7182-09-4Relevant articles and documents
CARBAZOLE-CONTAINING AMIDES, CARBAMATES, AND UREAS AS CRYPTOCHROME MODULATORS
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Paragraph 0394, (2015/10/28)
The subject matter herein is directed to carbazole-containing amide, carbamate, and urea derivatives and pharmaceutically acceptable salts or hydrates thereof of structural formula I wherein the variable R1, R2, R3, R4, R5, R6, R7, A, D, E, G, J, L, M, Q, a, and b are accordingly described. Also provided are pharmaceutical compositions containing the compounds of formula I to treat a Cry-mediated disease or disorder, such as diabetes, complications associated with diabetes, Cushing's syndrome, NASH, NAFLD, asthma, and COPD.
Antiandrogenic, maspin induction, and antiprostate cancer activities of tanshinone IIA and its novel derivatives with modification in ring A
Liu, Weiguo,Zhou, Jinming,Geng, Guoyan,Shi, Qingwen,Sauriol, Francoise,Wu, Jian Hui
supporting information; experimental part, p. 971 - 975 (2012/03/11)
Expression of metastatic suppressor maspin is lost in advanced prostate cancer. Clinically relevant mutations in androgen receptor (AR) convert antiandrogens into AR agonists, promoting prostate tumor growth. We discovered tanshinone IIA (TS-IIA) is a potent antagonist of mutated ARs and induces maspin expression through AR. TS-IIA suppressed AR expression and induced apoptosis in LNCaP cells. Syntheses of TS-IIA derivatives (1-9) revealed that the 4,4-dimethyl group at ring A is important for TS-IIA's antiandrogenic and maspin induction activities.
The total synthesis of (-)-aurafuron A
Hartmann, Olaf,Kalesse, Markus
supporting information; experimental part, p. 3064 - 3067 (2012/09/08)
The first total synthesis of (-)-aurafuron A is presented. It features a Suzuki cross-coupling reaction and a high yielding anionic aldol addition as central carbon skeleton building reactions. The synthesis confirms the proposed structure including its configuration and allows for detailed SAR studies.
Synthesis of syn-4,6-dimethyldodecanal, the male sex pheromone and trail-following pheromone of two species of the termite Zootermopsis
Ghostin,Bordereau,Braekman
scheme or table, p. 560 - 568 (2011/05/12)
Recently, we reported that syn-4,6-dimethyldodecanal is the male sex pheromone and the trail-following pheromone of the Termopsidae Zootermopsis nevadensis and Zootermopsis angusticollis. In this article, we describe the syntheses of the mixture of the fo
Synthesis, discovery and preliminary SAR study of benzofuran derivatives as angiogenesis inhibitors
Chen, Yuan,Chen, Shaopeng,Lu, Xin,Cheng, Hao,Ou, Yingyong,Cheng, Huimin,Zhou, Guo-Chun
scheme or table, p. 1851 - 1854 (2009/11/30)
A series of benzofuran derivatives were synthesized and evaluated against HUVEC proliferation. Among these compounds, compound 32 exhibited good inhibitory activity and remarkable selectivity to HUVEC. Our current data suggested that array order of methyl, acrylate and carboxylate groups in benzofuran scaffold is the basic requirement for inhibitory activity against HUVEC proliferation. These results demonstrated that benzofuran scaffold represents a promising structural core to discover a new class of active and selective angiogenesis inhibitors.
Synthesis and polymerization of methyl 3-methylcyclobutene-1-carboxylate
Kitayama, Tatsuki,Kawauchi, Takehiro,Ueda, Nori,Kniep, Carina S.,Shin, Won Suk,Padias, Anne B.,Hall Jr.
, p. 1591 - 1598 (2007/10/03)
A new icyclobutene monomer, methyl 3-methylcyclobutene-1-carboxylate (MMCB), has been synthesized and polymerized by radical and anionic initiators. The synthesis started from a [2 + 2] cycloaddition of N-(1-propenyl)piperidine to methyl acrylate, followed by methylation and treatment with base to yield the monomer. Free radical polymerization of MMCB led to low yields of low molecular weight polymers, probably due to chain transfer at the allytic hydrogen. However, p-methoxystyrene, styrene and methyl methacrylate gave high molecular weight copolymers with MMCB in high yields. Anionic homopolymerization with tert-butyllithium (t-BuLi), t-BuLi/bis(2,6-di-tert-butylphenoxy)ethylaluminum, lithium bis(trimethylsilyl)amide, and potassium bis(trimethylsilyl)amide in toluene at 0 and -78°C proceeded smoothly and gave polymers in high yields. NMR and IR analyses of the polymers suggested that the polymerization proceeds via addition mechanism without ring-opening. Thermal properties of the polymers are also described briefly. In contrast to MMCB, methyl 3,3-dimethylcyclobutene-1-carboxylate MDCB did not polymerize due to excessive steric hindrance.
