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Scope of the Problem
Published in Jason W. Birkett, John N. Lester, Endocrine Disrupters in Wastewater and Sludge Treatment Processes, 2002
Many EDCs compete with estradiol (female sex hormone) for the estrogen receptor, others compete with dihydrotestosterone (male sex hormone) for the androgen receptor. Hence, these substances exert a feminizing or masculinizing effect on the endocrine system. Substances that mimic these feminizing effects are known as “estrogenic;” those mimicking masculinizing effects are termed “androgenic.” It therefore follows that an antiandrogenic substance, such as flutamide, inhibits the biological actions of androgens by binding to and thus inactivating the androgen receptor of target tissue. An antiestrogenic substance, such as tamoxifen, inhibits the biological actions of estrogens by binding to and thus inactivating the estrogen receptor of target tissue.
Study of physicochemical properties of flutamide-loaded Ocimum basilicum microspheres with ex vivo mucoadhesion and in vitro drug release
Published in Particulate Science and Technology, 2018
Pradum Pundlikrao Ige, Rohit Ravindra Badgujar, Pankaj Padmakar Nerkar, Hitendra Shaligram Mahajan, Raju Onkar Sonawane, Sanjay Javarilal Surana
Flutamide is a potent inhibitor of testosterone stimulated prosthetic DNA synthesis and prevents the prostate cancer cells to grow. It occurs as a pale yellow, crystalline powder of acicular particle shape categorized in BCS class II and half life about 6 h. It is practically insoluble in water but is freely soluble in methanol and ethanol. Mainly because of poor solubility in water (1.43 mg/mL), limited dissolution rate and bioavailability (49%), the low bioavailability of flutamide after oral formulations may be due to poor wettability, low aqueous solubility, extensive first pass hepatic effect and low concentration at the absorption area. Therefore, developing novel formulations that mitigate solubility and dissolution will produce higher concentrations of flutamide in solution at the absorption site and hence may overcome the solubility-mediated poor bioavailability (Posti, Katila, and Kostiainen 2000; Zuo et al. 2002; Aizawa et al. 2003; Gronberg 2003; Fizazi and Navone 2005; Hodgson et al. 2007; Sahoo, Abbas, and Li 2008; Elgindy et al. 2010; Anitha et al. 2012; Piccionello et al. 2012; Samy 2012; Elzoghby et al. 2013; Milone et al. 2013).
Methods for the synthesis of N-aryl sulfonamides from nitroarenes: an overview
Published in Journal of Sulfur Chemistry, 2021
Jingjing Xia, Kehua Zhang, Evan Abdolkarim Mahmood
Drawing inspiration from this work, Chen, Wu, and co-workers developed a practical and efficient transition-metal-free three-component reductive coupling reaction between nitroarenes 34, arylboronic acids 35, and K2S2O5 under an atmosphere of air at 130°C (Scheme 15) [50]. The reactions proceeded in the presence of nBu4NCl/K2CO3 combination as a catalytic system in MeCN to afford the corresponding N-aryl sulfonamides 36 in moderate to excellent yields, ranging from 39% to 95%. The protocol was compatible with a diverse range of important functional groups including Fluoro, chloro, bromo, iodo, amino, cyano, ether, thioether, acid, ketone, ester, and amid functionalities, which are very useful for further synthetic transformations. Besides, both aromatic and heteroaromatic substrates were tolerated. Notably, the process can also be enlarged to gram scale without sacrificing the yield or outcome of the methodology. The mechanistic course of this sequential C−S and S−N bonds formation reaction is similar to the one depicted in Scheme 14. Concurrently, in a closely related investigation, the group of Fan-Wu reported the synthesis of thirty N-(hetero)aryl sulfonamides in moderate to excellent yields (44–92%) via three-component coupling of the respective nitro(hetero)arenes, (hetero)arylboronic acids, and K2S2O5 using 20 mol% of Cu(MeCN)4PF6 as a catalyst, 10 mol% of 1,10-phenanthroline as a ligand, and 2 equiv. of iPrOH as the reductant in NMP [51]. Noteworthy, the protocol was successfully applied on the gram-scale with little effect on the yield. Additionally, the procedure was served for the late-stage modification of Flutamide, an anti-prostatic cancer drug.