International Journal of Drug Discovery and Medical Research

RECENT ADVANCES IN INDAZOLE-BASED DERIVATIVES OF VEGFR-2 KINASE INHIBITORS AS AN ANTI-CANCER AGENT

2022-12-23T09:45:44-05:00

Cancer is a leading cause of death worldwide, accounting for nearly 10 million deaths in 2020. Cancer continues increasing a serious threat to a people health. Cancer is the uncontrolled growth of abnormal cells in the body; cancer develops when the body’s normal control mechanism stops working. Many anti-cancer agents have been developed in recent year but survival rate does not satisfy. Therefore, through many efforts to develop novel anti-cancer agents to cover up for deficiency. Indazole is class of heterocyclic bioactive compounds, making structural modification on active indazole derivatives giving a variety of biological activities such as anti-depressant and antitumor anti-bacterial, anti-inflammatory, anti- hypertensive. These study through various literature focus on recent research of indazole derivatives as an anti-cancer will be useful for further development of Indazole base derivatives with new scaffold and high potency as anti-cancer agent. Recently many efforts have been taken for the development of indazole derivatives as vascular endothelial growth factor-2 (VEGFR-2) kinase inhibitors give good anti-tumor activities. Vascular endothelial growth factor-2 plays a role in tumor angiogenesis. Newly synthesized 2-(4-(1H-indazol-6-yl)-1H-pyrazol-1-yl) acetamide derivatives were designed as VEGFR-2 inhibitors based on scaffold hopping strategy. These compounds exhibited the excellent inhibitory in both vegfr-2 and tumor cells proliferation. A novel vegfr2 inhibitor CHMFL-VEGFR2-002 showed high selectivity among structurally closed kinases including PDGFRs, FGFRs, CSF1R etc. CHMFL-VEGFR2-002 given potent inhibitory activity against VEGFR2 kinase. CHMFL-VEGRF2-002 as a research tool for developing new function of VEGFR2 kinase as well as a potential antiangiogenetic agent for the cancer therapy.

MIFEPRISTONE PLUS MISOPROSTOL VS. MISOPROSTOL FOR ABORTION IN 2ND PREGNANCY

2022-12-23T10:26:19-05:00

Objective: The present study was conducted with the aim to assess and comparatively evaluate the safety and efficacy of mifepristone plus misoprostol versus only misoprostol in second trimester termination of pregnancy

Materials and Methods: The present study was conducted in Rajindra Hospital, Government medical college, Patiala. Group A received Tab Mifepristone 200mg orally. After 48 hours 400 µg of Tab Misoprostol was placed vaginally.Then every 4^th hourly 400 µg of misoprostol tab was placed vaginally upto maximum of five doses including the first dose or till expulsion of foetus. Group B received tablet misoprostol as mentioned in group A without prior mifepristone.After 24 weeks of gestation 200 µg of misoprostol was used. The subjects were closely monitored for any side effects. Induction abortion interval is the time period between insertions of first intravaginal misoprostol tablet to expulsion of products of expulsion. The process was considered failure if abortion failed to occur even after 12 hours of last dose of misoprostol.

Results : Mean time for onset of contractions was 4.53 hours in group A and 7.43 hours in group B. Mean time of onset of bleeding was 4.54 hours in group A and 7.39 hours in group B(P value <0.001). Induction abortion interval when calculated in both groups came out to be 8.12 hours in group A and 13.41 hours in group B which was statistically significant. Mean dose of misoprostol was 769.89 µg in group A and 1043.2 µg in group B Side effect profile was similar in both groups. Shivering was the most common side effect in both groups followed by diarrhea followed by nausea and vomiting. Side effects were not related to number of doses of misoprostol given and occurred in most of the subjects quite early after 2^nd or 3^rd dose. The number of subjects who needed check curettage were almost similar in both groups. Success rate was 97% in group A and 87% in group B. The subjects who were unsuccessful either had drug failure or had to discontinue misoprostol due to severity of side effects.

Conclusion: Mifepristone and misoprostol combination is better than misoprostol alone for second trimester termination of pregnancy. The time of onset of contractions, the time of onset of bleeding, Induction abortion interval, mean doses of misoprostol are reduced with the combination regimen. Success rate of combination regimen is more as compared to misoprostol only regimen.

BIOACTIVE POTENTIAL AND PHYTOPHARMACOLOGICAL ACTIVITY OF ACACIA CATECHU

2022-12-23T10:30:39-05:00

Acacia catechu is also known as Cutch tree, and black cutch heartwood tree. It has bitter and astringent taste. The chief phytoconstituents as catechi and epicatechin. Wood contains 50% tannins, mainly cattechutannic acid 20-35%, acacatechin 2-10%, catechins 13-33%, epicatechin 2.5%, isorhamnetin, quercetin, phlobatannins 25-33%, tannic acid 22-50%, catechu-red, gum 20-35%. It is used for teeth disorders, itching of skin, cough, anorexia, obesity, worm infestation, diabetes, fever, ulcers, leukoderma, and anaemia. Acacia catechu is the best herb for the management of internal as well as external health problems. The pharmacological activity of acacia catechu has been reported such as antiviral, antimicrobials, antioxidant, anti-inflammatory, antipyretic, antidiabetic and hepatoprotective etc.