Aims: The present work focus to identify a new class of BRCA-1 mimetics that work differently from conventional anti estrogens. Background: It was found that breast cancer susceptibility protein1 (BRCA1) binds to estrogen receptor alpha (ERα) and inhibits its activity by direct interaction between domains within the amino terminus of BRCA1 and the carboxy terminus of ER alpha. Objective: A novel class of hybrids having coumate and benzimidazolone scaffolds were designed to mimic BRCA1 protein, supressing the tumor activity of breast cancer cell. Method: The in silico molecular docking studies of the designed ligands were performed on BRCA-1 binding cavity of ER alpha. The designed hybrids which have given significant docking scores and having optimum binding interactions with key residues been selected for synthesis and in-vitro assay. Result: The compounds NY1 and NY2 exhibited significant effects on suppressing MDA-MB-231 cells in the concentration of 24 µg/ml and 44 µg/ml respectively. Conclusion: The developed coumate-benzimidazolone hybrids may act as Leads as BRCA-1 mimetics. Other: However,to explore their BRCA-1 mimetics potential, additional experimental data are needed.

: Conventional drug discovery is a time overwhelming and expensive expedition with super less clinical preference achievement proportion intended for breast cancer therapy. Even if numerous novel approaches to the conformation of drugs have been introduced for breast cancer therapy, they have up till now to be implemented in clinical practice. This tempting strategy, facilitate a remarkable chance to take the entire benefit of existing drugs. Despite drug repurposing significantly decrease the investigational period and cost, it has got many objections and issues. Scaffold repurposing is the approach that procures a novel significance on the decrepit motto of “to commencement with a pristine drug” Hence, ourselves move into a probable and nearer approach, the exploitation of scaffolds originally developed for other purposes as well anti-tumour activity. In this review, we summarize the different drugs and scaffolds used in breast cancer therapy.

Background: : Epilepsy is a genuine neurological turmoil that effects around 50 million individuals around the world. Practically 30% of epileptic patients experience the ill effects of pharmaco-obstruction, which is related with social seclusion, subordinate conduct, low marriage rates, joblessness, mental issues and diminished personal satisfaction. At present accessible antiepileptic drugs have a restricted viability, and their negative properties limit their utilization and cause challenges in patient administration. Gabapentin 1-(aminomethyl)cyclohexane acetic acid, Gbp , (trade name Neurontin), a structural analog of γ-aminobutyric acid (GABA), BCS class 3 drug with having permeability issues. Objective: This work was an attempt to formulate and characterize a new approach to treat epilepsy by targeting to Phospholipase A2 Enzyme through Nanostructured Lipid Carrier. Methods: Docking studied carried out using Accelrys Discovery studio 4.1 Client and gabapentin and phosphotidylcholine were conjugated through chemical conjugation. Nanostructured lipid carrier (NLC) was prepared using hot homogenization technique. Results: The libdock score of Gabapentin- Phosphotidylcholine conjugate (192.535) were found to be more than Gabapentin (77.1084) and Phosphotidylcholine (150.212). For the optimized formulation the particle size (50.08), zeta potential (-1.48), PDI (0.472) and entrapment efficiency (77.8) was observed. The NLC was studies for in-vitro drug release studies and release kinetics. Finally found that the drug release from the NLC followed Higuchi release kinetic and the mode of drug release from the NLC was found to be Non- Fickian diffusion. Conclusion: The formulated Nanostructured lipid carrier of Gabapentin-Phosphotidylcholine conjugate may be able to use to prevent seizure.

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A sulphatase inhibitor 667 COUMATE is in clinical trials for estrogen-positive breast cancer therapy for postmenopausal women, while there are a number of similar sulphatase inbitors are under development. Schiff's bases are versatile pharmacophores in which the N atom involves in hydrogen bonding with active cell centers interfering in normal cell biology. A library of novel coumate analogues with Schiff bases were designed, and structural based drug design was performed with human estrogen receptor (PDB ID: 2IOG) (Already reported). Based on the in-silico outcomes, seven coumate-schiff bases were synthesized. The compounds were obtained in good yield. The novelty had been ascertained by sci inder software. The synthesized molecules were consistent with their assigned spectra such as IR, Mass and NMR spectral data which con irmed their formation. The cytotoxicity study was performed by MTT assay for all the synthesized compounds. Most of the compounds have good IC 50 values (below 100 µg/ml).Two of the synthesized compounds COU-2 and COU-5 have shown good IC 50 values such as 19µg/ml and 39µg/ml, respectively. They suppressed the proliferation of estrogen receptor overexpressed MCF-7 cells.