Anticancer and Molecular Docking Studies of 1-(5-substituted phenyl) isoxazol-3-yl)-5-phenyl-1H-tetrazoles

Cancer a leading cause of human mortality worldwide is characterised by the unseemly growth of cellular mass and signalled through the enlargement of stress. Management of cancer treatment is still buried andhas been recently alerting the need to discover a drug molecule with lesser side effects. The objective of the present study is to explore the anticancer activity and docking studies of 1-(5-substituted phenyl) isoxazol-3-yl)-5-phenyl-1H-tetrazole derivatives. The compounds were evaluated for in-vitroanticancer activity under the drug discovery program of National Cancer Institute (NCI), USA. Only seven compounds were selected and screened for anticancer activity at a single high dose (10-5M) using NCI 60 cancer cell lines. Among all the selected compounds, 4band 4iexhibited significant anticancer activity against Leukemia cell lines. Molecular docking studies for the 5-phenyl-1-(5-substituted phenylisoxazol-3-yl)-1H-tetrazole analogues was done by Schrodinger software. Docking results stated that the compounds 4band 4ihas good dock score among the other derivatives which shows good binding efficiency towards receptor

Stroke at moderate altitude.

OBJECTIVE: To know the clinical profile, presence of various risk factors for stroke at moderate altitude and to study its relationship with hypertension and polycythemia at moderate altitude. METHODS: We analyzed the data of 100 patients, consecutively admitted to a hospital situated at an moderate altitude of 2200 meters MSL of Sub-Himalayan ranges and studied the age, gender, geographical distribution, clinical features and presence of various risk factors in relation to stroke. This is not only the first study conducted in Himachal Pradesh but also first study in India to be conducted at moderate altitude (2000-3000 meters MSL). RESULTS: Males outnumbered females (66% males, 34% females) with rural predominance (73% rural, 27% urban). Cerebral infarction (69%) was more common but primary intracerebral haemorrhage (26%) was more common than found in the West. Hypertension (62%) and smoking (60%) were most common risk factors present and polycythemia was not a significant risk factor at this altitude. CONCLUSION: Incidence of stroke was found to be lower than the study conducted at low altitude. incidence of various types of stroke was similar to other Indian studies. The combination of opposite effects of decreased hypertension and increased haematocrit could not be demonstrated at this altitude and smoking was more common than in other studies and other risk factors prevalent were same as that for low altitude.

Mesenteric leiomyoma in infancy.

Leiomyoma of the mesentery is an uncommon tumor. This has been documented in adults and children. However, there is no such case reported in an infant, which is being presented in this report.

Quantitative analysis of nuclear area variation in benign and malignant breast fine needle aspirates.

The measurement of nuclear area was carried out in 30 benign and 32 malignant breast lumps using Omnicon Alpha 500 Image Analyzer. The mean nuclear area of duct cells in malignant group was greater (157.6 +/- 58.64 sq.microns with a peak around 140 sq.microns) and more heterogenous within and amongst cases than observed in duct cells from most of the cases of fibroadenoma (85.05 ae 14.2 sq.microns with a peak around 80 sq.microns). Taking into consideration 110 sq.microns as a differentiating limit, a significant difference was observed between benign and malignant conditions (p). Similarly taking 118 sq.microns as differentiating limit duct cell carcinomas could be divided into two groups i.e. 9(28.1%) cases of small nuclear type with a range of 80-118 sq.microns and 23(71.9%) cases of large nuclear type with a range of 118-320 sq microns .6(18.8%) cases with small nuclei had an overlap with fibroadenoma. Although 13(72.2%) cases of large nuclear type carcinomas had lymph node metastasis as against 4(44.4%) in small nuclear group, the difference was not statistically significant.

Calmodulin-like activity in mycobacteria.

Calmodulin-like activity has been reported for the first time in mycobacterial species, namely Mycobacterium tuberculosis BCG and M. smegmatis ATCC 14468. The activity was mainly located in the soluble fraction of the mycobacterial cells, Radioimmunoassay revealed maximum levels of calmodulin in young growing cells (early logarithmic phase of growth). Calmodulin-dependent phosphodiesterase activation assay revealed low activity (22%) of partially purified calmodulin either due to insufficient amount of calmodulin to activate phosphodiesterase or due to the presence of some factors interfering with the assay. Calmodulin antagonists, viz. trifluoperazine and phenothiazine, significantly inhibited the 32Pi incorporation into mycobacterial phospholipids. Similar inhibition was observed when EGTA (which removes calcium) was added to the medium. Significant inhibition of 32Pi incorporation in the presence of calmodulin antagonists suggested the involvement of calmodulin in mycobacterial phospholipid metabolism.

Role of ultrasonography in patients with normal oral cholecystogram.

The role of real-time ultrasonography was evaluated in 50 randomly selected cases with a strong clinical suspicion of gallbladder diseases and normal oral cholecystogram. Of these, 13(26%) cases showed abnormalities on ultrasonography.

Comparative study of ultrasonography and oral cholecystography in evaluation of gallbladder and biliary tract diseases.

50 cases, aged between 14-60 years, clinically suspected of gall-bladder and biliary tract diseases were evaluated by ultrasonography and oral cholecystography. Ultrasound with a preliminary radiograph of gallbladder region, proved to be more sensitive and reliable procedure than oral cholecystography. Besides providing ancillary information regarding adjacent anatomic structures, it also guided the surgeon to decide preoperatively about the mode of surgery to be employed. Further, from the present study it can be fairly concluded that ultrasound should be used as the primary screening technique for evaluating gallbladder and biliary tract diseases, after plain skiagram of the gallbladder region, since it is non-invasive, more sensitive than OCG and is devoid of use of contrast media and its toxicity.

Serodiagnosis of tuberculosis using purified mycobacterial proteins.

With a view to detect specific M. tuberculosis infection, mycobacterial proteins were purified initially by ammonium sulphate precipitation followed by ion-exchange chromatography. Out of the three fractions, namely P1, P2 and P3 precipitated with increasing concentrations (0-25%, 26-65% and 66-100% respectively) of ammonium sulphate, P2 fraction was found to be more immunoreactive. P2 fraction proteins were further fractionated into five fractions by salt gradient using DEAE-cellulose DE-52 ion-exchange chromatography. Immunoreactivity against tuberculous patients sera of all the fractions was assessed using ELISA test. The last fraction (DE-V) eluted with high salt concentration was found to have a more specific immunoreactive set of proteins within the range of 55 kD to 67 kD molecular weight. Multiple non-specific proteins were distributed in all the other fractions. ELISA test using P2 fraction proteins against tuberculous patients sera showed significantly higher (p less than 0.01) titre even in the absence of any other bacteriological evidence. DE-V fraction of P2 proteins was found to have a significantly high specificity for detecting M. tuberculosis infection in clinically confirmed and suspected tuberculous patients indicating its application in the diagnosis of the disease.

A comparative study between hysterosalpingography and laparoscopy in case of infertility.

From the present study it can be concluded that both the procedures have their own importance and no one can substitute the other, in diagnosing all the diseases. HSG has been found to be more rewarding in cases of abnormalities of the lumen of uterus and fallopian tubes for their patency. On the other hand laparoscopy has been more rewarding for the abnormalities of the surface of uterus, fallopian tubes and ovaries. It is suggested that in all the cases of infertility both the procedures should be done and the HSG should be done first followed by laparoscopy.

Cervical intraepithelial glandular neoplasia diagnosis and significance in relation to squamous precancerous lesions.

The endocervical epithelium of histologically confirmed dysplasia and carcinoma-in-situ cases of cervix uteri was examined for the presence or absence of intraepethelial glandular Neoplasia (CIGN). Results from 80 cases were compared with equal number of controls who were being operated for reasons other than Neoplasia. In the present communication we have used the criteria of Nuclear enlargement and elongation, hyperchromasia, stratification, increased N/C ratio, pleomorphism and dence clumping to distinguish CIGN from normal endocervical epithelial lining using the criteria mentioned above we recorded CIGN in eleven cases of test group while in two of controls which implied a statistically significant (p less than .5) association of CIGN with case series as compared to controls. Among the test group; 1, 2 (15.3%), 3 (23%) and 5 (10%) cases were associated with mild, moderate, sever dysplasia and carcinoma-in-situ respectively.

Role of ultrasonography in non-visualised gallbladder on oral cholecystography.

Real-time ultrasonography was done in 30 cases of non-visualised gallbladder on oral cholecystography. Surgico-pathological correlation revealed that a specific diagnosis indicating true pathology is possible preoperatively on ultrasonography.