72101-53-2Relevant academic research and scientific papers
A structure—activity relationship study of bis-benzamides as inhibitors of androgen receptor—coactivator interaction
Lee, Tae-Kyung,Ravindranathan, Preethi,Sonavane, Rajni,Raj, Ganesh V.,Ahn, Jung-Mo
supporting information, (2019/08/07)
The interaction between androgen receptor (AR) and coactivator proteins plays a critical role in AR-mediated prostate cancer (PCa) cell growth, thus its inhibition is emerging as a promising strategy for PCa treatment. To develop potent inhibitors of the
Preparation method of oxybuprocaine hydrochloride
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Paragraph 0042; 0043; 0053; 0054, (2017/08/31)
The invention discloses a preparation method of oxybuprocaine hydrochloride. The preparation method includes following steps: in the presence of alkali I, subjecting 3-hydroxy-4-ethyl nitrobenzoate and bromobutane to electrophilic substitution reaction to obtain 3-butoxy-4-ethyl nitrobenzoate; under alkaline condition, enabling 3-butoxy-4-ethyl nitrobenzoate to be in hydrolysis reaction, and adjusting pH value of a system after hydrolysis reaction to 1-3 to obtain 3-butoxy-4-nitrobenzoic acid; in the presence of alkali II, subjecting the 3-butoxy-4-nitrobenzoic acid and diethylamino ethyl chloride to electrophilic substitution reaction to obtain 4-nitro-2-butoxy nitrobenzoic acid-2-(diethylamino) ethyl ester, and subjecting the 4-nitro-2-butoxy nitrobenzoic acid-2-(diethylamino) ethyl ester to reduction reaction under action of ferric trichloride and hydrazine hydrate to obtain oxybuprocaine hydrochloride. 3-hydroxy-4-ethyl nitrobenzoate is adopted as a raw material to obtain a target product through four steps of conventional reaction; each step of reaction does not need high-pressure condition, and needed raw materials are all conventional compounds, so that the preparation method is easy to obtain and low in cost.
Estrogen receptor coregulator binding modulators (ERXs) effectively target estrogen receptor positive human breast cancers
Raj, Ganesh V.,Sareddy, Gangadhara Reddy,Ma, Shihong,Lee, Tae-Kyung,Viswanadhapalli, Suryavathi,Li, Rui,Liu, Xihui,Murakami, Shino,Chen, Chien-Cheng,Lee, Wan-Ru,Mann, Monica,Krishnan, Samaya Rajeshwari,Manandhar, Bikash,Gonugunta, Vijay K.,Strand, Douglas,Tekmal, Rajeshwar Rao,Ahn, Jung-Mo,Vadlamudi, Ratna K.
supporting information, (2017/09/18)
The majority of human breast cancer is estrogen receptor alpha (ER) positive. While anti-estrogens/aromatase inhibitors are initially effective, resistance to these drugs commonly develops. Therapy-resistant tumors often retain ER signaling, via interaction with critical oncogenic coregulator proteins. To address these mechanisms of resistance, we have developed a novel ER coregulator binding modulator, ERX-11. ERX-11 interacts directly wiTheR and blocks the interaction between a subset of coregulators with both native and mutant forms of ER. ERX-11 effectively blocks ER-mediated oncogenic signaling and has potent anti-proliferative activity against therapy-sensitive and therapy-resistant human breast cancer cells. ERX-11 is orally bioavailable, with no overt signs of toxicity and potent activity in both murine xenograft and patient-derived breast tumor explant models. This first-in-class agent, with its novel mechanism of action of disrupting critical protein-protein interactions, overcomes the limitations of current therapies and may be clinically translatable for patients with therapy-sensitive and therapy-resistant breast cancers.
