70441-03-1Relevant articles and documents
Design, Synthesis and Biological Investigation of Flavone Derivatives as Potential Multi-Receptor Atypical Antipsychotics
Chen, Yin,Gao, Lanchang,Hao, Chao,Jin, Jian,Liu, Bi-Feng,Liu, Xin,Ma, Ru,Xiong, Jiaying,Yang, Zhengge,Zhang, Guisen
, (2020/09/18)
The design of a series of novel flavone derivatives was synthesized as potential broad-spectrum antipsychotics by using multi-receptor affinity strategy between dopamine receptors and serotonin receptors. Among them, 7-(4-(4-(6-fluorobenzo[d]isoxazol-3-yl) piperidin- 1-yl) butoxy)-2,2-dimethylchroman-4-one (6j) exhibited a promising preclinical profile. Compound 6j not only showed high affinity for dopamine D2, D3, and serotonin 5-HT1A, 5-HT2A receptors, but was also endowed with low to moderate activities on 5-HT2C, α1, and H1 receptors, indicating a low liability to induce side effects such as weight gain, orthostatic hypotension and QT prolongation. In vivo behavioral studies suggested that 6j has favorable effects in alleviating the schizophrenia-like symptoms without causing catalepsy. Taken together, compound 6j has the potential to be further developed as a novel atypical antipsychotic.
Synthesis and antitubercular activity of amino alcohol fused spirochromone conjugates
Mujahid,Gonnade,Yogeeswari,Sriram,Muthukrishnan
supporting information, p. 1416 - 1419 (2013/03/14)
A series of 21 new amino alcohol fused spirochromone conjugates have been synthesized, characterized with analytical data and evaluated their antimycobacterial activity against Mycobacterium tuberculosis (virulent strain H37Rv) in vitro. Some of the compounds exerted significant inhibition, in particular, compound 4f found to be the most potent derivative exhibiting MIC = 3.13 μg/mL.
Development of a benzopyran-containing androgen receptor antagonist to treat antiandrogen-resistant prostate cancer
Oh, Sangmi,Nam, Hye Jin,Park, Jongmin,Beak, Sung Hee,Park, Seung Bum
experimental part, p. 529 - 533 (2010/12/25)
Antagonizing cancer 2 000 druglike small molecules were screened and a scaffold identified as a potentially novel androgen receptor antagonist framework. A focused library of 19 derivatives was then synthesized and evaluated in vitro against LNCaP prostate cancer cell line. A novel compound (6 f) was identified as a promising lead compound for the further development of new therapeutic agents against hormone-refractory prostate cancer.