880The synthesis of some new heterocyclic derivatives comprising imidazothaidiazole, diaryl ketone and chromen as starting compound has been reported. The new series of chromen analogues have been synthesized. The reaction has been monitored by Thin Layer Chromatography (TLC) using suitable mobile phase. The Rf values have been compared and the melting points of derivatives determined. Further, these derivatives have been characterized and confirmed by IR, 1H NMR and mass spectral (MS) studies. All the selected compounds submitted to National Cancer Institute (NCI) for in vitro anticancer assay have been evaluated for their anticancer activity

3-{2-[(3-{(E)-2-[4-(Dimethyl­amino)­phen­yl]ethen­yl}quinoxalin-2-yl)­oxy]eth­yl}-1,3-oxazolidin-2-one monohydrate

In the title compound, C23H24N4O3·H2O, the 1,3-oxazoline ring is nearly planar [maximum deviation = 0.059 (2) Å] and its mean plane is twisted by 30.12 (8)° with respect to the quinoxaline fused-ring system; the benzene ring is nearly coplanar with the quinoxaline fused-ring system [dihedral angle = 2.52 (2)°]. The water mol­ecule of crystallization is hydrogen-bond donor to an N atom of the quinoxaline ring system as well as an O atom of the oxazolinone unit, the two hydrogen bonds generating a chain running along the c axis

2D QSAR STUDIES ON THE DIFFERENTIAL INHIBITION OF ALDOSE REDUCTASE BY FLAVONIODS COMPOUNDS:A COMPARATIVE STUDY

A quantitative structure activity relationship study of  66 molecules was performed using MLR(Multiple Linear Regression) and PCR (Principal component Analysis) of aldose reductase by flavonoids compounds.Various descriptors, topological indices were used to characterize flavonoids molecules.In the developed model MLR is giving vary significant results wheras PCR  has revealed some important information. Keywords: Flavonoids, aldose reuctase, QSAR, Multiple Linear Regression, Principle Component Regressio

Synthesis of new 2,2-dimethyl-2H-chromen derivatives as potential anticancer agents

The synthesis of some new heterocyclic derivatives comprising imidazothaidiazole, diaryl ketone and chromen as starting compound has been reported. The new series of chromen analogues have been synthesized. The reaction has been monitored by Thin Layer Chromatography (TLC) using suitable mobile phase. The Rf values have been compared and the melting points of derivatives determined. Further, these derivatives have been characterized and confirmed by IR, 1H NMR and mass spectral (MS) studies. All the selected compounds submitted to National Cancer Institute (NCI) for in vitro anticancer assay have been evaluated for their anticancer activity.

N

The title mol­ecule, C(12)H(12)FN(3)O(2)S, shows a short intra­molecular S⋯O contact of 2.682 (18) Å. The dihedral angle between the thia­diazole ring and the benzene ring is 86.82 (11)°. In the crystal, N—H⋯O and C—H⋯O hydrogen bonds generate an R (2) (1)(6) graph-set motif between adjacent mol­ecules. Pairs of futher C—H⋯O hydrogen bonds form inversion dimers with R (2) (2)(8) ring motifs. These combine to generate a three-dimensional network and stack the mol­ecules along the b axis