Microwave-assisted synthesis, characterization and cytotoxic studies of novel estrogen receptor α ligands towards human breast cancer cells.

A new, simple, and microwave-assisted, solution-phase T3P®-DMSO mediated method for the preparation of a novel class of estrogen receptor alpha (ERα) ligands based on the 2-phenylquinoline scaffold was developed. Furthermore, the novel ERα ligands were tested for their bioactivity against ERα-positive and ERα-negative cell lines. The ligand (entry 4), with amine and nitro group substitution at C4 position, displayed significant cytotoxicity against MCF-7 and HepG2 cells with an IC50 value of 6 and 11µM, respectively. On the other hand, ERα-negative cells displayed resistance to quinolines induced cytotoxicity with an IC50 value >100Mm and they does not induce cytotoxicity in normal breast epithelial cells. Molecular docking analyses suggest a consistent binding mode for these ERα ligands in the ligand binding domain of the human ERα and predict the ligands to occupy the hydrophobic cavity in a similar fashion as estradiol or GW2368.

Radiation-free Insertion of Distal Interlocking Screw in Tibial and Femur Nailing: A Simple Technique.

BACKGROUND: Distal interlocking screw insertion in intramedullary nailing of long-bone fracture is a challenging task for orthopedic surgeons. It is difficult particularly when the surgeon is in his learning stage or when image intensifier is not available. We describe a radiation-free technique of distal interlocking screw insertion which is easy and practicable. MATERIALS AND METHODS: In this technique, a same length nail is placed over the skin (outer nail) and through its distal-most screw hole, a 3.2 mm drill bit is inserted to drill the distal locking screw hole of the intramedullary nail (inner nail). With a small skin incision over the distal screw holes, the distal-most screw hole is identified; the bone window overlying the screw hole is widened with an awl and a locking bolt is inserted with a washer under direct visualization. The other distal interlocking screw is simply drilled by matching the other three holes of the outer and inner nails. We have operated 86 patients (39 femoral shaft fracture and 47 tibial shaft fracture) in 1 year where this technique was used. There were 41 open fracture and 45 closed fracture. RESULTS: Within 6 months of follow-up, bony union was achieved in 36 of 39 femur fractures and 45 of 47 tibial fractures. No unwanted complications were observed during the postoperative period and in follow-up. CONCLUSION: This method of radiation-free distal interlocking screw insertion is simple and can be used in third world country where image intensifier facility is not available. However, surgeons are encouraged to use image intensifier facility where the facility is available.