IN SILICO AND IN VITRO STUDIES OF BENZOHYDRAZIDE ANALOGUES AS POTENT ANDROGEN RECEPTOR ANTAGONIST

摘要

In the late 1950s,the Prostate Cancer(PCa)is commonly diagnosed in men.The growth of PCa is largely due to the stimulation of the AR by androgens.Currently,hormonal therapy,surgery,and oral chemotherapeutic drugs are the main therapeutic for the treatments of prostate cancer.About 1,74,650 men were diagnosed and 31,620 deaths due to PCa in the U.S reported by the American Cancer Society.1 Androgens,testosterone,and Dihydrotestosterone binds with the ligand binding domain(LBD)of the androgen receptor(AR)and incite the growth of prostate cancer.There are few available drugs for androgen receptor antagonists such as bicalutamide,flutamide,and enzalutamide are used to prevent the activation of the androgen receptor.Currently,Sipuleucel-T is used as a drug for the immunotherapy to inhibit PCa.To reduce toxicity,lower the doses,and minimize drug resistance,numerous studies are enduring for the development of target based drugs.2 Recently,benzohydrazide derivative was reported for antifungal-antibacterial,anti-inflammatory,cruzipain inhibitor.Entamoeba histolytic,antimalarial,anti-tuberculosis activities,and as EGFR Tyrosine Kinase Inhibitors.Thus,benzohydrazides are the important moieties which play a vital role in effective inhibition against different cancer cell line HepG2,HeLa,A549,and MCF-7.